CN101365681B

CN101365681B - Iminopropene compound and use thereof

Info

Publication number: CN101365681B
Application number: CN200680052079.6A
Authority: CN
Inventors: 伊藤滋之; 岩田淳
Original assignee: Sumitomo Chemical Co Ltd
Current assignee: Sumitomo Chemical Co Ltd
Priority date: 2005-12-01
Filing date: 2006-11-08
Publication date: 2013-01-02
Anticipated expiration: 2026-11-08
Also published as: ZA200804378B; CN101365681A

Abstract

The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

Description

Iminopropene compound and uses thereof

Technical field

The present invention relates to Iminopropene compound and the purposes aspect desinsection thereof.

Background technology

Up to now, a lot of sterilants and found many effectively compounds of Control pests have been developed.Yet their activity is not always effective.Therefore, there is the further demand that exploitation is had the active new compound of insect control.

Invention is described

This invention is intended to provide and have the superior active compound of insect control.

For finding to have the superior active compound of insect control, the inventor conducts extensive research, and found that the Iminopropene compound that is represented by formula (I) has superior insect and controls active.Therefore, the present invention is accomplished.

Namely the invention provides following aspect:

The Iminopropene compound or its salt that are provided by formula (I):

Wherein,

X represents OX ¹, NX ²X ³, SX ⁴, S (O) _mX ⁵, Si (X ⁶) ₃Or N=C (X ⁷) ₂,

Y represents OY ¹, NY ²Y ³, SY ⁴, SO ₂Y ⁵Or N=C (Y ⁶) ₂,

Z represents cyano group, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁹¹) Z ^A, C (=O) OZ ^B, C (=Q ⁹²) NZ ^DZ ^E, SO ₂Z ^F, NZ ^GZ ^H, OZ ^KOr N=C (Z ^I) ₂,

X ¹The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ¹¹) X ^A1, C (=O) OX ^B1, C (=Q ¹²) NX ^D1X ^E1, SO ₂X ^F1, NX ^G1X ^H1Or N=C (X ^I1) ₂,

X ²The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ²¹) X ^A2, C (=O) OX ^B2, C (=Q ²²) NX ^D2X ^E2, SO ₂X ^F2, NX ^G2X ^H2, N=C (X ^I2) ₂, OX ^K2Or cyano group,

X ³Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ³¹) X ^A3, C (=O) OX ^B3, C (=Q ³²) NX ^D3X ^E3Or SO ₂X ^F3,

Perhaps, X ²And X ³The nitrogen representative ring structure that is bonded to each other with them,

X ⁴The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁴¹) X ^A4, C (=O) OX ^B4, C (=Q ⁴²) NX ^D4X ^E4Or S (O) _nX ^F4,

X ⁵The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

X ⁶The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional lower alkoxy that replaces

X ⁷Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the OX that replaces ^L7, SX ^M7Or NX ^G7X ^H7,

Perhaps, the carbon representative ring structure that is bonded to each other with them,

Y ¹The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁵¹) Y ^A1, C (=O) OY ^B1, C (=Q ⁵²) NY ^D1Y ^E1, S (O) _pY ^F1Or N=C (Y ^I1) ₂,

Y ²The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁶¹) Y ^A2, C (=O) OY ^B2, C (=Q ⁶²) NY ^D2Y ^E2, SO ₂Y ^F2, NY ^G2Y ^H2, N=C (Y ^I2) ₂, OY ^K2Or cyano group,

Y ³Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁷¹) Y ^A3, C (=O) OY ^B3, C (=Q ⁷²) NY ^D3Y ^E3Or SO ₂Y ^F3,

Y ⁴The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁸¹) Y ^A4, C (=O) OY ^B4, C (=Q ⁸²) NY ^D4Y ^E4Or S (O) _qY ^F4,

Y ⁵The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Y ⁶Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the OY that replaces ^L6, SY ^M6Or NY ^G6Y ^H6,

X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^AThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces,

X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

X ^D1, X ^D2, X ^D3, X ^D4, Y ^D1, Y ^D2, Y ^D3, Y ^D4And Z ^DRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OG that replaces ^A1,

With

X ^E1, X ^E2, X ^E3, X ^E4, Y ^E1, Y ^E2, Y ^E3, Y ^E4And Z ^ERepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe nitrogen representative ring structure that is bonded to each other with them,

X ^F1, X ^F2, X ^F3, Y ^F1, Y ^F2, Y ^F3And Z ^FThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

X ^F4And Y ^F4The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

X ^G1, X ^G2, X ^G7, Y ^G2, Y ^G6And Z ^GRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^G1) G ^A1, C (=O) OG ^B1, C (=Q ^G2) NG ^D1G ^E1Or SO ₂G ^F1,

With

X ^H1, X ^H2, X ^H7, Y ^H2, Y ^H6And Z ^HRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, X ^G1And X ^H1, X ^G2And X ^H2, X ^G7And X ^H7, Y ^G2And Y ^H2, Y ^G6And Y ^H6, and Z ^GAnd Z ^HThe nitrogen representative ring structure that is bonded to each other with them,

X ^I1, X ^I2, Y ^I1, Y ^I2And Z ^IRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the OG that replaces ^A2, SG ^A3Or NG ^G1G ^H1,

X ^K2, Y ^K2And Z ^KThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^K1) G ^A2, C (=O) OG ^B2, C (=Q ^K2) NG ^D2G ^E2Or SO ₂G ^F2,

X ^L7, X ^M7, Y ^L6And Y ^M6Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

G ^A1, G ^A2And G ^A3Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

G ^A1And G ^A2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

G ^B1And G ^B2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

G ^D1And G ^D2Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OG that replaces ^D1,

With

G ^E1And G ^E2Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, G ^D1And G ^E1, and G ^D2And G ^E2The nitrogen representative ring structure that is bonded to each other with them,

G ^F1And G ^F2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

G ^G1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^Ga) G ^A1-1, C (=O) OG ^B1-1, C (=Q ^Gb) NG ^D1-1G ^E1-1Or SO ₂G ^F1-1,

With

G ^H1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, G ^G1And G ^H1The nitrogen representative ring structure that is bonded to each other with them,

G ^D1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

G ^A1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

G ^B1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

G ^D1-1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OL that replaces

With

G ^E1-1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, G ^D1-1And G ^E1-1The nitrogen representative ring structure that is bonded to each other with them,

G ^F1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces

L represents hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Q ¹¹, Q ¹², Q ²¹, Q ²², Q ³¹, Q ³², Q ⁴¹, Q ⁴², Q ⁵¹, Q ⁵², Q ⁶¹, Q ⁶², Q ⁷¹, Q ⁷², Q ⁸¹, Q ⁸², Q ⁹¹, Q ⁹², Q ^G1, Q ^G2, Q ^K1, Q ^K2, Q ^GaAnd Q ^GbRepresent independently of one another oxygen or sulphur,

M represents integer 1 or 2,

N, p and q represent integer 0 or 2 independently of one another,

At this, 1) if X is benzoyloxy and Y is methoxyl group, then Z is not 2-(benzamido) vinyl,

2) if X ²Be methyl, then X ³Not methyl,

3) if X is methoxyl group and Y is trimethyl fluoride sulfonyl oxygen base, then Z is not 3-vinyl oxygen base propyl group (after this being called compound (I));

Comprise compound (I) as activeconstituents or the insect-killing composition of its salt and inert support; With the method for Control pests, it comprises the compound (I) of using significant quantity or the step of its salt insect or insect habitat.

Embodiments of the present invention

At first, the embodiment of compound (I) illustrates according to [1]-[33] hereinafter.

The Iminopropene compound or its salt that are provided by formula (I):

Wherein,

X, Y and Z as above define.

2) if X ²Be methyl, then X ³Not methyl,

3) if X is methoxyl group and Y is trimethyl fluoride sulfonyl oxygen base, then Z is not 3-vinyl oxygen base propyl group.

According to the compound of [1], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹And X ²Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom and X ^A2Be the optional low alkyl group that replaces), NX ^G1X ^H1Or N=C (X ^I1) ₂,

X ⁴And X ⁵Be independently of one another the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical or the C (=Q that replaces ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces),

X ³Be hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, X ²And X ³Form ring structure with its nitrogen that is bonded to each other),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical or the N=C (Y that replaces ^I1) ₂,

Y ²And Y ⁴Be independently of one another the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Y ³Be hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

Z is the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, C (=O) OZ ^B(wherein, Z ^BBe the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

SO ₂Z ^F(wherein, Z ^FBe the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces)

NZ ^GZ ^H(wherein, Z ^GAnd Z ^HBe hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces independently of one another

Perhaps, form ring structure with its nitrogen that is bonded to each other),

OZ ^K(wherein, Z ^KBe the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces), or

N=C (Z ^I) ₂(wherein, Z ^IBe hydrogen atom independently of one another, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces

Perhaps, form ring structure with its carbon that is bonded to each other).

The compound of compounds [2], wherein

X is SX ⁴

(wherein, X ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

Y is OY ¹, NY ²Y ³Or SY ⁴

Perhaps, form ring structure with its nitrogen that is bonded to each other),

N=C (Z ^I) ₂(wherein, Z ^IBe hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces independently of one another

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [3], wherein

X is SX ⁴

(wherein, X ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade alkenyl that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Be the optional low alkyl group that replaces, the optional aryl that replaces, optional heterocyclic radical or the N=C (Y that replaces ^I1) ₂(Y ^I1Be low alkyl group or aryl independently of one another),

Y ²And Y ³Be independently of one another the optional low alkyl group that replaces or the optional aryl that replaces,

Y ⁴Be the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional low-grade alkynyl that replaces or the optional heterocyclic radical that replaces),

The rudimentary alkylidene that Z replaces for the optional low alkyl group that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, lower alkoxycarbonyl, the optional aromatic hydrocarbons alkylsulfonyl that replaces, lower alkoxy that replaced by aryl and that replace by the optional amino that replaces of low alkyl group, fragrant-oxyl, by at least one aryl or by at least one aryl is amino.

According to the compound of [4], wherein

X is SX ⁴

(wherein, X ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) is chosen wantonly the heterocyclic radical that replaces by the optional aryl that replaces of at least one halogen, low alkyl group or lower alkoxy and (2) by at least one halogen; Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen atom, (2) nitro, (3) low alkyl group, (4) low-grade halogenated alkyl and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more low alkyl groups),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Serve as reasons and be selected from the low alkyl group of the optional replacement of at least one following substituting group: (1) chooses the aryl that replaces wantonly by at least one low alkyl group, and (2) are by the optional aryl that replaces of at least one halogen and (3) heterocyclic radical by at least one halogen replacement; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) nitro, (4) low alkyl group, (5) amino, (6) lower alkylthio, (7) low alkyl group alkylsulfonyl, (8) low-grade cycloalkyl, (9) aryl, (10) lower alkoxycarbonyl, (11) lower alkoxy, (12) heterocyclic radical, (13) low-grade alkylidene and (14) low-grade alkylidene dioxy base; Heterocyclic radical; Or amino by the optional rudimentary alkylidene that replaces of at least one aryl,

Y ²The optional low alkyl group that replaces of at least one aryl of serving as reasons, or aryl,

Y ³Be low alkyl group,

Y ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) by the optional aryl that replaces of at least one halogen, (2) are by the optional aryl that replaces of at least one low alkyl group and (3) low-grade cycloalkyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy and (4) elementary halogenated alkoxy; By being selected from the optional heterocyclic radical that replaces of following one or more independently substituting groups: (1) low alkyl group, the heterocyclic radical that (2) low-grade halogenated alkyl and (3) are replaced by at least one halogen; By the optional low-grade alkenyl that replaces of at least one halogen; Or low-grade alkynyl),

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) nitro, (3) cyano group, (4) low alkyl group, (5) lower alkoxy, (6) low-grade halogenated alkyl, (7) low-grade cycloalkyl and (8) fragrant-oxyl; Heterocyclic radical; Lower alkoxycarbonyl; The aromatic hydrocarbons alkylsulfonyl; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; By the lower alkoxy of at least one aryl replacement, or amino by the rudimentary alkylidene of at least one aryl replacement.

According to the compound of [2], wherein

X is OX ¹

(wherein, X ¹Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the NX that replaces ^G1X ^H1Or N=C (X ^I1) ₂),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, or N=C (Y ^I1) ₂,

Y ²And Y ⁴Be independently of one another the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces

Y ³Be hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces)

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [6], wherein

X is OX ¹

(wherein, X ¹Be the aryl of the optional low alkyl group that replaces, optional replacement, the optional low-grade cycloalkyl that replaces, two elementary alkyl amido, the optional rudimentary alkylidene amino that replaces, or the optional rudimentary ring alkylidene that replaces is amino),

Y is OY ¹Or SY ⁴

(wherein, Y ¹And Y ⁴Be independently of one another the optional low alkyl group that replaces, or the optional aryl that replaces),

Z is the optional aryl that replaces or the optional heterocyclic radical that replaces.

The compound of compounds [7], wherein

X is OX ¹

(wherein, X ¹Be the low alkyl groups that replaced by one or more at least one aryl that is selected from the optional replacement of following independent substituting group: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, (4) lower alkoxycarbonyl, (5) low-grade alkane acidyl, (6) lower alkylthio, (7) aryl, (8) cyano group, (9) nitro and (10) alkylenedioxy group; Amino by the optional alkylidene that replaces of at least one aryl; Rudimentary ring alkylidene is amino; Or two elementary alkyl amido),

Y is OY ¹Or SY ⁴

(wherein, Y ¹The low alkyl group that at least one aryl replaces of serving as reasons, or by being selected from the optional aryl that replaces of following one or more independently substituting groups: halogen and low alkyl group,

Y ⁴The serve as reasons optional low alkyl group that replaces of at least one aryl or aryl),

Z serves as reasons and is selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) rudimentary cycloalkylthio, (3) hydroxyl, (4) by the optional low alkyl group that replaces of at least one aryl, (5) low-grade alkenyl, (6) by the optional lower alkoxy that replaces of at least one halogen, (7) low-grade alkane acidyl oxygen base, (8) by at least one low alkyl group or the optional aryl that replaces of halogen, (9) heterocyclic radical, (10) lower alkylthio, (11) low alkyl group sulfinyl, (12) low alkyl group alkylsulfonyl, (13) arylthio, (14) elementary alkoxy carbonyl, (15) low-grade alkane acidyl, (16) aromatic hydrocarbons carbonyl, (17) low-grade alkynyl, (18) low-grade alkylidene dioxy base and (19) low-grade alkylidene; Or heterocyclic radical.

The compound of compounds [2], wherein

X is NX ²X ³, or S (O) ₂X ⁵

(wherein, X ²And X ⁵Be independently of one another the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, or C (=Q ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces),

X ³Be hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces)

Y is OY ¹, NY ²Y ³Or SY ⁴

Z is the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, C (=O) OZ ^B(wherein, Z ^BBe the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [9], wherein

X is NX ²X ³, or S (O) ₂X ⁵

(wherein, X ²Be the optional low alkyl group that replaces, the optional aryl that replaces, or C (=Q ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces),

X ³Be the optional low alkyl group that replaces, or the optional aryl that replaces,

Perhaps, X ²And X ³Form ring structure with its nitrogen that is bonded to each other,

X ⁵Be the optional aryl that replaces),

Y is OY ¹, or SY ⁴

(wherein, Y ¹And Y ⁴Be the optional aryl that replaces),

Z is the optional aryl that replaces.

According to the compound of [10], wherein

X is NX ²X ³, or S (O) ₂X ⁵

(wherein, X ²The low alkyl group that at least one aryl replaces of serving as reasons, aryl or low-grade alkane acidyl,

X ³Be low alkyl group or aryl,

Perhaps, X ²And X ³Form piperidino-(1-position only) or morpholino with its nitrogen that is bonded to each other,

X ⁵Be aryl),

Y is OY ¹, or SY ⁴

(wherein, Y ¹And SY ⁴Be aryl),

Z is aryl.

According to the compound of [2], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹And X ²Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces), NX ^G1X ^H1, or N=C (X ^I1) ₂,

X ⁴And X ⁵Be independently of one another the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, or C (=Q ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces),

X ³Be hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces

Y is OY ¹

Z is cyano group, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces

C (=O) OZ ^B(wherein, Z ^BBe the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [12], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be the low alkyl group of optional replacement, the aryl of choosing replacement wantonly, the optional low-grade cycloalkyl that replaces, two elementary alkyl amido, the rudimentary alkylidene amino of choosing replacement wantonly, the optional rudimentary ring alkylidene amino that replaces,

X ²Be the optional low alkyl group that replaces, the optional aryl that replaces, or C (=Q ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces),

X ³Be the optional low alkyl group that replaces or the optional aryl that replaces,

X ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade alkenyl that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces, or the optional heterocyclic radical that replaces, X ⁵Be the optional aryl that replaces),

Y is OY ¹

(wherein, Y ¹Be the optional low alkyl group that replaces, the optional aryl that replaces, optional heterocyclic radical or the N=C (Y that replaces ^I1) ₂(Y ^I1Be low alkyl group or aryl independently of one another)

Z is the optional aryl that replaces, or the optional heterocyclic radical that replaces.

According to the compound of [13], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be the low alkyl groups that replaced by one or more at least one aryl that is selected from the optional replacement of following independent substituting group: (1) halogen, (2) low alkyl group and (3) lower alkoxy; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, (4) lower alkoxycarbonyl, (5) low-grade alkane acidyl, (6) lower alkylthio, (7) aryl, (8) cyano group, (9) nitro and (10) alkylenedioxy group; Low-grade cycloalkyl; Amino by the optional alkylidene that replaces of at least one aryl; Rudimentary ring alkylidene is amino; Or two elementary alkyl amido,

X ²Low alkyl group, the aryl that at least one aryl replaces of serving as reasons, or low-grade alkane acidyl,

X ³Be low alkyl group or aryl,

X ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) is chosen wantonly the heterocyclic radical that replaces by the optional aryl that replaces of at least one halogen, low alkyl group or lower alkoxy and (2) by at least one halogen; Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen atom, (2) nitro, (3) low alkyl group, (4) low-grade halogenated alkyl and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more low alkyl groups,

X ⁵Be aryl),

Y is OY ¹,

(wherein, Y ¹For by one or more optional low alkyl groups that replace of following substituting group that are selected from: (1) by the optional aryl that replaces of at least one low alkyl group, the heterocyclic radical that (2) are replaced by at least one halogen by the optional aryl that replaces of at least one halogen and (3); By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) nitro, (4) low alkyl group, (5) amino, (6) lower alkylthio, (7) low alkyl group alkylsulfonyl, (8) low-grade cycloalkyl, (9) aryl, (10) lower alkoxycarbonyl, (11) lower alkoxy, (12) heterocyclic radical, (13) low-grade alkylidene dioxy base and (14) low-grade alkylidene; Heterocyclic radical; Or amino by the optional rudimentary alkylidene that replaces of at least one aryl),

Z serves as reasons and is selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) hydroxyl, (4) by optional low alkyl group or the aryl that replaces of at least one halogen, (5) low-grade alkenyl, (6) by the optional lower alkoxy that replaces of at least one halogen, (7) low-grade alkane acidyl oxygen base, (8) by at least one halogen or the optional aryl that replaces of low alkyl group, (9) heterocyclic radical, (10) lower alkylthio, (11) low alkyl group sulfinyl, (12) low alkyl group alkylsulfonyl, (13) arylthio, (14) elementary alkoxy carbonyl, (15) low-grade alkane acidyl, (16) aromatic hydrocarbons carbonyl, (17) low-grade alkynyl, (18) rudimentary cycloalkylthio, (19) low-grade alkylidene dioxy base, (20) low-grade alkylidene, (21) low-grade cycloalkyl, (22) aryloxy and (23) nitro; Heterocyclic radical.

According to the compound of [2], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹And X ²Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom, and X ^A2Be the optional low alkyl group that replaces), NX ^G1X ^H1Or N=C (X ^I1) ₂,

Y is SY ⁴

(wherein, Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces)

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [15], wherein

X is OX ¹, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be optional aryl, the X that replaces ⁴Be the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces, and X ⁵Be the optional aryl that replaces),

Y is SY ⁴

(wherein, Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

Z is the optional low alkyl group that replaces, the optional aryl that replaces, lower alkoxycarbonyl, the optional aromatic hydrocarbons alkylsulfonyl that replaces, lower alkoxy that replaced by aryl and that replace by the optional amino that replaces of low alkyl group, fragrant-oxyl, by at least one aryl, or amino by the optional rudimentary alkylidene that replaces of at least one aralkyl.

According to the compound of [16], wherein

X is OX ¹, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹The expression aryl,

X ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of optional at least one aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, (4) nitro; Or heterocyclic radical,

X ⁵Be aryl),

Y is SY ⁴

(wherein, Y ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) by the optional aryl that replaces of at least one halogen, (2) are by the optional aryl that replaces of at least one low alkyl group and (3) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy and (4) elementary halogenated alkoxy; By being selected from the optional heterocyclic radical that replaces of following one or more independently substituting groups: (1) low alkyl group, the heterocyclic radical that (2) low-grade halogenated alkyl and (3) are replaced by at least one halogen; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Or low-grade alkynyl),

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Lower alkoxycarbonyl; The optional aromatic hydrocarbons alkylsulfonyl that replaces; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; Lower alkoxy by at least one aryl replacement; Or amino by the rudimentary alkylidene of at least one aryl replacement.

According to the compound of [15], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

Y is SY ⁴

(wherein, Y ⁴Be the optional aryl that replaces or the optional heterocyclic radical that replaces),

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [18], wherein

X is OX ¹, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹The optional aryl that replaces of expression,

X ⁴Be the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, or the optional aryl that replaces,

X ⁵Be the optional aryl that replaces),

Y is SY ⁴

According to the compound of [19], wherein

X is OX ¹, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹The expression aryl,

X ⁴Low alkyl group, the low-grade cycloalkyl that at least one aryl replaces of serving as reasons, or by optional aryl or the lower alkoxy that replaces of at least one low alkyl group,

X ⁵Be aryl),

Y is SY ⁴

(wherein, Y ⁴Serving as reasons, at least one is selected from the optional aryl that replaces of following substituting group: (1) halogen, (2) chosen wantonly the lower alkoxy that replaces by at least one halogen by the optional low alkyl group that replaces of at least one halogen and (3), or by one or more optional heterocyclic radicals that replace of following substituting group that are selected from: (1) is by the optional low alkyl group that replaces of at least one halogen, and (2) are by the heterocyclic radical of at least one halogen replacement)

The Z low alkyl group that at least one halogen replaces of serving as reasons; By one or more optional aryls that replace of following substituting group that are selected from: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Lower alkoxycarbonyl; The optional aromatic hydrocarbons alkylsulfonyl that replaces; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; Lower alkoxy by at least one aryl replacement; Or amino by the rudimentary alkylidene of at least one aryl replacement.

According to the compound of [15], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

Y is SY ⁴

(wherein, Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, or senior alkynyl),

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [21], wherein

X is SX ⁴

(wherein, X ⁴Be the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces, or the optional heterocyclic radical that replaces),

Y is SY ⁴

(wherein, Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, optional low-grade alkenyl, the senior thiazolinyl that replaces, or the optional low-grade alkynyl that replaces),

Z is the optional aryl that replaces.

According to the compound of [22], wherein

X is SX ⁴

(wherein, X ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of optional at least one aryl that replaces of following one or more substituting groups: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Low-grade cycloalkyl; By one or more optional aryls that replace of following substituting group that are selected from: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, and (4) nitro; Or heterocyclic radical),

Y is SY ⁴

(wherein, Y ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) is by the optional aryl that replaces of at least one halogen and (2) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Or low-grade alkynyl),

The Z optional aryl that replaces of at least one low alkyl group of serving as reasons.

According to the compound of [2], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

Y is NY ²Y ³

(wherein, Y ²Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces

Perhaps, form ring structure with its nitrogen that is bonded to each other),

Perhaps, form ring structure with its carbon that is bonded to each other).

According to the compound of [24], wherein

X is SX ⁴

(wherein, X ⁴Be the optional aryl that replaces),

Y is NY ²Y ³

(wherein, Y ²Be the optional low alkyl group that replaces, and Y ³Be the optional low alkyl group that replaces, or the optional aryl that replaces),

Z is the optional aryl that replaces.

According to the compound of [25], wherein

X is SX ⁴

(wherein, X ⁴The optional aryl that replaces of at least one halogen or low alkyl group of serving as reasons),

Y is NY ²Y ³

(wherein, Y ²The optional low alkyl group that replaces of at least one aryl and Y serve as reasons ³Be low alkyl group or aryl),

Z is aryl.

According to the compound of [2], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

Y is OY ¹, NY ²Y ³Or SY ⁴

Z is the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, C (=O) OZ ^B(wherein, Z ^BBe the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

SO ₂Z ^F(wherein, Z ^FBe the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

NZ ^GZ ^H(wherein, Z ^GAnd Z ^HBe hydrogen atom, the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces independently of one another, the optional aryl that replaces or the optional heterocyclic radical that replaces,

Perhaps, form ring structure with its nitrogen that is bonded to each other),

OZ ^K(wherein, Z ^KBe the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces), or

N=C (Z ^I) ₂(wherein, Z ^IBe hydrogen atom, the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces independently of one another,

Perhaps, form ring structure with its nitrogen that is bonded to each other).

According to the compound of [27], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be the optional low alkyl group that replaces, the optional aryl that replaces, the optional low-grade cycloalkyl that replaces, two elementary alkyl amido, amino, the X of the amino or optional rudimentary ring alkylidene that replaces of the optional rudimentary alkylidene that replaces ²Be the optional low alkyl group that replaces, the optional aryl that replaces, or C (=Q ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom and X ^A2Be the optional low alkyl group that replaces),

X ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade alkenyl that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces, and X ⁵Be the optional aryl that replaces),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Be the optional low alkyl group that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, or N=C (Y ^I1) ₂, (Y ^I1Independent is low alkyl group or aryl), Y ²And Y ³Be independently of one another the optional low alkyl group that replaces or the optional aryl that replaces, and Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

Z chooses the low alkyl group that replaces, the optional aryl that replaces, the heterocyclic radical of choosing replacement wantonly, lower alkoxycarbonyl, the optional aromatic hydrocarbons alkylsulfonyl that replaces, amino that replaced by aryl and chosen wantonly replacement by low alkyl group wantonly; and fragrant-oxyl, the lower alkoxy that replaced by at least one aryl, or amino by the optional rudimentary alkylidene that replaces of at least one aralkyl.

According to the compound of [28], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

X ³Be low alkyl group or aryl,

X ⁴Serve as reasons and be selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) low alkyl group and (3) lower alkoxy; By the optional low alkyl group that replaces of optional at least one heterocyclic radical that replaces of at least one halogen; Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) nitro, (3) low alkyl group, (4) junior alkyl halides, and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more low alkyl groups,

X ⁵Be aryl),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹For by one or more optional low alkyl groups that replace of following substituting group that are selected from: (1) by the optional aryl that replaces of at least one low alkyl group, the heterocyclic radical that (2) are replaced by at least one halogen by the optional aryl that replaces of at least one halogen and (3); By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) nitro, (4) low alkyl group, (5) amino, (6) lower alkylthio, (7) low alkyl group alkylsulfonyl, (8) low-grade cycloalkyl, (9) aryl, (10) lower alkoxycarbonyl, (11) lower alkoxy, (12) heterocyclic radical, (13) low-grade alkylidene and (14) low-grade alkylidene dioxy base; Heterocyclic radical; Or amino by the optional rudimentary alkylidene that replaces of at least one aryl,

Y ³Be low alkyl group,

Y ⁴For by one or more optional low alkyl groups that replace of following substituting group that are selected from: (1) by the optional aryl that replaces of at least one halogen, (2) are by the optional aryl that replaces of at least one low alkyl group and (3) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy and (4) elementary halogenated alkoxy; By being selected from the optional heterocyclic radical that replaces of following one or more independently substituting groups: (1) low alkyl group, the heterocyclic radical that (2) low-grade halogenated alkyl and (3) are replaced by at least one halogen; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Or low-grade alkynyl),

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) hydroxyl, (4) by optional low alkyl group or the aryl that replaces of at least one halogen, (5) low-grade alkenyl, (6) by the optional lower alkoxy that replaces of at least one halogen, (7) low-grade alkane acidyl oxygen base, (8) by at least one alkyl or the optional aryl that replaces of halogen, (9) heterocyclic radical, (10) lower alkylthio, (11) low alkyl group sulfinyl, (12) low alkyl group alkylsulfonyl, (13) arylthio, (14) elementary alkoxy carbonyl, (15) low-grade alkane acidyl, (16) aromatic hydrocarbons carbonyl, (17) low-grade alkynyl, (18) rudimentary cycloalkylthio, (19) low-grade alkylidene dioxy base, (20) low-grade alkylidene and (21) nitro; Heterocyclic radical; Lower alkoxycarbonyl; The aromatic hydrocarbons alkylsulfonyl; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; By the lower alkoxy of at least one aryl replacement, or amino by the rudimentary alkylidene of at least one aryl replacement.

According to the compound of [2], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be the low alkyl group of optional replacement, the aryl of choosing replacement wantonly, the optional low-grade cycloalkyl that replaces, two elementary alkyl amido, the rudimentary alkylidene amino of choosing replacement wantonly or the optional rudimentary ring alkylidene amino that replaces,

X ²Be the optional low alkyl group that replaces, optional aryl or the C (=Q that replaces ²¹) X ^A2(wherein, Q ²¹Be Sauerstoffatom and X ^A2Be the optional low alkyl group that replaces),

X ⁴Be the optional low alkyl group that replaces, senior thiazolinyl, the optional low alkyl group that replaces, the optional low-grade cycloalkyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces, X ⁵Be the optional aryl that replaces),

Y is OY ¹, NY ²Y ³Or SY ⁴

(wherein, Y ¹Be the optional low alkyl group that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, or N=C (Y ^I1) ₂(Y ^I1Independent is low alkyl group or aryl,

Y ²Be the optional aryl that replaces,

Y ³Be the optional low alkyl group that replaces or the optional aryl that replaces,

Y ⁴Be the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional low-grade alkynyl that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces),

Z is the optional low alkyl group that replaces, the optional aryl that replaces, the optional heterocyclic radical that replaces, lower alkoxycarbonyl, the optional aromatic hydrocarbons alkylsulfonyl that replaces, lower alkoxy that replaced by aryl and that replace by the optional amino that replaces of low alkyl group, fragrant-oxyl, by at least one aryl, or amino by the optional rudimentary alkylidene that replaces of at least one aralkyl.

According to the compound of [30], wherein

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

(wherein, X ¹Be the low alkyl groups that replaced by one or more at least one aryl that is selected from the optional replacement of following independent substituting group: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Or by being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, (4) lower alkoxycarbonyl, (5) lower alkylthio, (6) aryl, (7) cyano group, (8) nitro and (9) alkylenedioxy group

X ³Be low alkyl group or aryl,

X ⁴For by one or more optional low alkyl groups that replace of following substituting group that are selected from: the heterocyclic radical that (1) is replaced by at least one halogen by at least one halogen or the optional aryl that replaces of low alkyl group and (2); Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) nitro, (3) low alkyl group, (4) low-grade halogenated alkyl and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more substituting groups, and X ⁵Be aryl),

Y is OY ¹, NY ²Y ³Or SY ⁴

Y ²The optional low alkyl group that replaces of at least one aryl of serving as reasons,

Y ³Be low alkyl group or aryl,

Y ⁴For by one or more optional low alkyl groups that replace of following substituting group that are selected from: (1) is by the optional aryl that replaces of at least one halogen and (2) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Low-grade alkynyl; By one or more optional aryls that replace of following substituting group that are selected from: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen with by the optional lower alkoxy that replaces of at least one halogen; Or by one or more optional heterocyclic radicals that replace of following substituting group that are selected from: the heterocyclic radical that (1) is replaced by at least one halogen by the optional low alkyl group that replaces of at least one halogen and (2)),

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) hydroxyl, (4) by optional low alkyl group or the aryl that replaces of at least one halogen, (5) low-grade alkenyl, (6) by the optional lower alkoxy that replaces of at least one halogen, (7) low-grade alkane acidyl oxygen base, (8) by at least one alkyl or the optional aryl that replaces of halogen, (9) heterocyclic radical, (10) lower alkylthio, (11) low alkyl group sulfinyl, (12) low alkyl group alkylsulfonyl, (13) arylthio, (14) elementary alkoxy carbonyl, (15) low-grade alkane acidyl, (16) aromatic hydrocarbons carbonyl, (17) low-grade alkynyl, (18) rudimentary cycloalkylthio, (19) low-grade alkylidene dioxy base, (20) low-grade alkylidene and (21) nitro; Heterocyclic radical; Lower alkoxycarbonyl; The aromatic hydrocarbons alkylsulfonyl; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; Lower alkoxy by at least one aryl replacement; Or amino by the rudimentary alkylidene of at least one aryl replacement.

According to the compound of [1], wherein

X serves as reasons, and at least one is selected from the optional thiophenyl that replaces of following substituting group: halogen, methyl, trifluoromethyl and methoxyl group; Or be selected from the optional phenoxy group that replaces of following substituting group by at least one: halogen, methyl, trifluoromethyl and methoxyl group;

Y serves as reasons, and at least one is selected from the optional thiophenyl that replaces of following substituting group: halogen, methyl, trifluoromethyl and methoxyl group; Be selected from the optional phenoxy group that replaces of following substituting group by at least one: halogen, methyl, trifluoromethyl and methoxyl group; Be selected from the optional benzylthio-that replaces of following substituting group by at least one: halogen, and methyl; Secondary butylthio; The cyclohexyl methylthio group; Or hexamethylene sulfenyl:

Z serves as reasons, and at least one is selected from the optional phenyl that replaces of following substituting group: halogen, methyl, sec.-propyl, trifluoromethyl and methoxyl group.

According to the compound of [1], wherein

Y serves as reasons, and at least one is selected from the optional thiophenyl that replaces of following substituting group: halogen, methyl, trifluoromethyl and methoxyl group; Be selected from the optional phenoxy group that replaces of following substituting group by at least one: halogen, methyl, trifluoromethyl and methoxyl group; Or hexamethylene sulfenyl:

Suitable example and the practical examples of the various definition that are used for the application's context-descriptive that the present invention includes will be described in more detail below.

Unless other regulation, term " lower " means have 6 or the group of carbon atom still less.

Unless stipulate that in addition term " senior " means to have the group of 7-20 carbon atom.

The suitable example of " one or more " can comprise 1-6, preferred 1-3.

" low alkyl group ", " low-grade alkyl group " and " low alkyl group " suitable example in term " the optional low alkyl group that replaces " comprise straight or branched C _1-6Alkyl is such as, methyl, ethyl, n-propyl, sec.-propyl, normal-butyl, isobutyl-, sec-butyl, the tertiary butyl, n-pentyl, sec.-amyl sec-pentyl secondary amyl, isopentyl, neo-pentyl, n-hexyl, isohexyl etc.

The suitable example of " senior alkyl " comprises straight or branched C _7-20Alkyl, for example, heptyl, octyl group, 3,5-dimethyl octyl group, 3,7-dimethyl octyl group, nonyl, decyl, undecyl, dodecyl, tridecyl, tetradecyl, hexadecyl, heptadecyl, octadecyl, nonadecyl, eicosyl (icosyl) etc.

The suitable example of " low-grade alkenyl " and " low-grade alkenyl " in term " the optional low-grade alkenyl that replaces " comprises straight or branched C _2-6Thiazolinyl, for example, vinyl, allyl group, pseudoallyl, isobutenyl, 1-methacrylic, 3-methyl-2-butene base, pentenyl, 2-hexenyl etc.

The suitable example of " senior thiazolinyl " comprises straight or branched C _7-20Thiazolinyl, for example, heptenyl, octenyl, 3,5-dimethyl-octa thiazolinyl, 3,7-dimethyl-6-octenyl, geranyl (geranyl) etc.

The suitable example of " low-grade alkynyl " and " low-grade alkynyl " in term " the optional low-grade alkynyl that replaces " comprises C _2-6Alkynyl, for example, ethynyl, propargyl, 2-butyne base, 3-butynyl, 3-pentynyl, 3-hexin base etc.

The suitable example of " senior alkynyl " comprises straight or branched C _7-20Alkynyl, for example, heptyne base, octyne base, 3,5-dimethyl-octa alkynyl, 3,7-dimethyl-octa alkynyl etc.

The suitable example of " low-grade cycloalkyl " and " low-grade cycloalkyl " in term " the optional low-grade cycloalkyl that replaces " comprises C _3-6Cycloalkyl, for example, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl etc., and preferably can be C _4-6Cycloalkyl, most preferably cyclohexyl.

The suitable example of " lower alkenyl ring " and " lower alkenyl ring " in term " the optional lower alkenyl ring that replaces " comprises C _3-6Cycloalkenyl group, for example, cyclopropenyl radical, cyclobutene base, cyclopentenyl, cyclohexenyl (as, 2-tetrahydrobenzene-1-base, 3-tetrahydrobenzene-1-yl) etc., and this " lower alkenyl ring " can have low alkyl group.

" aryl " in term " the optional aryl that replaces ", the suitable example of " aryl " and " aryl " comprise, for example, optional phenyl with at least one low alkyl group (as, phenyl, 2,4,6-trimethylphenyl, xylyl, tolyl etc.) and C _6-14Aryl such as naphthyl, anthryl, indanyl, tetralyl etc., and preferably can be phenyl and naphthyl, and should " aryl " can have suitable substituting group such as low alkyl group, halogen, lower alkoxy, low-grade cycloalkyl etc.

" heterocyclic radical " in term " the optional heterocyclic radical that replaces ", and the suitable example of " heterocycle " part comprises unsaturated 3 to 8-units (more preferably 5 to the 6-units) heteromonocyclic group that contains 1-4 nitrogen-atoms, for example, pyrryl, pyrrolinyl (pyrrolynyl), imidazolyl, pyrazolyl, pyridyl, the dihydropyridine base, pyrimidyl, pyrazinyl, pyridazinyl, triazolyl (as, 4H-1,2, the 4-triazolyl, 1H-1,2, the 3-triazolyl, 2H-1,2,3-triazolyl etc.), tetrazyl (as, the 1H-TETRAZOLE base, 2H-tetrazyl etc.) etc.; 3 to 8-saturated units (more preferably 5 to the 6-units) heteromonocyclic group that contains the 1-4 nitrogen-atoms, for example, pyrrolidyl, imidazolidyl, piperidyl, piperidino-(1-position only), piperazinyl (piperadinyl) etc.; The undersaturated annelated heterocycles base that contains the 1-4 nitrogen-atoms, for example, indyl, pseudoindoyl, indolinyl, indolyl (indolidinyl), benzimidazolyl-, quinolyl, isoquinolyl, indazolyl, benzotriazole base, imidazopyridyl, Imidazothiazole base etc.; Undersaturated 3 to 8-units (more preferably 5 to the 6-units) heteromonocyclic group that contains one or two a Sauerstoffatom and 1-3 nitrogen-atoms, Li such as ， oxazolyl, isoxazolyl, oxadiazolyl (as, 1,2,4-oxadiazolyl, 1,3,4-oxadiazolyl, 1,2,5-oxadiazolyl etc.) etc.; 3 to 8-saturated units (more preferably 5 to the 6-units) heteromonocyclic group that contains one or two a Sauerstoffatom and 1-3 nitrogen-atoms, such as morpholinyl, morpholino etc.; The undersaturated annelated heterocycles base that contains one or two a Sauerstoffatom and 1-3 nitrogen-atoms, for example, benzoxazolyl, Ben Bing oxadiazolyl etc.; Undersaturated 3 to 8-units (more preferably, 5 to the 6-units) heteromonocyclic group that contains one or two a sulphur atom and 1-3 nitrogen-atoms, for example, thiazolyl, isothiazolyl, thiadiazolyl group (as, 1,2,3-thiadiazolyl group, 1,2,4-thiadiazolyl group, 1,3,4-thiadiazolyl group, 1, and dihydro thiazinyl etc. 2,5-thiadiazolyl group etc.); Saturated 3 to 8-units (more preferably 5 to the 6-units) heteromonocyclic group that contains one or two a sulphur atom and 1-3 nitrogen-atoms, for example, thiazolidyl, thio-morpholinyl, thiomorpholine generation etc.; Undersaturated 3-8 unit (more preferably, the 5-6 unit) heteromonocyclic group that contains one or two sulphur atom, for example, thienyl, dihydro dithiene base (dithiinyl), dihydro dithione base etc.; The saturated heteromonocyclic group that contains one or two sulphur atom, for example, tetrahydro-thienyl, dithiane base etc.; Contain one or two sulphur atom and the undersaturated annelated heterocycles base that contains 1-3 nitrogen-atoms, for example, benzothiazolyl, diazosulfide base, imidazo thiadiazolyl group etc.; Undersaturated 3-8-unit (more preferably, the 5-6 unit) heteromonocyclic group that contains one or two Sauerstoffatom, for example, furyl, dihydro pyranyl, dioxine base (dioxynyl) etc.; Saturated 3-8-unit (more preferably, the 5-6 unit) heteromonocyclic group that contains one or two Sauerstoffatom, for example, tetrahydrofuran base, THP trtrahydropyranyl, dioxane base etc.; The undersaturated annelated heterocycles base that contains one or two Sauerstoffatom, for example, benzofuryl, benzo dioxolanyl, benzo dioxane base etc.; Undersaturated 3-8-unit (more preferably, the 5-6 unit) heteromonocyclic group that contains Sauerstoffatom and one or two sulphur atom, for example, Er Qing Evil thiophene thiazolinyl (xathiinyl) etc.; The undersaturated annelated heterocycles base that contains one or two sulphur atom, for example, benzothienyl, benzo dithiene base etc.; The undersaturated annelated heterocycles base that contains Sauerstoffatom and one or two sulphur atom, for example, Ben Bing Evil thiophene thiazolinyl (benzoxathiinyl) etc.; And the part of being somebody's turn to do " heterocyclic radical " and " heterocycle " can have at least one suitable substituting group such as low alkyl group, halogen, lower alkoxy or low-grade cycloalkyl etc.

Halogen represents fluorine, chlorine, bromine or iodine.

The suitable example of " low-grade halogenated alkyl " comprises the fluoro methyl, difluoromethyl, trifluoromethyl, chloro methyl, pentafluoroethyl group etc.

" lower alkoxy " in term " the optional lower alkoxy that replaces ", the suitable example of " lower alkoxy groups " and " lower alkoxy " comprise straight or branched C _1-6Alkoxyl group, for example, methoxyl group, oxyethyl group, propoxy-, isopropoxy, butoxy, isobutoxy, uncle-butoxy, pentyloxy, uncle-pentyloxy, new-pentyloxy, hexyloxy, different hexyloxy etc., preferably, methoxyl group, oxyethyl group, propoxy-, butoxy, pentyloxy, hexyloxy and different hexyloxy.

The suitable example of " rudimentary cyclopentyloxy " and " rudimentary cyclopentyloxy " in term " the optional rudimentary cyclopentyloxy that replaces " comprises C _3-6Cyclopentyloxy such as cyclopropyl oxygen base, cyclobutyl oxygen base, cyclopentyloxy, cyclohexyl oxygen base etc.

" carboxyl groups " and " acyl group " comprises aliphatic acyl, aromatic acyl group, aryl aliphatic acyl, heterocyclic radical acyl group and the heterocyclic radical aliphatic acyl of derived from carboxylic acid, carbonic acid, carboxylamine, sulfonic acid etc.

The suitable example of above-mentioned " acyl group " comprises those following acyl groups.

Carboxyl; Formamyl; One or two-elementary alkyl amido methanoyl (as, methylamino formyl radical, formyl-dimethylamino, ethylamino formyl radical, diethylamino formyl radical etc.); One or the ammonia diaryl base formyl radical (as, phenyl amino formyl radical, diphenyl amino formyl radical etc.); The low-grade alkylaryl formamyl (as, aminomethyl phenyl formamyl etc.); Thiocarbamoyl; One or two-low alkyl group sulfo-formamyl (as, methyl thiocarbamoyl, dimethyl thiocarbamoyl, ethylenebis dithiocarbamate formamyl, diethyl thiocarbamoyl etc.); One or the diaryl thiocarbamoyl (as, phenyl thiocarbamoyl, phenylbenzene thiocarbamoyl etc.); The low-grade alkylaryl thiocarbamoyl (as, aminomethyl phenyl thiocarbamoyl etc.);

Aliphatic acyl,

For example, low-grade alkane acidyl (as, C _1-6Alkyloyl such as formyl radical, ethanoyl, propionyl, butyryl radicals, 2-methylpropionyl, pentanoyl, 2,2-dimethyl propylene acyl group, caproyl etc.); Senior alkyloyl (as, C _7-20Alkyloyl such as oenanthyl, capryloyl, nonanoyl, decanoyl, undecanoyl, lauroyl, tridecanoyl, tetradecanoyl, pentadecanoyl, hexadecanoyl, heptadecane acyl group, octadecanoyl, nonadecane acyl group, eicosane acyl group (icosanoyl) etc.); Elementary alkoxy carbonyl (as, C _1-6Alkoxy carbonyl such as methoxycarbonyl, ethoxy carbonyl, propoxycarbonyl, butoxy carbonyl, uncle-butoxy carbonyl, uncle-pentyloxy carbonyl, hexyloxy carbonyl etc.); Senior alkoxy carbonyl (as, C _7-20Alkoxy carbonyl such as heptyl oxygen base carbonyl, octyl group oxygen base carbonyl, nonyl oxygen base carbonyl, decyl oxygen base carbonyl, undecyl oxygen base carbonyl etc.); The low alkyl group alkylsulfonyl (as, C _1-6Alkyl sulphonyl such as methyl sulphonyl, ethylsulfonyl, sulfonyl propyl base, sec.-propyl alkylsulfonyl, normal-butyl alkylsulfonyl, tertiary butyl alkylsulfonyl, n-pentyl alkylsulfonyl, hexyl alkylsulfonyl etc.); The senior alkyl alkylsulfonyl (as, C _7-20Alkyl sulphonyl such as heptyl alkylsulfonyl, octyl group alkylsulfonyl, nonyl alkylsulfonyl, decyl alkylsulfonyl, dodecyl alkylsulfonyl, pentadecyl alkylsulfonyl etc.); The lower alkoxy alkylsulfonyl (as, C _1-6Alkoxyl group alkylsulfonyl such as methoxyl group alkylsulfonyl, oxyethyl group alkylsulfonyl, propoxy-alkylsulfonyl, butoxy alkylsulfonyl, uncle-butoxy alkylsulfonyl, pentyloxy alkylsulfonyl, hexyloxy alkylsulfonyl etc.); Senior alkoxyl group alkylsulfonyl (as, C _7-20Alkoxyl group alkylsulfonyl such as heptyl oxygen base alkylsulfonyl, octyl group oxygen base alkylsulfonyl, nonyl oxygen base alkylsulfonyl, decyl oxygen base alkylsulfonyl, undecyl oxygen base alkylsulfonyl etc.);

Aromatic acyl group,

For example, aroyl (as, benzoyl, toluyl, naphthoyl etc.); The aryl low-grade alkane acidyl (as, phenyl (C _1-6) alkyloyl such as phenyl acetyl, phenyl propionyl, phenyl butyryl radicals, phenyl isobutyryl, phenyl pentanoyl, phenyl caproyl etc., naphthyl (C _1-6) alkyloyl such as naphthyl ethanoyl, naphthyl propionyl, naphthyl acyl group etc.); The rudimentary enoyl-of aryl (alkenoyl) (as, phenyl (C _3-6) enoyl-such as phenyl acryloyl, phenyl crotonoyl, phenyl methacryloyl, phenyl pentenoyl, phenyl hexenoyl etc., naphthyl (C _1-6) enoyl-such as naphthyl acryl, naphthyl enoyl-etc.); The aryl-lower alkoxy carbonyl (as, phenyl (C _1-6) alkoxy carbonyl such as benzyloxycarbonyl etc., fluorenyl (C _1-6) alkoxy carbonyl such as fluorenyl methyl oxygen base carbonyl etc.); The aryloxy carbonyl (as, phenyloxycarbonyl, naphthyl oxygen base carbonyl etc.); The aryloxy low-grade alkane acidyl (as, phenoxy group ethanoyl, phenoxy group propionyl etc.); Aryl glyoxyl-based (as, phenyl is glyoxyl-based, naphthyl is glyoxyl-based etc.); Optional aryl sulfonyl with 1-4 low alkyl group (as, phenyl sulfonyl, p-tolylsulfonyl-base etc.) etc.; With

The heterocyclic radical acyl group

For example, heterocyclic radical carbonyl; The heterocyclic radical low-grade alkane acidyl (as, heterocyclic radical (C _1-6) alkyloyl such as heterocyclic radical ethanoyl, heterocyclic radical propionyl, heterocyclic radical butyryl radicals, heterocyclic radical pentanoyl, heterocyclic radical caproyl etc.); The rudimentary enoyl-of heterocyclic radical (as, heterocyclic radical (C _1-6) enoyl-such as heterocyclic radical acryl, heterocyclic radical crotonoyl, heterocyclic radical pentenoyl, heterocyclic radical hexenoyl etc.); Heterocyclic radical is glyoxyl-based etc.At this, at term " heterocyclic radical carbonyl ", suitable " heterocyclic radical " part in " heterocyclic radical low-grade alkane acidyl ", " the rudimentary enoyl-of heterocyclic radical " and " heterocyclic radical is glyoxyl-based ", above-mentioned " heterocyclic radical " part can be mentioned.

The suitable example of " rudimentary alkylidene is amino " comprises C _1-6Alkylidene amino oxygen base (as, ethidine is amino, the propylidene base is amino, isopropylidene is amino, cyclohexylidene is amino etc.).

The suitable example of " rudimentary alkylidene amino oxygen base " comprises C _1-6Alkylidene amino (as, ethidine amino oxygen base, propylidene base amino oxygen base, isopropylidene amino oxygen base, cyclohexylidene amino etc.).

The suitable example of " rudimentary alkylidene diazanyl " comprises C _1-6The alkylidene diazanyl (as, ethidine diazanyl, propylidene base diazanyl, isopropylidene diazanyl, cyclohexylidene diazanyl etc.).

The suitable example of " rudimentary alkylidene hydrazono-" comprises C _1-6The alkylidene hydrazono-(as, ethidine hydrazono-, propylidene base hydrazono-, isopropylidene hydrazono-, cyclohexylidene hydrazono-etc.).

The suitable example of " low-grade alkane acidyl oxygen base " comprises C _1-6Alkyloyl oxygen base (as, formyl radical oxygen base, ethanoyl oxygen base, propionyl oxygen base, butyryl radicals oxygen base, 2-methylpropionyl oxygen base, pentanoyl oxygen base, 2,2-dimethyl propylene acyloxy, caproyl oxygen base etc.).

The suitable example of " lower alkylthio " comprises C _1-6Alkylthio (as, methylthio group, ethylmercapto group, rosickyite base etc.).

The suitable example of " low alkyl group sulfinyl " comprises C _1-6Alkyl sulphinyl (as, methylsulfinyl, ethyl sulfinyl, propyl group sulfinyl etc.).

The suitable example of " low alkyl group alkylsulfonyl " comprises C _1-6Alkyl sulphonyl (as, methyl sulphonyl, ethylsulfonyl, sulfonyl propyl base etc.).

The suitable example of " arylthio " comprises thiophenyl, 2,4,6-trimethylbenzene sulfenyl, xylyl sulfenyl, tolyl sulfenyl, naphthyl sulfenyl etc.

In compound (I), X represents OX ¹, NX ²X ³, SX ⁴, S (O) _mX ⁵, Si (X ⁶) ₃Or N=C (X ⁷) ₂

And the aryl that the optional low alkyl group that replaces or optional replacement are arranged of preferably mentioning, the low alkyl group that at least one aryl of serving as reasons of particularly preferably mentioning replaces or the optional aryl that replaces.

To being used for X ¹Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For above-mentioned to X ¹" senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

To being used for X ¹Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

To being used for X ¹Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ¹Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

To being used for X ¹Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

To being used for X ¹Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ¹Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

To being used for X ¹Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

To being used for X ¹Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

Be used for X ¹Term " optional replace low alkyl group "; " the optional low-grade cycloalkyl that replaces "; " the optional low-grade alkenyl that replaces "; substituent suitable example in " the optional lower alkenyl ring that replaces " and " the optional low-grade alkynyl that replaces " comprises low alkyl group; low-grade alkenyl; low-grade alkynyl; lower alkoxy; low-grade alkane acidyl oxygen base; low-grade halogenated alkyl (as; the fluoro methyl; difluoromethyl; trifluoromethyl etc.); elementary halogenated alkoxy (as; the fluoro methoxyl group; difluoro-methoxy; trifluoromethoxy etc.), hydroxyl; nitro; cyano group; carboxyl; sulfo group; oxo; halogen; low-grade cycloalkyl; lower alkenyl ring; the optional aryl that replaces; the optional heterocyclic radical that replaces; acyl group; rudimentary alkylidene is amino; rudimentary alkylidene amino oxygen base; rudimentary alkylidene diazanyl; rudimentary alkylidene hydrazono-;

By formula :-SO _TX ^1AThe group of expression,

By formula :-OX ^1BThe group of expression,

By formula :-N (X ^1C) ₂The group of expression,

By formula :-ON (X ^1D) ₂The group of expression,

By formula :=NX ^1EThe group of expression,

By formula :=NOX ^1FThe group of expression,

By formula :-N (X ^1G) N (X ^1H) ₂The group of expression,

By formula :=NN (X ^1I) ₂The group of expression,

By formula :-C (=Q ^1A) N (X ^1J) ₂The group of expression,

By formula :-C (=Q ^1B) N (X ^1K) N (X ^1L) ₂The group of expression, etc.,

And substituent number is in commutable scope and be 1-5, preferred 1-3.

In following formula, T represents integer 0,1 or 2,

X ^1AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

X ^1B, X ^1C, X ^1D, X ^1E, X ^1F, X ^1G, X ^1H, X ^1I, X ^1J, X ^1KAnd X ^1LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^1PThe group of expression, or

By formula :-C (=Q ^1C) N (X ^1Q) ₂The group of expression.

At this, X ^1PAnd X ^1QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical, and Q ^1A, Q ^1BAnd Q ^1CRepresent independently of one another Sauerstoffatom or sulphur atom.

When " substituting group " in term " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces " and " the optional low-grade alkynyl that replaces " is acyl group, C _1-6Alkylidene is amino, C _1-6Alkylidene amino oxygen base, C _1-6Alkylidene diazanyl or C _1-6During the alkylidene hydrazono-,

Or, work as X ^1A, X ^1B, X ^1C, X ^1D, X ^1E, X ^1F, X ^1G, X ^1H, X ^1I, X ^1J, X ^1K, X ^1L, X ^1PAnd X ^1QIn one or more when being low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring or low-grade alkynyl,

These groups can further be replaced by following group: nitro, cyano group, carboxyl, sulfo group, oxo, halogen, aryl, low-grade cycloalkyl, lower alkenyl ring, heterocyclic radical, acyl group, rudimentary alkylidene amino, rudimentary alkylidene amino oxygen base, rudimentary alkylidene diazanyl, rudimentary alkylidene hydrazono-,

By formula :-SO _UX ^2AThe group of expression,

By formula :-OX ^2BThe group of expression,

By formula :-N (X ^2C) ₂The group of expression,

By formula :-ON (X ^2D) ₂The group of expression,

By formula :=NX ^2EThe group of expression,

By formula :=NOX ^2FThe group of expression,

By formula :-N (X ^2G) N (X ^2H) ₂The group of expression,

By formula :=NN (X ^2I) ₂The group of expression,

By formula :-C (=Q ^2A) N (X ^2J) ₂The group of expression,

By formula :-C (=Q ^2B) N (X ^2K) N (X ^2L) ₂, etc.In this case, substituent number is preferably 1-3.

In following formula, U represents integer 0,1 or 2,

X ^2AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces, and X ^2B, X ^2C, X ^2D, X ^2E, X ^2F, X ^2G, X ^2H, X ^2I, X ^2J, X ^2KAnd X ^2LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^2PThe group of expression, or

By formula :-C (=Q ^2C) N (X ^2Q) ₂The group of expression.

At this, X ^2PAnd X ^2QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical.

Q ^2A, Q ^2BAnd Q ^2CRepresent independently of one another Sauerstoffatom or sulphur atom.

When " substituting group " in term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces " and " the optional low-grade alkynyl that replaces " represents aryl, low-grade cycloalkyl, lower alkenyl ring or heterocyclic radical

Or, work as X ^1A, X ^1B, X ^1C, X ^1D, X ^1E, X ^1F, X ^1G, X ^1H, X ^1I, X ^1J, X ^1K, X ^1L, X ^1PAnd X ^1QIn one or more expression aryls, low-grade cycloalkyl, lower alkenyl ring or during heterocyclic radical,

These groups can further be replaced by following group: low alkyl group, lower alkoxy, low-grade halogenated alkyl (such as, fluoro methyl, difluoromethyl, trifluoromethyl etc.), nitro, cyano group, carboxyl, sulfo group, halogen, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, the optional aromatic hydrocarbons that replaces, the optional heterocyclic radical that replaces, acyl group, rudimentary alkylidene amino, rudimentary alkylidene amino oxygen base, rudimentary alkylidene diazanyl, rudimentary alkylidene hydrazono-,

By formula :-SO _VX ^3AThe group of expression,

By formula :-OX ^3BThe group of expression,

By formula :-N (X ^3C) ₂The group of expression,

By formula :-ON (X ^3D) ₂The group of expression,

By formula :=NX ^3EThe group of expression,

By formula :=NOX ^3FThe group of expression,

By formula :-N (X ^3G) N (X ^3H) ₂The group of expression,

By formula :=NN (X ^3I) ₂The group of expression,

By formula :-C (=Q ^3A) N (X ^3J) ₂The group of expression, or

By formula :-C (=Q ^3B) N (X ^3K) N (X ^3L) ₂In this case, substituent number is preferably 1-3.

In following formula, V represents integer 0,1 or 2,

X ^3AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

X ^3B, X ^3C, X ^3D, X ^3E, X ^3F, X ^3G, X ^3H, X ^3I, X ^3J, X ^3KAnd X ^3LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^3PThe group of expression, or

By formula :-C (=Q ^3C) N (X ^3Q) ₂The group of expression.

At this, X ^3PAnd X ^3QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical.

Q ^3A, Q ^3BAnd Q ^3CRepresent independently of one another Sauerstoffatom or sulphur atom.

And described aryl, low-grade cycloalkyl, lower alkenyl ring or heterocyclic radical have at least one substituting group,

Or work as X ^1A, X ^1B, X ^1C, X ^1D, X ^1E, X ^1F, X ^1G, X ^1H, X ^1I, X ^1J, X ^1K, X ^1L, X ^1PAnd X ^1QDuring for aryl, low-grade cycloalkyl or lower alkenyl ring, the first heterocyclic radical of described 3-8 has at least one substituting group, and

When these substituting groups are acyl group, alkylidene amino, alkylidene amino oxygen base, alkylidene diazanyl or alkylidene hydrazono-, or work as X ^3A, X ^3B, X ^3C, X ^3D, X ^3E, X ^3F, X ^3G, X ^3H, X ^3I, X ^3J, X ^3K, X ^3L, X ^3PAnd X ^3QIn one or more when being low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring or low-grade alkynyl,

These groups can further be replaced by following group: nitro, cyano group, carboxyl, sulfo group; oxo; halogen; aryl; low-grade cycloalkyl, lower alkenyl ring; heterocyclic radical, acyl group, rudimentary alkylidene amino, rudimentary alkylidene amino oxygen base, rudimentary alkylidene diazanyl, rudimentary alkylidene hydrazono-

By formula :-SO _WX ^4AThe group of expression,

By formula :-OX ^4BThe group of expression,

By formula :-N (X ^4C) ₂The group of expression,

By formula :-ON (X ^4D) ₂The group of expression,

By formula :=NX ^4EThe group of expression,

By formula :=NOX ^4FThe group of expression,

By formula :-N (X ^4G) N (X ^4H) ₂The group of expression,

By formula :=NN (X ^4I) ₂The group of expression,

By formula :-C (=Q ^4A) N (X ^4J) ₂The group of expression, or

By formula :-C (=Q ^4B) N (X ^4K) N (X ^4L) ₂The group of expression.In this case, substituent number is preferably 1-3.

In following formula, W represents integer 0,1 or 2,

X ^4AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical, and X ^4B, X ^4C, X ^4D, X ^4E, X ^4F, X ^4G, X ^4H, X ^4I, X ^4J, X ^4KAnd X ^4LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^4PThe group of expression, or

By formula :-C (=Q ^4C) N (X ^4Q) ₂The group of expression.

At this, X ^4PAnd X ^4QRepresent independently of one another low alkyl group, low-grade cycloalkyl, C _2-6Thiazolinyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

Q ^4A, Q ^4BAnd Q ^4CRepresent independently of one another Sauerstoffatom or sulphur atom.

At X ¹The substituent suitable example of term " optional replace aryl " comprise low alkyl group; low-grade alkenyl; low-grade alkynyl; lower alkoxy; low-grade alkane acidyl oxygen base; low-grade halogenated alkyl (as; the fluoro methyl; difluoromethyl; trifluoromethyl etc.); elementary halogenated alkoxy (as, the fluoro methoxyl group; difluoro-methoxy; trifluoromethoxy etc.); hydroxyl; nitro; cyano group; carboxyl; sulfo group; halogen; low-grade cycloalkyl; lower alkenyl ring; the optional aryl that replaces; the optional heterocyclic radical that replaces; acyl group; rudimentary alkylidene is amino; rudimentary alkylidene amino oxygen base; rudimentary alkylidene diazanyl; rudimentary alkylidene hydrazono-;

By formula :-SO _KX ^5AThe group of expression,

By formula :-OX ^5BThe group of expression,

By formula :-N (X ^5C) ₂The group of expression,

By formula :-ON (X ^5D) ₂The group of expression,

By formula :=NX ^5EThe group of expression,

By formula :=NOX ^5FThe group of expression,

By formula :-N (X ^5G) N (X ^5H) ₂The group of expression,

By formula :=NN (X ^5I) ₂The group of expression,

By formula :-C (=Q ^5A) N (X ^5J) ₂The group of expression,

By formula :-C (=Q ^5B) N (X ^5K) N (X ^5L) ₂The group of expression, etc.,

And substituent number is preferably 1-5, more preferably 1-3.

In following formula, K represents integer 0,1 or 2,

X ^5AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

X ^5B, X ^5C, X ^5D, X ^5E, X ^5F, X ^5G, X ^5H, X ^5I, X ^5J, X ^5KAnd X ^5LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^5PThe group of expression, or

By formula :-C (=Q ^5C) N (X ^5Q) ₂The group of expression.

At this, X ^5PAnd X ^5QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

And Q ^5A, Q ^5BAnd Q ^5CRepresent independently of one another Sauerstoffatom or sulphur atom.

When the substituting group in " optional replace aryl " is acyl group, alkylidene amino, alkylidene amino oxygen base, alkylidene diazanyl or alkylidene hydrazono-,

Or, work as X ^5A, X ^5B, X ^5C, X ^5D, X ^5E, X ^5F, X ^5G, X ^5H, X ^5I, X ^5J, X ^5K, X ^5L, X ^5PAnd X ^5QIn one or more when being low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring or low-grade alkynyl,

These groups can further be selected from following 1-3 substituting group and be replaced: nitro, cyano group, carboxyl, sulfo group, oxo; halogen; aryl, heterocyclic radical, acyl group, rudimentary alkylidene amino, rudimentary alkylidene amino oxygen base, rudimentary alkylidene diazanyl, rudimentary alkylidene hydrazono-

By formula :-SO _LX ^6AThe group of expression,

By formula :-OX ^6BThe group of expression,

By formula :-N (X ^6C) ₂The group of expression,

By formula :-ON (X ^6D) ₂The group of expression,

By formula :=NX ^6EThe group of expression,

By formula :=NOX ^6FThe group of expression,

By formula :-N (X ^6G) N (X ^6H) ₂The group of expression,

By formula :=NN (X ^6I) ₂The group of expression,

By formula :-C (=Q ^6A) N (X ^6J) ₂The group of expression,

By formula :-C (=Q ^6B) N (X ^6K) N (X ^6L) ₂The group of expression, etc.

In following formula, L represents integer 0,1 or 2,

X ^6AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

And X ^6B, X ^6C, X ^6D, X ^6E, X ^6F, X ^6G, X ^6H, X ^6I, X ^6J, X ^6KAnd X ^6LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^6PThe group of expression, or

By formula :-C (=Q ^6C) N (X ^6Q) ₂The group of expression.

At this, X ^6PAnd X ^6QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

And Q ^6A, Q ^6BAnd Q ^6CRepresent independently of one another Sauerstoffatom or sulphur atom.

When the substituting group in " optional replace aryl " is aryl, low-grade cycloalkyl, lower alkenyl ring or heterocyclic radical, or work as X ^5A, X ^5B, X ^5C, X ^5D, X ^5E, X ^5F, X ^5G, X ^5H, X ^5I, X ^5J, X ^5K, X ^5L, X ^5PAnd X ^5QIn one or more when being aryl, low-grade cycloalkyl or heterocyclic radical,

These groups can further be selected from following 1-3 substituting group and be replaced: nitro, cyano group, carboxyl, sulfo group, halogen, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical, acyl group, rudimentary alkylidene amino, rudimentary alkylidene amino oxygen base, rudimentary alkylidene diazanyl, rudimentary alkylidene Asia hydrazine,

By formula :-SO _MX ^7AThe group of expression,

By formula :-OX ^7BThe group of expression,

By formula :-N (X ^7C) ₂The group of expression,

By formula :-ON (X ^7D) ₂The group of expression,

By formula :=NX ^7EThe group of expression,

By formula :=NOX ^7FThe group of expression,

By formula :-N (X ^7G) N (X ^7H) ₂The group of expression,

By formula :=NN (X ^7I) ₂The group of expression,

By formula :-C (=Q ^7A) N (X ^7J) ₂The group of expression,

By formula :-C (=Q ^7B) N (X ^7K) N (X ^7L) ₂The group of expression, etc.

In following formula, M represents integer 0,1 or 2,

X ^7AExpression hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical,

X ^7B, X ^7C, X ^7D, X ^7E, X ^7F, X ^7G, X ^7H, X ^7I, X ^7J, X ^7KAnd X ^7LRepresent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, C _2-6Alkynyl, aryl, heterocyclic radical, acyl group,

By formula :-SO ₂X ^7PThe group of expression, or

By formula :-C (=Q ^7C) N (X ^7Q) ₂The group of expression.

At this, X ^7PAnd X ^7QRepresent independently of one another low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl or heterocyclic radical, and Q ^7A, Q ^7BAnd Q ^7CRepresent independently of one another Sauerstoffatom or sulphur atom.

For at X ¹" optional replace heterocyclic radical " in substituting group, described substituting group is identical with the exemplary substituting group that " aryl of optional replacement " mentioned.

And the aryl that the optional low alkyl group that replaces, optional replacement are arranged of preferably mentioning, or C (=Q ²¹) X ^A2(at this, Q ²¹Expression Sauerstoffatom, and X ^A2The optional low alkyl group that replaces of expression), low alkyl group, aryl or low-grade alkane acidyl that at least one aryl of serving as reasons of particularly preferably mentioning replaces.

For at X ²Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For at X ²In above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ²Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ²Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For at X ²In above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For at X ²Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ²Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ²In above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ²Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ²Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ²Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " heterocyclic radical of optional replacement " in substituting group, above-mentioned to X ¹" substituting group " can be mentioned.

For X ²X ^B2, Q ²², X ^D2, X ^E2, X ^F2, X ^G2X ^H2, X ^I2And X ^K2, can mention following group.

And the low alkyl group that optional replacement is arranged of preferably mentioning, or the optional aryl that replaces, what particularly preferably mention is low alkyl group or aryl.

For at X ³Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ³Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ³Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ³Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For at X ³Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ³Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ³Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ³Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ³Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ³Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " heterocyclic radical of optional replacement " in substituting group, " can mention above-mentioned to X ¹" substituting group.

For X ³X ^A3, X ^B3, Q ³², X ^D3, X ^E3And X ^F3, can mention following radicals.

For by X ²And X ³With " ring structure " that its nitrogen connected to one another represents, can mention with by X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe structure that following " ring structure " that represents together with its nitrogen connected to one another is identical.

X ⁴The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, the optional lower alkenyl ring that replaces, senior thiazolinyl, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁴¹) X ^A4, C (=O) OX ^B4, C (=Q ⁴²) NX ^D4X ^E4Or S (O) _nX ^F4,

And the low alkyl group for optional replacement that the optional low alkyl group that replaces, senior alkyl, the aryl of choosing the low-grade alkenyl that replaces, the optional low-grade cycloalkyl that replaces, optional replacement wantonly or the optional heterocyclic radical that replaces is arranged, particularly preferably mention of preferably mentioning, senior alkyl, low-grade cycloalkyl, low-grade alkenyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

For X ⁴Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For at X ⁴Term " optional replace low alkyl group " in substituting group, can mention X ¹" substituting group ", and preferably mention the optional aryl that replaces or the optional heterocyclic radical that replaces, the optional aromatic hydrocarbons that replaces of at least one halogen of serving as reasons of particularly preferably mentioning or the heterocyclic radical that is replaced by at least one halogen arranged.

For X ⁴Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ⁴Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ⁴Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ⁴Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For at X ⁴Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ⁴Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ⁴Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ⁴Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ⁴Above-mentioned term " optional replace aryl " in substituting group, can mention above-mentioned X ¹" substituting group ", and preferably mention halogen, nitro, low alkyl group, low-grade halogenated alkyl or lower alkoxy arranged.

For at X ⁴Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ⁴Above-mentioned term " optional replace heterocyclic radical " in substituting group, can mention above-mentioned X ¹" substituting group ", and preferably mention low alkyl group arranged.

For at X ⁴Term " optional replace low-grade cycloalkyl ", " the optional low-grade alkenyl that replaces ", the substituting group in " the optional lower alkenyl ring that replaces " and " low-grade alkynyl of optional replacement " can be mentioned above-mentioned X ¹" substituting group ".

For X ⁴Q ⁴¹, X ^A4, X ^B4, Q ⁴², X ^D4, X ^E4And X ^F4, can mention after a while described group.

And preferably mention the optional aryl that replaces arranged, and mention especially aryl arranged.

For at X ⁵Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ⁵Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ⁵Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ⁵Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ⁵Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For at X ⁵Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ⁵Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ⁵Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ⁵Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ⁵Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ⁵Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", substituting group in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned X ¹" substituting group ".

X ⁶The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional lower alkoxy that replaces.

For at X ⁶Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ⁶Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ⁶Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ⁶Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ⁶Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For at X ⁶Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ⁶Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ⁶Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ⁶Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ⁶Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ⁶Term " optional replace lower alkoxy " in above-mentioned " lower alkoxy ", above-mentioned " lower alkoxy " can be mentioned.

For at X ⁶Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces ", the substituting group in " the optional heterocyclic radical that replaces " and " the optional lower alkoxy that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

X ⁷Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the OX that replaces ^L7, SX ^L7Or NX ^G7X ^H7,

Perhaps, with its carbon atom representative ring structure connected to one another.

For at X ⁷Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ⁷Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For at X ⁷Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For at X ⁷Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ⁷Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For at X ⁷Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For at X ⁷Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For X ⁷Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For at X ⁷Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For at X ⁷Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For at X ⁷Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " heterocyclic radical of optional replacement " in substituting group, can mention above-mentioned X ¹" substituting group ".

For " heterocyclic radical " in the term " the optional heterocyclic radical that replaces " of X, can mention above-mentioned " heterocyclic radical ", and preferably mention heterocyclic radical, particularly preferably mention piperidino-(1-position only) or morpholino group.

For X ^L7, X ^M7, X ^G7And X ^H7, can mention following group.

By each X ⁷" ring structure " that represent with its carbon connected to one another means to comprise carbon atom as the 3-8 unit cyclic group that becomes annular atoms, and can mention and comprise carbon atom as becoming annular atoms, and optional have 1-3 heteroatoms such as a nitrogen-atoms (choosing wantonly oxidized), Sauerstoffatom, the 3-8 unit of sulphur atom (optional by one or two-oxidation) etc. (preferably, 5-6 unit) cyclic group, for example, cyclopentylidene, cyclohexylidene, inferior suberyl, inferior ring octyl group, inferior cyclopentenes, phenylidene, inferior cycloheptenyl, inferior cyclooctene base, cyclopentadienylidene (cyclopentadienylidene), phenylidene (cyclohexadienylidene), inferior cycloheptadiene base (cycloheptadienylidene), inferior cyclooctadiene base (cyclooctadienylidene), tetrahydrofuran (THF) fork base, dihydrofuran fork base, tetrahydropyrans fork base, dihydropyrane fork base, pyrans fork base (pyranylidene), dioxolane fork base (dioxolanylidene), dioxole fork base (dioxolylidene), dioxane fork base, dioxine fork base (dioxinylidene), tetramethylene sulfide fork base, dihydro-thiophene fork base, tetrahydric thiapyran fork base, dihydro thiapyran fork base, thiapyran fork base, dithiolane fork base (dithiolanylidene), between dithiole fork base (dithiolylidene), dithiane fork base, dithia tetrahydrobenzene fork base (dithiinylidene), 2H-pyrrolin fork base, 2H-pyrroles pitches base, 3H-pyrroles pitches base, 2H-imidazoles fork base, 3H-triazole fork base etc.; With by make phenyl ring or 3-8 unit (preferably, 5-6 unit) heterocyclic radical (this heterocyclic radical has 1-4 optional oxidized nitrogen-atoms, Sauerstoffatom, optional by one or the sulphur atom of two-oxidation) condense with above-mentioned cyclic group and the group that obtains.

" comprise carbon atom as the 3-8 unit cyclic group that becomes annular atoms " can by as to X ¹" optional replace aryl " on the identical substituting group of the substituting group that exemplifies replace.The substituent number of The number ofthe is in commutable scope and be 1-5, preferred 1-3.

Q ^XA1, Q ^XA2, Q ^XA3, Q ^XA4, Q ^XA5, Q ^XA6, Q ^XA7, Q ^XA8, Q ^XB1, Q ^XB2, Q ^XB3, Q ^XB4, Q ^XB5And Q ^XB6Represent independently of one another Sauerstoffatom or sulphur atom.

R ^XA1, R ^XA2, R ^XA3, R ^XA4, R ^XA5, R ^XA6, R ^XA7, R ^XA8, R ^XA9, R ^XA10, R ^XA11, R ^XA12, Q ^XB1, Q ^XB2, Q ^XB3, Q ^XB4, Q ^XB5, Q ^XB6, Q ^XB7, Q ^XB8And Q ^XB9Represent independently of one another hydrogen atom, low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl or aryl.

In compound (I), Y represents OY ¹, NY ²T ³, ST ⁴, SO ₂Y ⁵Or N=C (Y ⁶) ₂

Y ¹The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁵¹) X ^A1, C (=O) OY ^B1, C (=Q ⁵²) NY ^D1Y ^E1, S (O) _pY ^F1Or N (Y ^I1) ₂,

And preferably mention the optional low alkyl group that replaces, the optional aryl that replaces or the optional heterocyclic radical that replaces arranged, and particularly preferably mention the optional low alkyl group that replaces, optional aryl or the heterocyclic radical that replaces arranged.

For Y ¹Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ¹Term " optional replace low alkyl group " in substituting group, can mention above-mentioned to X ¹" substituting group ", and preferably mention the optional aryl that replaces or the optional heterocyclic radical that replaces, the optional aromatic hydrocarbons that replaces of at least one low alkyl group of serving as reasons of particularly preferably mentioning or halogen or the heterocyclic radical that is replaced by at least one halogen arranged.

For Y ¹Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For Y ¹Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ¹Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ¹Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ¹Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ¹Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ¹Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ¹Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ¹Term " optional replace aryl " in substituting group, can mention above-mentioned to X ¹" substituting group ", and preferably mention halogen, low alkyl group, cyano group and nitro arranged.

For Y ¹Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ¹Term " optional replace heterocyclic radical " in substituting group, can mention above-mentioned X ¹" substituting group ".

For Y ¹Term " optional replace low-grade cycloalkyl ", " the optional low-grade alkenyl that replaces ", the substituting group in " the optional lower alkenyl ring that replaces " and " low-grade alkynyl of optional replacement " can be mentioned above-mentioned to X ¹" substituting group ".

For Q ⁵¹, Y ^A1, Y ^B1, Q ⁵², Y ^D1, Y ^E1, Y ^F1And Y ^I1, can mention after a while described group.

Y ³The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁶¹) Y ^A2, C (=O) OY ^B2, C (=Q ⁶²) NY ^D2Y ^E2, SO ₂Y ^F2, NY ^G2Y ^H2, N=C (Y ^I2) ₂, OY ^K2Or cyano group,

And the low alkyl group that the replacement chosen wantonly is arranged of preferably mentioning, or the optional aryl that replaces, and low alkyl group or the aryl that optional replacement is arranged mentioned especially.

For Y ²Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ²Term " optional replace low alkyl group " in substituting group, can mention above-mentioned to X ¹" substituting group ", and preferably mention aryl arranged.

For Y ²Above-mentioned " senior alkyl " in, above-mentioned " senior alkyl " can be mentioned.

For Y ²Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ²Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ²Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ²Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ²Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ²Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ²Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ²Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ²Term " optional replace low-grade cycloalkyl ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", substituting group in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

For Q ⁶¹, Y ^A2, Y ^B2, Q ⁶², Y ^D2, Y ^E2, Y ^F2, Y ^G2, Y ^H2, Y ^I2And Y ^K2, can mention after a while described group.

Y ³The expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, C (=Q ⁷¹) Y ^A3, C (=O) OY ^B3, C (=Q ⁷²) NY ^D3Y ^E3Or SO ₂Y ^F3,

And preferably mention the optional low alkyl group that replaces arranged, and mention especially low alkyl group arranged.

For Y ³Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ³Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For Y ³Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ³Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ³Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ³Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ³Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ³Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ³Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ³Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ³Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", substituting group in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

For Q ⁷¹, Y ^A3, Y ^B3, Q ⁷², Y ^D3, Y ^E3And Y ^F3, can mention after a while described group.

And the low alkyl group that optional replacement is arranged of preferably mentioning, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional aryl that replaces or the optional heterocyclic radical that replaces, and the low alkyl group that optional replacement is arranged of mentioning especially,, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, optional aryl or the heterocyclic radical that replaces.

For Y ⁴Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ⁴Term " optional replace low alkyl group " in substituting group, can mention above-mentioned to X ¹" substituting group ", and preferably mention the optional aryl that replaces, the aryl that at least one halogen of serving as reasons of particularly preferably mentioning replaces arranged.

For Y ⁴Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For Y ⁴Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ⁴Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ⁴Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ⁴Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ⁴Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ⁴Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ⁴Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ⁴Term " optional replace aryl " in substituting group, can mention above-mentioned to X ¹" substituting group ", and preferably mention halogen, low-grade halogenated alkyl, lower alkoxy and elementary halogenated alkoxy arranged.

For Y ⁴Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ⁴Term " optional replace low-grade cycloalkyl ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", the substituting group in " the optional low-grade alkynyl that replaces " and " heterocyclic radical of optional replacement " can be mentioned above-mentioned to X ¹" substituting group ".

For Q ⁸¹, Y ^A4, Y ^B4, Q ⁸², Y ^D4, Y ^E4And Y ^F4, can mention after a while described group.

Y ⁵The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

For Y ⁵Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ⁵Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For Y ⁵Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ⁵Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ⁵Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ⁵Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ⁵Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ⁵Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ⁵Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ⁵Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ⁵Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", substituting group in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

Perhaps, the carbon representative ring structure that is bonded to each other with them.

For Y ⁶Term " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For Y ⁶Above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For Y ⁶Term " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For Y ⁶Term " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For Y ⁶Above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For Y ⁶Term " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For Y ⁶Term " optional replace low-grade alkynyl " in above-mentioned " low-grade alkynyl ", above-mentioned " low-grade alkynyl " can be mentioned.

For Y ⁶Above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For Y ⁶Term " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For Y ⁶Term " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For Y ⁶Term " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", substituting group in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned X ¹" substituting group ".

For Y ^L6, Y ^M6, Y ^G6And Y ^H6, can mention following group.

For by each Y ⁶With " ring structure " that its carbon connected to one another represents, can mention with by each X ⁷The structure that above-mentioned " ring structure " that represents together with its carbon connected to one another is identical.

In compound (I), Z represents cyano group, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ⁹¹) Z ^A, C (=O) OZ ^B, C (=Q ⁹²) NZ ^DZ ^E, SO ₂Z ^F, NZ ^GZ ^H, OZ ^KOr N=C (Z ^I) ₂,

And the aryl that optional replacement is arranged of preferably mentioning, optional heterocyclic radical or the SO that replaces ₂Z ^F(wherein, Z ^FBe the optional aryl that replaces), the aryl for optional replacement of particularly preferably mentioning, heterocyclic radical or SO ₂Z ^F(wherein, Z ^FBe aryl).

For above-mentioned " low alkyl group " in the term " the optional low alkyl group that replaces " of Z, above-mentioned " low alkyl group " can be mentioned.

For Z above-mentioned " senior alkyl ", above-mentioned " senior alkyl " can be mentioned.

For above-mentioned " low-grade cycloalkyl " in the term " the optional low-grade cycloalkyl that replaces " of Z, above-mentioned " low-grade cycloalkyl " can be mentioned.

For above-mentioned " low-grade alkenyl " in the term " the optional low-grade alkenyl that replaces " of Z, above-mentioned " low-grade alkenyl " can be mentioned.

For Z above-mentioned " senior thiazolinyl ", above-mentioned " senior thiazolinyl " can be mentioned.

For above-mentioned " lower alkenyl ring " in the term " the optional lower alkenyl ring that replaces " of Z, above-mentioned " lower alkenyl ring " can be mentioned.

For above-mentioned " low-grade alkynyl " in the term " the optional low-grade alkynyl that replaces " of Z, above-mentioned " low-grade alkynyl " can be mentioned.

For Z above-mentioned " senior alkynyl ", above-mentioned " senior alkynyl " can be mentioned.

For above-mentioned " aryl " in the term " the optional aryl that replaces " of Z, above-mentioned " aryl " can be mentioned.

For the substituting group in the term " the optional aryl that replaces " of Z, can mention above-mentioned to X ¹" substituting group ", and preferably mention halogen, nitro, cyano group, hydroxyl, low alkyl group, low-grade halogenated alkyl, low-grade alkenyl, lower alkoxy, low-grade alkane acidyl oxygen base, aryl, heterocyclic radical, lower alkylthio, low alkyl group sulfinyl, low alkyl group alkylsulfonyl or arylthio arranged.

For above-mentioned " heterocyclic radical " in the term " the optional heterocyclic radical that replaces ", above-mentioned " heterocyclic radical " can be mentioned.

For term " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", substituting group in " the optional low-grade alkynyl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

For Q ⁹¹, Z ^A, Z ^B, Q ⁹², Z ^D, Z ^E, Z ^F, Z ^G, Z ^H, Z ^KAnd Z ^I, can mention after a while described group.

X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^AThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z _ATerm " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace low-grade alkynyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For X ^A1, X ^A2, X ^A3, X ^A4, Y ^A1, Y ^A2, Y ^A3, Y ^A4And Z ^ATerm " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " substituting group " in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace low alkyl group " in above-mentioned " low alkyl group ", above-mentioned " low alkyl group " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace low-grade cycloalkyl " in above-mentioned " low-grade cycloalkyl ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace low-grade alkenyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace lower alkenyl ring " in above-mentioned " lower alkenyl ring ", above-mentioned " lower alkenyl ring " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace low-grade alkynyl " in above-mentioned " low-grade alkenyl ", above-mentioned " low-grade alkenyl " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace aryl " in above-mentioned " aryl ", above-mentioned " aryl " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace heterocyclic radical " in above-mentioned " heterocyclic radical ", above-mentioned " heterocyclic radical " can be mentioned.

For X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BTerm " optional replace low alkyl group ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " substituting group " in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

To X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BAbove-mentioned " optional replace amino " expression by optional one or the diamino that replaces of following substituting group: the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, the optional acyl group that replaces, the optional formamyl that replaces or by-SO ₂The group that R represents (wherein, R represents the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl or the optional aryl that replaces).

For " low alkyl group " in the substituent term " the optional low alkyl group that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " low alkyl group " can be mentioned.

For " low-grade cycloalkyl " in the substituent term " the optional low-grade cycloalkyl that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For " low-grade alkenyl " in the substituent term " the optional low-grade alkenyl that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " low-grade alkenyl " can be mentioned.

For " lower alkenyl ring " in the substituent term " the optional lower alkenyl ring that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " lower alkenyl ring " can be mentioned.

For " aryl " in the substituent term " the optional aryl that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " aryl " can be mentioned.

For " heterocyclic radical " in the substituent term " the optional heterocyclic radical that replaces " of above-mentioned conduct on " the optional amino that replaces ", above-mentioned " heterocyclic radical " can be mentioned.

For as " substituting group " in the substituent term on " the optional amino that replaces " " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " the optional heterocyclic radical that replaces ", can mention above-mentioned to X ¹" substituting group ".

" substituting group " on " the optional acyl group that replaces " comprises (when this acyl is low-grade alkane acidyl or elementary alkoxy carbonyl),

For example, lower alkylthio (as, C _1-6Alkylthio such as methylthio group, ethylmercapto group, positive rosickyite base, isopropyl sulfenyl, isobutyl sulfenyl etc.), halogen, lower alkoxy, nitro, lower alkoxycarbonyl, Alkoximino be (such as, C _1-6Alkoximino such as methoxyimino, ethoxy imino, just-propoxy-imino-, uncle-butoxy imino-, n-hexyl oxygen base-imino-etc.), and oxyimino.Substituent number is in commutable scope and be 1-5, preferred 1-3.

When this acyl group is aroyl, aryloxy carbonyl, aryl low-grade alkane acidyl, aryl-lower alkoxy carbonyl, 5-6 unit's heterocyclic radical carbonyl or 5-6 unit heterocyclic radical ethanoyl,

Described " substituting group " comprises; for example; low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, lower alkoxy, acyl group, nitro, amino, hydroxyl, cyano group, sulfamyl, sulfydryl, halogen, lower alkylthio (as, C _1-6Alkylthio such as methylthio group, ethylmercapto group, positive rosickyite base, isobutyl sulfenyl etc.) etc.Substituent number is in commutable scope and be 1-5, preferred 1-3.

" substituting group " on " the optional formamyl that replaces " comprises low alkyl group, low-grade cycloalkyl, low-grade alkenyl, lower alkenyl ring, low-grade alkynyl, aryl, heterocyclic radical and acyl group.

" formamyl " is optional to be replaced by one or two above-mentioned substituting group.

X ^D1, X ^D2, X ^D3, X ^D4, Y ^D1, Y ^D2, Y ^D3, Y ^D4And Z ^DRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OG that replaces ^A1, and

Perhaps, X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe nitrogen representative ring structure that is bonded to each other with them.

For " low alkyl group " in the term " the optional low alkyl group that replaces ", above-mentioned " low alkyl group " can be mentioned.

For " low-grade cycloalkyl " in the term " the optional low-grade cycloalkyl that replaces ", above-mentioned " low-grade cycloalkyl " can be mentioned.

For " low-grade alkenyl " in the term " the optional low-grade alkenyl that replaces ", above-mentioned " low-grade alkenyl " can be mentioned.

For " lower alkenyl ring " in the term " the optional lower alkenyl ring that replaces ", above-mentioned " lower alkenyl ring " can be mentioned.

For " low-grade alkynyl " in the term " the optional low-grade alkynyl that replaces ", above-mentioned " low-grade alkynyl " can be mentioned.

For " aryl " in the term " the optional aryl that replaces ", above-mentioned " aryl " can be mentioned.

For " heterocyclic radical " in the term " the optional heterocyclic radical that replaces ", above-mentioned " heterocyclic radical " can be mentioned.

For " substituting group " in term " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " the optional heterocyclic radical that replaces ", can mention above-mentioned to X ¹" substituting group ".

As for " the optional amino that replaces ", can mention X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BIllustrational identical " the optional amino that replaces ".

By X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4" ring structure " of expression, and Z ^DAnd Z ^EMean to comprise nitrogen-atoms as the 3-8 unit heterocyclic radical that becomes annular atoms with its nitrogen connected to one another, and the 3-8 that is mentioned unit (preferably, 5-6 unit) contains nitrogen-atoms as becoming annular atoms, and optional has the 1-3 heteroatoms such as optional oxidized nitrogen-atoms, Sauerstoffatom, optional by one or the nitrogen heterocycle of the sulphur atom of titanium dioxide etc., for example, 1-nitrogen heterocyclic propyl group, 1-aziridinyl (azirinyl), 1-azete base (azetyl), 1-azelidinyl (azetydinyl), 1-perhydro azepine

Base (perhydroazepynyl), 1-perhydroazosynyl, the 1-pyrrolidyl, the 1-pyrrolinyl, the 1-pyrryl, the 1-pyrazolyl, the 1-imidazolyl, 1,2,3-triazole-1-or 2-base, 1,2,4-triazole-1-or 4-base, 1H-TETRAZOLE-1-base, 2H-tetrazolium-2-base, piperidino, the 4-thio-morpholinyl, the 4-morpholinyl, 1-dihydropyridine base, the 1-tetrahydro pyridyl, 2-or 4-oxo-dihydro pyridine-1-base, the 1-tetrahydro-pyrimidine base, 1-perhydro pyrimidyl, 1-dihydrogen triazine base, 1-tetrahydrotriazine base, 2-oxo-dihydro triazine-1-base, 1,4-Evil-4-base, 1,4-thiazine-4-base, 1,3-thiazine-3-base, the 1-piperazinyl, 1-perhydro pyridazinyl, indoles-1-base, indoline-1-base, isoindole-2-base, isoindoline-2-base, 1H-indazole-1-base, 2,3-Er hydrogen benzoxazole-3-base, 2,3-dihydro-benzothiazole-3-base, benzotriazole-1-base, the 7-purine radicals, 9-carbazyl (carbazoyl) etc.; With by make phenyl ring or 3-8 unit (preferably, 5-6 unit) heterocyclic radical (this heterocyclic radical has 1-4 optional oxidized nitrogen-atoms, Sauerstoffatom, or optional by one or the sulphur atom of titanium dioxide) condense the group of acquisition with above-mentioned nitrogen heterocycle.

" containing nitrogen-atoms as the 3-8 unit heterocyclic radical that becomes annular atoms " can be by for X ¹" optional replace aryl " on the identical substituting group that exemplifies of substituting group replace.Substituent number is in commutable scope and be 1-5, preferred 1-3.

X ^F1, X ^F2, X ^F3, X ^F4, Y ^F1, Y ^F2, Y ^F3, Y ^F4And Z ^FThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, or the optional amino that replaces.

As for " the optional amino that replaces ", can mention X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BIdentical " the optional amino that replaces " that exemplifies.

X ^G1, X ^G2, X ^G7, Y ^G2, Y ^G6And Z ^GRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^G1) G ^A1, C (=O) OQ ^B1, C (=Q ^G2) NG ^D1G ^E1Or SO ₂G ^F1, and

X ^H1, X ^H2, X ^H7, Y ^H2, Y ^H6And Z ^HRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces

Perhaps, X ^G1And X ^H1, X ^G2And X ^H2, X ^G7And X ^H7, Y ^G2And Y ^H2, Y ^G6And Y ^H6, and Z ^GAnd Z ^HThe nitrogen representative ring structure that is bonded to each other with them.

For Q ^G1, G ^A1, G ^B1, Q ^G2, G ^D1, G ^E1Or G ^F1, following description can be mentioned.

For term " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " substituting group " in " the optional aryl that replaces " and " the optional heterocyclic radical that replaces " can be mentioned above-mentioned to X ¹" substituting group ".

To by X ^G1And X ^H1, X ^G2And X ^H2, X ^G7And X ^H7, Y ^G2And Y ^H2, Y ^G6And Y ^H6And Z ^GAnd Z ^H" ring structure " that represents with its nitrogen connected to one another is and by X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe structure that above-mentioned " ring structure " that represents together with its nitrogen connected to one another is identical can be mentioned.

X ^I1, X ^I2, Y ^I1, Y ^I2And Z ^IRepresent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the OG that replaces ^A2, SG ^A3, or NG ^G1G ^H1,

For G ^A2, G ^A3, G ^G1And G ^H1, following description can be mentioned.

For by X ^I1, X ^I2, Y ^I1, Y ^I2And Z ^I" ring structure " that represents with its carbon connected to one another is and by each X ⁷The structure that above-mentioned " ring structure " that represents together with its carbon connected to one another is identical can be mentioned.

X ^K2, Y ^K2And Z ^KThe optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^K1) G ^A2, C (=O) OG ^B2, C (=Q ^K2) NG ^D2G ^E2Or SO ₂G ^F2

For Q ^K1, G ^A2, G ^B2, Q ^K2, G ^D2, G ^E2Or G ^F2, following description can be mentioned.

X ^L7, X ^M7, Y ^L6And Y ^M6Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

For " low-grade alkynyl " in the term " the optional low-grade alkenyl that replaces ", above-mentioned " low-grade alkenyl " can be mentioned.

G ^A1, G ^A2And G ^A3Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

For " low-grade alkenyl " in the term " the optional low-grade alkynyl that replaces ", above-mentioned " low-grade alkenyl " can be mentioned.

G ^A1And G ^A2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

G ^B1And G ^B2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces.

As for " optional replace amino ", and to X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BIdentical " the optional amino that replaces " that exemplifies can be mentioned.

G ^D1And G ^D2Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OG that replaces ^D1, and

G ^E1And G ^E2Represent independently of one another hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, or the optional heterocyclic radical that replaces

Perhaps, G ^D1And G ^E1, and G ^D2And G ^E2The nitrogen representative ring structure that is bonded to each other with them.

For term " the optional aryl that replaces " " aryl ", above-mentioned " aryl " can be mentioned.

For " substituting group " in above-mentioned term " the optional low alkyl group that replaces ", " the optional low-grade cycloalkyl that replaces ", " the optional low-grade alkenyl that replaces ", " the optional lower alkenyl ring that replaces ", " the optional low-grade alkynyl that replaces ", " the optional aryl that replaces " and " the optional heterocyclic radical that replaces ", can mention above-mentioned to X ¹" substituting group ".

As for " optional replace amino ", and to X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BIdentical " the optional amino that replaces " that exemplifies explanation can be mentioned.

For by G ^D1And G ^E1, and G ^D2And G ^E2" ring structure " that represents with its nitrogen connected to one another is and by X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe structure that above-mentioned " ring structure " that forms together with its nitrogen connected to one another is identical can be mentioned.

G ^F1And G ^F2The optional low alkyl group that replaces of independently of one another expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, or the optional amino that replaces.

As for " optional replace amino ", and to X ^B1, X ^B2, X ^B3, X ^B4, Y ^B1, Y ^B2, Y ^B3, Y ^B4And Z ^BIllustrational identical " the optional amino that replaces " can be mentioned.

G ^G1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, optional heterocyclic radical, the C (=Q that replaces ^Ga) G ^A1-1, C (=O) OG ^B1-1, C (=Q ^Gb) NG ^D1-1G ^E1-1Or SO ₂G ^F1-1, and

Perhaps, G ^G1And G ^H1The nitrogen representative ring structure that is bonded to each other with them.

For by G ^G1And G ^H1" ring structure " that represents with its nitrogen connected to one another is and to X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe structure that above-mentioned " ring structure " that represents together with its nitrogen connected to one another is identical can be mentioned.

For Q ^Ga, G ^A1-1, G ^B1-1, Q ^Gb, G ^D1-1, G ^E1-1And G ^F1-1, following description can be mentioned.

G ^D1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

G ^A1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

G ^B1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces.

G ^D1-1Expression hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces, optional amino, cyano group or the OL that replaces, and

Perhaps, G ^D1-1And G ^E1-1The nitrogen representative ring structure that is bonded to each other with them.

For by G ^D1-1And G ^E1-1" ring structure " that represents with its nitrogen connected to one another is and by X ^D1And X ^E1, X ^D2And X ^E2, X ^D3And X ^E3, X ^D4And X ^E4, Y ^D1And Y ^E1, Y ^D2And Y ^E2, Y ^D3And Y ^E3, Y ^D4And Y ^E4, and Z ^DAnd Z ^EThe structure that above-mentioned " ring structure " that represents together with its nitrogen connected to one another is identical can be mentioned.

G ^F1-1The optional low alkyl group that replaces of expression, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces, the optional heterocyclic radical that replaces or the optional amino that replaces.

L represents hydrogen atom, the optional low alkyl group that replaces, senior alkyl, the optional low-grade cycloalkyl that replaces, the optional low-grade alkenyl that replaces, senior thiazolinyl, the optional lower alkenyl ring that replaces, the optional low-grade alkynyl that replaces, senior alkynyl, the optional aryl that replaces or the optional heterocyclic radical that replaces.

Q ¹¹, Q ¹², Q ²¹, Q ²², Q ³¹, Q ³², Q ⁴¹, Q ⁴², Q ⁵¹, Q ⁵², Q ⁶¹, Q ⁶², Q ⁷¹, Q ⁷², Q ⁸¹, Q ⁸², Q ⁹¹, Q ⁹², Q ^G1, Q ^G2, Q ^K1, Q ^K2, Q ^GaAnd Q ^GbRepresent independently of one another Sauerstoffatom or sulphur atom.

M represents integer 1 or 2,

And n, p and q represent integer 0 or 2 independently of one another.

Compound (I) can be for example by following preparation method 1-7 preparation.

The preparation method 1

Compound (I) can be by making the compound by formula (II) expression:

(wherein, M ¹The expression leavings group, and other symbol as above defines) react to prepare with the compound that is represented by formula (III):

Y-H (III)

(symbol in this formula as above defines).

For by M ¹The leavings group of expression for example can use halogen, acyloxy (C _1-10Acyloxy is such as the C by the optional replacement of 1-3 halogen _1-6Alkyl-carbonyl oxygen base such as formyl radical oxygen base, acetoxyl group, propionyl oxygen base, trifluoroacetyl oxygen base etc.; By the optional C that replaces of at least one low alkyl group _7-9Benzoyl oxygen base such as benzoyl oxygen base, 4-methyl benzoyl oxygen base etc.; C _1-6Alkoxy-carbonyl oxy such as methoxycarbonyl oxygen base, uncle-butoxy carbonyl oxygen base etc.) or by formula: R ^pSO _rGroup (wherein, the R of expression ^PRepresents low alkyl group or choose the phenyl that replaces wantonly by at least one low alkyl group, and r is integer 0,1 or 2) etc.

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (III) expression, and can be with large excessive in solvent, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (II) expression.

In order to promote reaction and to reduce by product, in some cases,, can obtain a good result by adding under alkali or the effect at alkali in the reaction front and back.For such alkali, can use alkali alcoholate, for example, sodium ethylate, sodium methylate, sodium tert-butoxide etc.; Organic bases as, for example, triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine, DMA etc.; Mineral alkali as, for example, salt of wormwood, yellow soda ash, sodium hydroxide, potassium hydroxide, sodium bicarbonate, saleratus etc.; Metal hydride, for example, lithium hydride, sodium hydride, potassium hydride KH etc.; Or organolithium reagent as, for example, butyllithium, sec.-propyl lithamide etc.The amount of used alkali has no particular limits, as long as it does not have adverse influence to this reaction, and can also large excessive use get final product to be used as solvent simultaneously.

In this reaction, also can use salt and alkali (by aforementioned preparation) by the compound of formula (III) expression.For such salt, the suitable metal-salt that lithium, sodium and potassium are arranged, and the alkaline earth salt of magnesium and calcium etc.The amount of described salt has no particular limits and this salt can be with large excessive use, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (II) expression.

This reaction can use suitable solvent to carry out.Such solvent has no particular limits, as long as it does not generate by product with reaction substrate, reaction reagent and product reaction, and these solvents need solubilizing reaction substrate and reaction reagent.As having of such solvent, for example, aliphatic hydrocrbon such as pentane, hexane, heptane, sherwood oil etc., aromatic hydrocarbon such as benzene, toluene, dimethylbenzene etc., ester such as methyl acetate, ethyl acetate, ethyl formate, ethyl propionate etc., ketone such as acetone, methyl ethyl ketone etc., ether such as ether, dipropyl ether, Di Iso Propyl Ether, dibutyl ether, tetrahydrofuran (THF), dioxane etc., nitrile such as acetonitrile, propionitrile etc., acid amides such as dimethyl formamide, N,N-DIMETHYLACETAMIDE etc., sulfoxide such as methyl-sulphoxide etc., sulfone such as tetramethylene sulfone etc., phosphamide (phosphoric amides) is such as hexamethylphosphoramide etc., halohydrocarbon such as methylene dichloride, chloroform, 1, the 2-ethylene dichloride, tetracol phenixin etc., aromatic amine such as pyridine, picoline, lutidine, quinoline etc., and mixed solvent, water, also has the mixed solvent of these compounds and water.

Temperature of reaction is generally-50 to 200 ℃ approximately, preferred-30 to 150 ℃ approximately.Reaction times is generally about 0.1-96 hour, and preferred 0.1-72 hour, more preferably about 0.1-24 hour.

The preparation of compound methods known in the art and/or the purifying that generate, for example, concentrated, concentrating under reduced pressure, liquid-phase conversion (liquid nature conversion), shift dissolving (transferencedissolution), solvent extraction, distillation, crystallization, recrystallization, chromatography etc.

The preparation method 2

Compound (I) can be by making the compound by formula (IV) expression:

(wherein, X ^P1Expression O, S, NH or NX ², and other symbol as above defines) with by the compound reaction of formula (V) expression and prepare:

X ^P2-M ² (V)

(wherein, X ^P2Expression X ¹, X ³Or X ⁴, M ²The expression leavings group).

For by M ²The leavings group of expression for example can use halogen, acyloxy (C _1-10Acyloxy is such as the C by the optional replacement of 1-3 halogen _1-6Alkyl-carbonyl oxygen base such as formyl radical oxygen base, acetoxyl group, propionyl oxygen base, trifluoroacetyl oxygen base etc.; By the optional C that replaces of at least one alkyl _7-9Benzoyl oxygen base such as benzoyl oxygen base, 4-methyl benzoyl oxygen base etc.; C _1-6Alkoxy-carbonyl oxy such as methoxycarbonyl oxygen base, uncle-butoxy carbonyl oxygen base etc.) or by formula: R ^pSO _rGroup (wherein, the R of expression ^PRepresents low alkyl group or choose the phenyl that replaces wantonly by at least one low alkyl group, and r is integer 0,1 or 2) etc.

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (V) expression, and can be with large excessive in solvent, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (IV) expression.

In order to promote reaction and to reduce by product,, can obtain a good result in some cases by adding under alkali or the effect at alkali in the reaction front and back.As for alkali, can use alkali alcoholate as, for example, sodium ethylate, sodium methylate, sodium tert-butoxide etc.; Organic bases as, for example, triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine, DMA etc.; Mineral alkali as, for example, salt of wormwood, yellow soda ash, sodium hydroxide, potassium hydroxide, sodium bicarbonate, saleratus etc.; Metal hydride, for example, lithium hydride, sodium hydride, potassium hydride KH etc.; Or organolithium reagent as, for example, butyllithium, sec.-propyl lithamide etc.The amount of used alkali has no particular limits, as long as it does not have adverse influence to this reaction, and can also large excessive use get final product to be used as solvent simultaneously.

This reaction can use suitable solvent to carry out.Such solvent has no particular limits, as long as it does not generate by product with reaction substrate, reaction reagent and product reaction, and these solvents need solubilizing reaction substrate and reaction reagent.As having of such solvent, for example, aliphatic hydrocrbon such as pentane, hexane, heptane, sherwood oil etc., aromatic hydrocarbon such as benzene, toluene, dimethylbenzene etc., ester such as methyl acetate, ethyl acetate, ethyl formate, ethyl propionate etc., ketone such as acetone, methyl ethyl ketone etc., ether such as ether, dipropyl ether, Di Iso Propyl Ether, dibutyl ether, tetrahydrofuran (THF), dioxane etc., nitrile such as acetonitrile, propionitrile etc., acid amides such as dimethyl formamide, N,N-DIMETHYLACETAMIDE etc., sulfoxide such as methyl-sulphoxide etc., sulfone such as tetramethylene sulfone etc., phosphamide such as hexamethylphosphoramide etc., halohydrocarbon such as methylene dichloride, chloroform, 1,2-ethylene dichloride, tetracol phenixin etc., aromatic amine such as pyridine, picoline, lutidine, quinoline etc., and mixed solvent, water, the in addition mixed solvent of these compounds and water.

The preparation of compound methods known in the art and/or the purifying that generate, such as, concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, recrystallization, chromatography etc.

The preparation method 3

Compound (I) can be by making the compound by formula (VI) expression:

(wherein, symbol as above defines) reacted with the compound that is represented by formula (VII) and prepared:

X-H (VII)

(wherein, symbol as above defines).

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (VII) expression, and can be with large excessive in solvent, and the preferably amount use to work as with respect to the about 0.8-5 of compound by formula (IV) expression.

The preparation of compound methods known in the art and/or the purifying that generate, for example, concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, recrystallization, chromatography etc.

The preparation method 4

Compound (I) can prepare by the compound of hydrogenation by formula (IIX) expression:

(wherein, symbol as above defines).As for hydrogenant agent, can use hydrogen, formic acid, hydride reagent (as, sodium borohydride, POTASSIUM BOROHYDRIDE, sodium cyanoborohydride etc.).

In this reaction, the amount of above-mentioned hydrogenant agent has no particular limits, and can a large excessive use, and preferably with the amount use of about 0.8-5 equivalent.

In order to promote reaction and to reduce by product, in some cases, by using catalyzer, can obtain a good result.For such catalyzer, for example can use transition-metal catalyst such as palladium-carbon, palladium-barium sulfate, Lindlar catalyzer (palladium-calcium carbonate (lead poisoning)), platinum-carbon, platinum oxide etc.The used amount of catalyzer has no particular limits, and needing only it does not have adverse influence to this reaction, and is preferably the amount with respect to the 0.001-0.1wt% of the compound that is represented by formula (IIX).

The preparation method 5

Compound (I) can be by making the compound by formula (IX) expression:

(wherein, M ³Expression leavings group, and other symbol as above defines) with by the compound reaction of formula (VII) expression and prepare:

X-H (VII)

(symbol in this formula as above defines).

For by M ³The leavings group of expression for example can use halogen, acyloxy (C _1-10Acyloxy is such as the C by the optional replacement of 1-3 halogen _1-6Alkyl-carbonyl oxygen base such as formyl radical oxygen base, acetoxyl group, propionyl oxygen base, trifluoroacetyl oxygen base etc.; By the optional C that replaces of at least one low alkyl group _7-9Benzoyl oxygen base such as benzoyl oxygen base, 4-methyl benzoyl oxygen base etc.; C _1-6Alkoxy-carbonyl oxy such as methoxycarbonyl oxygen base, uncle-butoxy carbonyl oxygen base etc.), lower alkoxy (C _1-6Alkoxyl group such as methoxyl group, oxyethyl group, propoxy-etc.), aryloxy is (by the optional C that replaces of at least one low alkyl group _6-10Aryloxy such as phenoxy group, 4-methylphenoxy, 2-naphthyloxy etc.), two-low-grade alkyl amino (two-C _1-6Alkylamino such as dimethylamino, diethylamino etc.) or by formula: R ^pSO _rGroup (wherein, the R of expression ^PRepresents low alkyl group or choose the phenyl that replaces wantonly by at least one low alkyl group, and r is integer 0,1 or 2) etc.

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (VII) expression, and can be with large excessive in solvent, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (IX) expression.

In order to promote reaction and to reduce by product, in some cases,, can obtain a good result by adding under alkali or the effect at alkali in the reaction front and back.For such alkali, can use alkali alcoholate as, for example, sodium ethylate, sodium methylate, sodium tert-butoxide etc.; Organic bases as, for example, triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine, DMA etc.; Mineral alkali as, for example, salt of wormwood, yellow soda ash, sodium hydroxide, potassium hydroxide, sodium bicarbonate, saleratus etc.; Metal hydride, for example, lithium hydride, sodium hydride, potassium hydride KH etc.; Or organolithium reagent as, for example, butyllithium, sec.-propyl lithamide etc.The amount of used alkali has no particular limits, as long as it does not have adverse influence to this reaction, and can also large excessive use get final product to be used as solvent simultaneously.

In this reaction, can use the compound that represented by formula (VII) and alkali (by aforementioned preparation).An alkali metal salt of lithium, sodium and potassium, and the alkaline earth salt of magnesium and calcium etc. is suitable.The amount of described salt has no particular limits and this salt can be with large excessive use, and preferably with the amount use by the about 0.8-5 equivalent of compound of formula (IX) expression.

The preparation of compound methods known in the art and/or the purifying that generate, for example concentrated, concentrating under reduced pressure, liquid-phase conversion shifts dissolving, solvent extraction, distillation, crystallization, recrystallization, chromatography etc., and separation and/or purifying aftertreatment.

The preparation method 6

Compound (I) can be by making the compound by formula (X) expression:

(wherein, symbol as above defines) reacted with the compound that is represented by formula (XI) and prepared:

Y ^P1-M ⁴ (XI)

(wherein, Y ^P1The optional alkyl that replaces of expression, the optional thiazolinyl that replaces or the optional alkynyl that replaces, M ⁴Expression leavings group and other symbol as above define).

For by M ⁴The leavings group of expression for example can use halogen, acyloxy (C _1-10Acyloxy is such as the C by the optional replacement of 1-3 halogen _1-6Alkyl-carbonyl oxygen base such as formyl radical oxygen base, acetoxyl group, propionyl oxygen base, trifluoroacetyl oxygen base etc.; By the optional C that replaces of at least one alkyl _7-9Benzoyl oxygen base such as benzoyl oxygen base, 4-methyl benzoyl oxygen base etc.; C _1-6Alkoxy-carbonyl oxy such as methoxycarbonyl oxygen base, uncle-butoxy carbonyl oxygen base etc.) or by formula: R ^pSO _rGroup (wherein, the R of expression ^PRepresents low alkyl group or choose the phenyl that replaces wantonly by at least one low alkyl group, and r is integer 0,1 or 2) etc.

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (XI) expression, and can be with large excessive in solvent, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (X) expression.

The preparation of compound methods known in the art and/or the purifying that generate, for example, atomizing (pulverization), concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, redeposition (re-deposition), recrystallization, chromatography, high performance liquid chromatography (HPLC), desalination resin column chromatography etc.

The preparation method 7

Compound (I) can be by making the compound by formula (XII) expression:

(wherein, symbol as above defines) reacted with the compound that is represented by formula (XIII) and prepared:

(Y ^P2) ₃O·BF ₄ (XIII)

(wherein, Y ^P2The optional alkyl that replaces of expression, the optional thiazolinyl that replaces or the optional alkynyl that replaces).

In this reaction, had no particular limits by the amount of the compound of above-mentioned formula (XIII) expression, and can be with large excessive in solvent, and preferably with respect to the amount use by the about 0.8-5 equivalent of compound of formula (XII) expression.

This reaction can use suitable solvent to carry out.Such solvent has no particular limits, as long as it does not generate by product with reaction substrate, reaction reagent and product reaction, and these solvents need solubilizing reaction substrate and reaction reagent.As having of such solvent, for example, aliphatic hydrocrbon such as pentane, hexane, heptane, sherwood oil etc., aromatic hydrocarbon such as benzene, toluene, dimethylbenzene etc., ester such as methyl acetate, ethyl acetate, ethyl formate, ethyl propionate etc., ketone such as acetone, methyl ethyl ketone etc., ether such as ether, dipropyl ether, Di Iso Propyl Ether, dibutyl ether, tetrahydrofuran (THF), dioxane etc., nitrile such as acetonitrile, propionitrile etc., acid amides such as dimethyl formamide, N,N-DIMETHYLACETAMIDE etc., sulfoxide such as methyl-sulphoxide etc., sulfone such as tetramethylene sulfone etc., phosphamide such as hexamethylphosphoramide etc., halohydrocarbon such as methylene dichloride, chloroform, 1, the 2-ethylene dichloride, tetracol phenixin etc., and mixed solvent.

The compound methods known in the art preparation that generates and/or purifying, such as, atomizing, concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, redeposition, recrystallization, chromatography, high performance liquid chromatography (HPLC), desalination resin column chromatography etc.

Compound by above-mentioned preparation method's preparation can also experience methods known in the art; for example, alkylation, alkylene; ethynylation; acidylate, ammonification, sulfuration; sulfurous acidylate (sulfinylation); sulfonation, oxidation, reduction, halogenation, nitrated, crosslinking reaction etc. are to be converted into its substituting group other required substituting group.

The compound that is obtained by above-mentioned preparation method can separate and/or purifying by ordinary method, for example, atomizing, concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, redeposition, recrystallization, chromatography, high performance liquid chromatography (HPLC), desalination resin column chromatography etc.

With reference to the preparation method

Preparation method for the preparation of the compound of compound (I) will be described below.

M wherein ¹The compound (II) of expression halogen atom can be by making the compound by formula (XIV) expression:

Obtain with the halogenating agent reaction.

For the halogenating agent that can be used for this reaction, can mention thionyl chloride, SULPHURYL CHLORIDE, phosphoryl chloride, phosphorus pentachloride, tetracol phenixin, carbon tetrabromide etc.

In this reaction, the amount of above-mentioned halogenating agent has no particular limits, and can be used as solvent with excessive greatly, and preferably uses with the amount with respect to the about 0.8-5 equivalent of compound that is represented by formula (XIV).

In order to promote reaction and to reduce by product, in some cases,, can obtain a good result by adding under alkali or the effect at alkali in the reaction front and back.For such alkali, can use organic bases as, for example, triethylamine, diisopropylethylamine, pyridine, 4-dimethylaminopyridine, DMA etc.; Metal hydride, for example, lithium hydride, sodium hydride, potassium hydride KH etc.; Organolithium reagent as, for example, butyllithium, di-isopropyl lithamide etc.; Or phosphorus compound as, for example, triphenyl phosphine etc.The amount of used alkali has no particular limits, as long as it does not have adverse influence to this reaction, and can also large excessive use get final product to be used as solvent simultaneously.

This reaction can use suitable solvent to carry out.Such solvent has no particular limits, as long as it does not generate by product with reaction substrate, reaction reagent and product reaction, and these solvents need solubilizing reaction substrate and reaction reagent.As having of such solvent, for example, aliphatic hydrocrbon such as pentane, hexane, heptane, sherwood oil etc., aromatic hydrocarbon such as benzene, toluene, dimethylbenzene etc., ester such as methyl acetate, ethyl acetate, ethyl formate, ethyl propionate etc., ketone such as acetone, methyl ethyl ketone etc., ether such as ether, dipropyl ether, Di Iso Propyl Ether, dibutyl ether, tetrahydrofuran (THF), dioxane etc., nitrile such as acetonitrile, propionitrile etc., acid amides such as dimethyl formamide, N,N-DIMETHYLACETAMIDE etc., sulfoxide such as methyl-sulphoxide etc., sulfone such as tetramethylene sulfone etc., phosphamide such as hexamethylphosphoramide etc., halohydrocarbon such as methylene dichloride, chloroform, 1, the 2-ethylene dichloride, tetracol phenixin etc., aromatic amine such as pyridine, picoline, lutidine, quinoline etc., and mixed solvent.

The preparation of compound methods known in the art and/or the purifying that generate, for example, filter, atomizing, concentrated, concentrating under reduced pressure, transfer dissolving, solvent extraction, distillation, crystallization, redeposition, recrystallization etc., and separation subsequently and/or purifying, perhaps for its reaction mixture, can be used as the raw material of following reaction.As the compound of the initial substance of this reaction be known compound maybe can prepare by currently known methods (Chem.Pharm.Bull.48, P1854,2000, etc.).

Compound by formula (III) expression belongs to, for example, and mercaptan, alcohol, phenol, primary amine or secondary amine, and these maybe can prepare by currently known methods for known compound.

By the compound of formula (VI) expression be known compound maybe can prepare by currently known methods (Chem.Lett.P1261,1989, Chem.Berichte 109, P1643,1976, etc.).

Compound by formula (VII) expression belongs to, for example, and mercaptan, alcohol, phenol, primary amine or secondary amine, and these maybe can prepare by currently known methods for known compound.

That known compound maybe can prepare by currently known methods (Chem.Lett.P1261,1989, etc.) by the compound of formula (IIX) expression.

Can also experience methods known in the art by above-mentioned preparation method 1-7 with reference to the compound of preparation method preparation; for example; alkylation, alkylene, ethynylation, arylation, heteroaryl, acidylate, ammonification, sulfuration, sulfurous acidylate, sulfonation, oxidation, reduction, halogenation, nitrated etc. are to be converted into its substituting group other required substituting group.

Can be separated and/or purifying, for example by ordinary method atomizing, concentrated, concentrating under reduced pressure, liquid-phase conversion, transfer dissolving, solvent extraction, distillation, crystallization, redeposition, recrystallization, chromatography, high performance liquid chromatography (HPLC), desalination resin column chromatography etc. by above-mentioned preparation method 1-7 and the compound that obtains with reference to the preparation method.

Also can obtain with the form of its hydrate by above-mentioned preparation method 1-7 with reference to the compound that the preparation method obtains, and its hydrate is also included within the scope of the invention.

For compound (I); substituent acidic groups such as alkylsulfonyl, carboxyl can form the basic salt of acceptable mineral alkali, organic bases etc. on the Pesticide Science on the molecule, and the amino in the basic group on the molecule such as basic nitrogen atom, the substituting group etc. can form the acid salt of acceptable mineral acid, organic acid etc. on the Pesticide Science.

Inorganic base salts comprises, for example, basic metal (sodium, potassium etc.), the salt of alkaline-earth metal (calcium etc.) and ammonia, and inorganic base salts comprises, for example, with dimethylamine, triethylamine, N, accelerine, piperazine, tetramethyleneimine, piperidines, pyridine, 2-phenyl-ethyl amine, benzylamine, thanomin, diethanolamine, 1, the salt that 8-diazabicyclo [5.4.0] undecylene (after this, referred to as DBU) etc. becomes.

Inorganic acid addition salt comprises, for example, the salt that becomes with hydrochloric acid, Hydrogen bromide, hydroiodic acid HI, sulfuric acid, nitric acid, phosphoric acid and perchloric acid, and organic acid addition salt comprises, for example, salt that becomes with trifluoroacetic acid with formic acid, acetic acid, propionic acid, oxalic acid, succsinic acid, phenylformic acid, p-toluenesulphonic acids, methanesulfonic etc.

Each compound (I) can contain steric isomer as based on the optical isomer of one or more unsymmetrical carbons with based on geometrical isomer of one or more pairs of keys etc.Such isomer and composition thereof also is included in the scope of the present invention fully.

Compound (I) can comprise isomer such as tautomer, geometrical isomer, steric isomer etc., and within the scope of the present invention, these isomer and composition thereof all are included in the formula (I).

Some compounds (I) are the form (for example, hydrate etc.) of solvate, and these forms are also included within the scope of the invention.

Some compounds (I) are the form of crystallization and/or amorphous substance, and these forms are also included within the scope of the invention.

In the present invention, some compounds are the form of prodrug, and these forms are also included within the scope of the invention.

Compound (I) is effectively controlled the parasite of sanitary insect pest and animal and plant, and demonstrates very strong biocidal activity by the animal and plant that reaches of processing the insect parasitism.In addition, compound (I) only has seldom phytotoxin effect to plant, and fish are had seldom toxicity, thereby has safe and favourable character and be used for health, livestock industry, pet, gardening and agricultural as sterilant.

When compound (I) is used as sterilant, during especially as insecticide, compound uses with the form of Pesticides and veterinary drugs usually, namely with formulation such as emulsion, solution, microemulsion, preparation easily flows, oily solution, wettable powder, powder, particle, fine particle, seed coating agent (a seedcoating agent), fumigant, tablet, microcapsule, sprays, aerosol, carbon dioxide agent, hot fumigant such as mosquito-repellent incense, electricity mosquito sheet and electric insecticidal solution (electric insecticidal solution), the EW agent, ointment, poison bait, pill, injection, resin formulation, the uses such as shampoo, even method be by make as one or both of activeconstituents more kinds of (preferably one or more, and being no more than three kinds) compound (I) or its salt is dissolved or dispersed in the suitable liquid vehicle, or mix with suitable solid carrier (depending on application target) or be adsorbed in the suitable solid carrier.For these preparations, if necessary, can add emulsifying agent, suspending agent, developer, permeate agent, wetting agent, thickening material, stablizer etc., and they can prepare by methods known in the art.That is, insect-killing composition of the present invention comprises compound (I) or its salt and the inert support as activeconstituents.

For the liquid vehicle (solvent) that uses, for example, solvent such as water, alcohol is (such as methyl alcohol, ethanol, n-propyl alcohol, Virahol, benzylalcohol, ethylene glycol etc.), ketone is (such as acetone, methyl ethyl ketone, methyl iso-butyl ketone (MIBK), pimelinketone etc.), ether is (such as tetrahydrofuran (THF), methyl glycol, methyl carbitol, Diethylene Glycol one ether, propylene glycol monomethyl ether etc.), aliphatic hydrocrbon is (such as oil, kerosene, heavy oil, machine oil etc.), aromatic hydrocarbon is (such as toluene, dimethylbenzene, solvent naphtha, methylnaphthalene etc.), halohydrocarbon is (such as methylene dichloride, chloroform, tetracol phenixin etc.), acid amides is (such as N, dinethylformamide, N,N-dimethylacetamide, N-Methyl pyrrolidone etc.), ester is (such as ethyl acetate, butylacetate, glycerin fatty acid ester, gamma-butyrolactone etc.), nitrile is (such as acetonitrile, propionitrile etc.), carbonic ether (such as propylene carbonate etc.), vegetables oil is (such as rapeseed oil, the cottonseed wet goods) etc. be suitable for.Use suitably even these carriers can one or both be multiple by mixing with suitable ratio (preferably one or more, and be no more than three kinds).

As for solid carrier (thinner, buffer reagent), can use Vegetable powder (such as powdered soybean, tobacco powder, the wheat powder, wood powder etc.), mineral dust is (such as clay such as kaolin, wilkinite, acid clay etc., talcum such as talcum powder, agalmatolite powder etc., silicon-dioxide such as diatomite, mica powder etc.), alumina, the sulphur powder, activated carbon, calcium carbonate, Repone K, ammonium sulfate, sodium bicarbonate, lactose, urea etc., and these carriers can even one or both be multiple by mixing with suitable ratio (preferably one or more, and be no more than three kinds) and use suitably.

As for carrier gas, for example, can use fluorocarbon, butagas, LPG (liquefied petroleum gas (LPG)), dme, carbonic acid gas etc., and these carriers can use suitably by mix one or both with suitable ratio.

In addition, for the ointment base raw material, for example, even one or both are multiple (preferably, one or more, and be no more than three kinds) be selected from the polyol ester of polyoxyethylene glycol, pectin, higher fatty acid such as glyceryl monostearate etc., derivatived cellulose such as methylcellulose gum etc., sodiun alginate, wilkinite, higher alcohols, polyvalent alcohol such as glycerine etc., Vaseline, white vaseline, whiteruss, lard, each vegetable oil, lanolin, anhydrous lanolin, the raw material of winterized stearin, resin etc., or these raw materials that following various tensio-active agent adds wherein can use aptly.

For the tensio-active agent as emulsifying agent, developer, permeate agent, dispersion agent etc., according to whether essential, can use aptly nonionic and anion surfactant such as soap, and polyoxyethylene alkylaryl ether [such as Neugen (trade(brand)name), EA142 (trade(brand)name); By Dai-ichiKogyo Seiyaku Co., Ltd produces, Nonal (trade(brand)name); By Toho ChemicalIndustries Co., Ltd produces], and alkyl-sulphate [such as Emar 10 (trade(brand)name), Emar 40 (trade(brand)name); Produced by Kao Corporation], and alkylbenzene sulfonate [such as Neogen (trade(brand)name), Neogen T (trade(brand)name); By Dai-ichi Kogyo Seiyaku Co., Ltd produces, Neoperex; Produced by Kao Corporation], polyethylene alkyl ether [as, Neugen ET-135 (trade(brand)name); By Dai-ichi Kogyo Seiyaku Co., Ltd produces], polyoxyethylene polyoxypropylene block copolymer [as, Nonipol PE-64 (trade(brand)name); By Sanyo Chemical Industries, Ltd produces], and polyol ester [such as polysorbas20 (trade(brand)name), tween 80 (trade(brand)name); Produced by KaoCorporation], alkyl sulfo succinate is [such as Sanmolin OT20 (trade(brand)name); By Sanyo Chemical Industries, Ltd produces, Newcalgen EX70 (trade(brand)name); By Takemoto Oil ﹠amp; Fat Co., Ltd produces], sulfonated alkyl naphathalene is [such as Newcalgen WG-1 (trade(brand)name); By Takemoto Oil ﹠amp; Fat Co., Ltd produces], alkenyl sulphonate is [such as Solpol5115 (trade(brand)name); By Toho Chemical Industries Co., Ltd produces] etc. can use suitably by mix one or both with suitable ratio with these tensio-active agents.In addition, compound (I) also can with for example, other agricultural chemicals (pyrethroid insectide, organic phosphorous insecticide, carbamate pesticide, intend anabasine (neonicotinoid) sterilant, natural insecticide etc.), miticide, machine oil, nematocides, weedicide, the plant hormone medicine, plant growth regulating substance, mycocide is (such as the copper fungicide agent, organochlorine mycocide, organic sulfur fungicide, phenol mycocide etc.), synergistic agent, attractant insecticide, repellent, the drug damages light-weight additive, pigment, fertilizer, animal-feed (the feed that is used for livestock such as ox, pig and chicken, the feed that is used for pet such as dog and cat, the feed that is used for pisciculture such as brisling and sea bream), veterinary drug (breed fish treatment or prevention livestock, the medicine of pet and fish), nutrient substances for animals etc. mix and use aptly.

The ratio of the compound (I) that insect-killing composition of the present invention is contained is generally the about 0.1-80% weight with respect to the said composition total amount, preferably about 1-20% weight.Particularly, when compound is used as emulsion, when solution or wettable powder (such as the wettable powder of particulate state), usually be suitably for about 1-80% weight, preferably about 1-20% weight.When as oily solution or powder, usually be suitably for about 0.1-50% weight, preferably about 0.1-20% weight.When using with particle form, usually be suitably for about 1-50% weight, preferably about 1-20% weight.

Be mixed in activeconstituents (such as Insecticides (tech) ﹠ Herbicides (tech), miticide and/or mycocide) on other the agricultural chemicals in the insect-killing composition of the present invention usually with the about 0.1-80% weight with respect to the preparation total amount, preferably the scope of about 1-20% weight is used.

According to the kind of activeconstituents or the difference of consumption or preparation formulation, the amount of the additive of non-aforementioned activeconstituents can change, and is generally about 0.001-99.9% weight, preferably about 1-99% weight.The most particularly, the common preferred about 1-20% weight that adds with respect to the said composition total amount, the tensio-active agent of 1-15% weight more preferably from about, the glidant of about 1-20% weight, and about 1-90% weight, the preferably carrier of about 1-70% weight.Particularly, when the preparation solution, usually preferably add about 1-20% weight, the tensio-active agent of preferred 1-10% weight, and the water of about 20 to, 90% weight.Emulsion or wettable powder (such as the wettable powder of particulate state) answer water suitably to dilute (according to appointment 100-5,000-doubly) to be used for spraying.

Can mix with compound of the present invention (I) or its salt the mycocide that uses, plant hormone medicine, plant growth regulating substance, weedicide, and agricultural chemicals such as sterilant, (comprising isomer and salt thereof) such as miticide and nematocidess is that representative instance is as follows.

(1) organo phosphorous compounds

Ortho 12420, aluminium phosphide, special Pyrimitate, cadusafos, earth worm chlorine phosphorus, Zaprawa enolofos, Chlorpyrifos 94, chlorpyrifos_methyl, cynock (CYAP), diazinon, DCIP (dichloro Di Iso Propyl Ether), dichlofenthion (ECP), SD-1750 (DDVP), Rogor, N-nitrosodimethylamine, thiodemeton, EPN, Nialate, kairine goes out, the oxygen Pyrimithate, Tiguvon (MPP), Sumithion (MEP), thiazolone phosphorus, the peace fruit, phosphuret-(t)ed hydrogen, the third ammonia phosphorus karphos, the Malathion, the first oxydemeton_methyl, methidathion (DMTP), monocrotophos, naled (BRP), Thiometan (ESP), thiophos, Gophacide, R-1504 (PMP), pirimiphosmethyl, Ofunack, diethquinalphione, Tsidial (PAP), Profenofos, Kayaphos, Toyodan, pyraclofos, dioxabenzofos, the second Toyodan, Tebupirimphos, temephos, tetrachlorvinphos, Terbufos, thiometon, Trichlorphon (DEP), vamidothion etc.;

(2) carbamate compounds

Alanycarb, bendiocarb, the third phosphorus carbofuran, BPMC, carbaryl, carbofuran, fourth phosphorus carbofuran, cloethocarb, benzene worm prestige, Osbac, fenothiocarb, ABG-6215, furathiocarb, Ro 7-5050 (MIPC), meta-tolyl-N-methylcarbamate (MTMC), methomyl, metmercapturon, NAC, oxamyl, Aphox, Propoxur (PHC), XMC, UC-51762, xylylcarb etc.;

(3) synthetic pyrethroid compound

Fluorine ester chrysanthemum ester, esbiothrin, visit Funing (benfluthrin), β-cyfloxylate, bifenthrin, cycloprothrin, cyfloxylate, cyhalothrin, Cypermethrin, Deltamethrin, esfenvalerate, ether chrysanthemum ester, Fenvalerate, fenvalerate, fluoro-Cyano chrysanthemate, flufenoprox, flumethrin, taufluvalinate, halogen ether chrysanthemum ester, miaow alkynes chrysanthemum ester, permethrin, prallethrin, worm chrysanthemum ester falls, benzyl furan chrysanthemum, σ-Cypermethrin, deinsectization silicon ether, tefluthrin, tralomethrin, transfluthrin, 2,3,5,6-tetrafluoro-4-(methoxymethyl) benzyl (EZ)-(1RS, 3RS; 1RS, 3SR)-2,2-dimethyl-3-third-1-thiazolinyl cyclopropanecarboxylcompound, 2,3,5,6-tetrafluoro-4-methyl-benzyl (EZ)-(1RS, 3RS; 1RS, 3SR)-2,2-dimethyl-3-third-1-thiazolinyl cyclopropanecarboxylcompound, 2,3,5,6-tetrafluoro-4-(methoxymethyl) benzyl (1RS, 3RS; 1RS, 3SR)-2,2-dimethyl-3-(2-methyl-1-propylene base) cyclopropanecarboxylcompound etc.;

(4) nereistoxin compound

Cartap, bensultap, thiocyclarn, desinsection list, disosultap etc.;

(5) intend the anabasine compound

Provado, nitenpyram, pyrrole worm are clear, Diacloden (thiamethoxam), thiacloprid (thiacloprid), nitre monooctyl ester, clothianidin (clothianidin) etc.;

(6) benzoyl carbamide compound

UC 62644, bistrifluron (bistrifluron), kill that mite sulphur is grand, diflubenzuron, fluorine fluazuron, flucycloxuron, flufenoxuron, HEXAFLUMURON, fluorine benzyloxy urea, Rimon, noviflumuron (noviflumuron), Teflubenzuron, desinsection are grand etc.;

(7) phenyl pyrazole compounds

Acetyl worm nitrile (Acetoprole), ethiprole (ethiprole), Frontline, fluorine pyrazoles worm, ethiprole (pyriprole), pyrazoles ethiprole (pyrafluprole) etc.;

(8) Bt toxin

Live spore and by bacillus thuringiensis derive and the crystalline toxin that produces, and composition thereof;

(9) hydrazine compound

Can fragrant promise (Chromafenozide), RH 0345, Runner, RH-5992 etc.;

(10) organochlorine compound

Aldrin, Dieldrin-attapulgite mixture, Hooker HRS 16,5a,6,9,9a-hexahydro-6,9-methano-2,4, methoxychlor etc.;

(11) natural insecticide

Machine oil, nicotine-sulfuric ester etc.;

(12) other sterilant

Avermectin-B, ester bromopropionylamino, Buprofezin, Chlorfenapyr (chlorphenapyr), cyromazine, D-D (1, the 3-dichloropropylene), emamectin-benzoate (emamectin-benzoate), fenazaquin, pyrrole fluorine sulphur phosphorus (flupyrazofos), Entocon ZR 512 oxadiazole worm, metoxadiazone, beautiful times mycin (milbemycin)-A, pymetrozine, pyridalyl (pyridalyl), pyriproxyfen, SPINOSAD, sulfluramid, Tolfenpyrad (tolfenpyrad), triaxamate, flubendiamide, SI-0009, cyflumetofen, arsenic acid, benclothiaz, nitrolim(e), many sulfurations, Niran, DDT, DSP, Flubendiamide (flufenerim), flonicamid (flonicamid), flurimfen, formetanate, metamsodium-ammonium salt, metamsodium-sodium, monobromomethane, nidinotefuran, potassium oleate, protrifenbute, Spiromesifen (spiromesifen), sulphur, metaflumizone, spiral shell worm ethyl ester (spirotetramat), metadiazine (pyrifluquinazon), chlorantraniliprole (Chlorantraniliprole)

The compound of a kind of formula (A) expression

[wherein, R ¹Expression methyl, chlorine atom, bromine atoms or fluorine atom, R ²Expression fluorine atom, chlorine atom, bromine atoms C _1-4Haloalkyl or C _1-4Halogenated alkoxy, R ³Expression fluorine atom, chlorine atom or bromine atoms, R ⁴The expression hydrogen atom; By methoxyl group, the optional C that replaces of one or more halogen atoms, cyano group, methylthio group, methylsulfinyl or methyl sulphonyl _1-4Alkyl; C _3-4Thiazolinyl; C _3-4Alkynyl; Or C _3-5Cycloalkyl, R ⁵Expression hydrogen atom or methyl, R ⁶Expression hydrogen atom, fluorine atom or chlorine atom, R ⁷Expression hydrogen atom, fluorine atom or chlorine atom] etc.

Miticide (being used for acaricidal activeconstituents) comprises, for example, acequinocyl, amitraz, benzoximate (benzoximate), Bifenazate, ester bromopropionylamino, chinomethionate, Ovotran, CPCBS (chlorfenson), clofentezine, cyflumetofen (cyflumetofen), clean (Mitigan) Te Ben oxazole of mite, fenbutatin oxide, fenothiocarb, fenpyroximate, Fluacrypyrim (fluacrypyrim), fluproxyfen, hexythiazox (hexythiazox), propargite (BPPS), polynactin, pyridaben, the pyramine phenylate, tebufenpyrad, tetradifon, spirodiclofen (spirodiclofen), amidoflumet etc.

The nematocides activeconstituents of nematocides (be used for) comprises, for example, and DCIP, thiazolone phosphorus, levamisole, Trapex (methyisothiocyanate), tartrate trimethylammonium pyrantel (morantel tartarate) etc.

Fungicide comprises, for example, and thiadiazoles element-S-methyl, ambam, the phenalgin phosphonic acids, anilazine, the nitrile Fluoxastrobin, M 9834 (benalaxyl), benodanil, benomyl, benzene metsulfovax (benthiavalicarb), benzene thiophene bacterium clear (benthiazole), betulin (bethoxazin), Bitertanol, blasticidin S-S, bordeaux mixture, Boscalid (boscalid), bromuconazole, buthiobate, calcium hypochlorite, calcium polysulfide, captan, carbendazim, carboxin, carpropamide, the pest of going out azoles, chloroneb, trichloronitromethane, Bravo (TPN), chlormephos, cinnamic acid, clozylacon, CNA (2, the 6-Dichloro-4-nitroaniline), Kocide SD, copper sulphate, cyazofamid (cyazofamid), cyfluphenamid, cymoxanil, cyproconazole, encircle the third pyrimidine, cyprofuram, dazomet, two ethoxy imidazoles prestige, Euparen, D-D (1,3-dichloropropylene), frost chlorine zarilamid (diclocymet), diclomezine, the mould prestige of second, Difenoconazole, the fluorine mepanipyrim, dimefluazole, Milcurb, dimethomorph, alkene azoles alcohol-M, dinocap, Hinosan, oxole bacterium, nickel dimethyldithiocarbamate, etaconazole, Guardian (ethaboxam), Milstem, kobam, the azolactone bacterium, Fenamidone (fenamidone), fenarimol, RH-7592, Fendazosulam, fenhexamid (fenhexamid), fenoxanil (fenoxanil), fenpiclonil, fenpropidin, butadiene morpholine, celdion, fentin hydroxide, ferimzone, fluazinam, Fu Evil bacterium, fluorine biphenyl bacterium, flumorph, fluorine bacterium amine (fluoroimide), the spirit of bacterium azoles, fluoxastrobin (fluoxastrobin), Fluquinconazole, Flusilazole, flusulfamide, flutolanil, Flutriafol, fosetyl-Al, Rabcide, fuberidazole, Furalaxyl, the spirit of furan pyrazoles, sterilizing amine, furconazole_cis, own azoles alcohol, hydroxyisoxazole, IBP, IMAZALIL, the acid amides azoles, biguanide spicy acid salt-albesilate, biguanide spicy acid salt, propiconazole (iodocarb), cycltebuconazole, isopropyl is fixed, the third gloomy suffering (iprovalicarb), Isoprothiolane, kasugarnycin, the imines bacterium, Mancozeb, maneb, mepanipyrim, mepronil, metalaxyl, Metalaxyl-M, metham-sodium-sodium, methasulfocarb (methasulfocarb), methyl bromide, encircle penta azoles bacterium, the first methuroxam, fork phenalgin acid amides, metrafenone (metrafenone), metsulfovax, midolthromycin, milneb, nitrile bacterium azoles, myclozolin, Dithane A40, orysastrobin (orysastrobin), fenfuram, the spirit of Evil frost, Oxolinic Acid, Evil imidazoles (oxpoconazole), oxycarboxin, terramycin, pefurazoate, penconazole, sterilization is grand, ZEN 90160 (picoxystrobin), polyurethanes, polyoxin, saleratus, probenazole, the third ammonia spirit, the sterilization profit, the clever mono-hydrochloric salts of hundred dimensions, propiconazole, antracole, the third oxygen quinoline (proquinazid), prothiocarb, prothioconazoles (prothioconazole), pyracarbolid, pyraclostrobin (pyraclostrobin), Ppyrazophos, pyributicarb, pyrifenox, pyrimethanil, cough up oxazolone, quinoxyfen, pentachloronitrobenzene (PCNB), Silthiopham (silthiopham), simeconazoles (simeconazole), plant bacterium azoles (sipconazole), inferior borous acid sodium (Sodium bibarbonate), clorox, the luxuriant amine of Luo Evil, ((E)-2[2-(2,5-dimethyl phenoxy methyl) phenyl]-2-methoxyimino-N-methylacetamide), streptomysin, sulphur, Tebuconazole, tecloftalam, fluorine ether azoles, Apl-Luster, thiadinil, thiram (TMTD), thifluzamide, thiophanate-methyl, tolelofos-methyl, TPN, triazolone, triadimenol, azoles bacterium piperazine, poplar bacterium amine (triclamide), tricyclazole, tridemorph, fluorine bacterium azoles, oxime bacterium ester (trifloxystrobin), triforine, triticonazole, valida, vinclozolin, alkene frost benzyl azoles, zineb, ziram and oxamides (zoxamide).

Weedicide, the plant hormone medicine, the activeconstituents of plant-growth regulator comprises, for example, dormin, acetochlor, acifluorfen, alachlor, witheredly extremely reach, ametryn, amicarbazone (amicarbazone), sulphur ammonia is yellow grand, amino ethoxy vinyl glycerate, chloroaminopyridine acid (aminopyralid), AC94,377, amiprophosmethl, ancymidol, asulam, atrazine, Ai Wei hormone (aviglycine), tetrazolium is yellow grand, beflubutamid (beflubutamid), benfluralin, benfuresate, dogstail benzyl mixture, bensulide (SAP), bentazon, thiobencarb, isoxaben, benzfendizone (benzfendizone), benzo dicyclo ketone (benzobicyclon), benzofenap, benzyladenine, benzylaminopurine, bilanafos, bifenox, brassinolide, bromacil, bromo-propionic acid, Machete, butafenacil (butafenacil), Glufosinate ammonium, butylate, benzophenone azoles (cafenstrole), calcium carbonate, calcium peroxide, sevin, chlomethoxynil, pyrazon, chlorimuron, Mu Ke, Y 3, chlorsulfuron, chlorthal-dimethyl, chlorothiamid (DCBN), Lipotril, cinidon-ethyl (cinidon-ethyl), cinmethylin, ether is yellow grand, clethodim, clomeprop, cloxyfonac, choline dichloride, 4-CPA (4-chlorinated benzene ethoxyacetic acid), cliprop, the acid of benzene pyridazone, cumyluron (cumyluron, bladex, cyclanilide, ring third is yellow grand, cyhalofop-butyl (cyhalofop-butyl), 2,4-dichlorophenoxyacetic acid salt, 2,4-drip propionic acid (2,4-DP), vanilla is grand, dalapon (DPA), Dimethenamid-P, daminozide, dazomet, nonylcarbinol, dicamba 98-sodium (MDBA), Niagara 5006 (DBN), diflufenican, dikegulac, dimepiperate, penta Kusatsu, P DimethenamidP, diquat, dithiopyr, Diuron Tech, endothal, propionylbrassinolide (epocholeone), esprocarb, ethrel, thiadiazoles is grand, the ethoxy ethyl methyl, the fruit juice element, diphenyl, fenarimol oxazole diclofop-methyl, fentrazamide (fentrazamide), the pyridine ethyl methyl, florasulam (florasulam), fluazifop, fluazolate (fluazolate), flucarbazonesodium (flucarbazone), flufenacet (flufenacet), flufenpyrethyl (flufenpyr), maleic Min Fu oxazinone, tetrapion, the fluorine pyridine is yellow grand, flurprimidol, reach careless fluorine, foramsulfuron (foramsulfuron), forchlorfenuron, prowers (formesafen), Plant hormones regulators,gibberellins, grass ammonium phosphine, glyphosate, the pyrrole chlorsulfuron, six piperazines together, imazamox, AC 263222 (imazapic), Arsenal, Scepter, the pyridine miaow is yellow grand, inabenfide, indolylacetic acid (IAA), indolebutyric acid, methyl-iodide sulphur swells (iodosulfuron), ioxynil-octylate, isouron, chlorine humulone (isoxachlortole) Shuan Ben oxazole acid (isoxadifen), karbutilate, lactofen, lenacil, methoxydiuron, LGC-42153, MALEIC ANHYDRIDE, the adjacent phenyl of using of Z-[(4-chloro-) oxygen] propionic acid (MCPP), 2-methyl-4-chlorinated benzene ethoxyacetic acid salt, the MCPA-thio-ethyl, 2-methyl-4-chloro phenoxybutyhc ethyl ester, mefenacet, fluorine grass sulphur, help strong element, mesosulfuronmethyl (mesosulfuron), Mesotrione (mesotrione), methyldaimuron oxazole acyl grass amine (metamifop), metolachlor, sencorex, metsulfuron-methyl, Hydram, naphthyl acetic acid, the 1-naphthalene acetamide, naproanilide, napropamide, nonylcarbinol, nicoculsfuron, n-phenyl phthalamic acid, orbencarb, oxadiazon Lv oxazinone, oxyquinoline sulfate acid, paclobutrazol, Paraquat, n-nonanoic acid, pendimethalin, penoxsuam (penoxsulam) Wu oxazole grass, pethoxamide, phenmedipham, picloram, fluorine pyrrole acyl grass amine (picolinafen), Piperonyl Butoxide, piperophos, the third careless amine, Fluoropyrimidinesulfuron, the third careless sulphur swells (procarbazone), prodiamine, fluorine metazachlor (profluazol), clefoxidim (profoxydim), the hexamethylene calcium picrolonate, jasmonic propyl ester (prohydrojasmon), prometryn, Stam F-34, the propoxy-p-carbamylaminophenylarsonic acid, pronamide, pyraclonil (pyraclonil), the fluorine carfentrazone, pyrazolate, pyrazosulfuron, pyrazoxyfen, phonetic benzene grass oxime, pyributicarb, pyridafol, reaching grass ends, pyriftalid (pyriftalid), oxime pyridine grass, phonetic sulphur phenylformic acid, quiclorac, quinoclamine, quizalofopPethyl, rimsulfuron, sethoxydim, Tupersan, simazine, simetryn, sodium chlorate, lead ethyl xanthate is yellow grand, swep (MCC), Metribuzin, the quinone oximes grass, terbacil, Azac (MBPMC), thiophene ether grass amine, the match azoles is grand, match diazole element, thiophene methyl, phenoxy propylamine Tianjin, De-Green, triclopyr, tridiphane, trifloxysulfuron (trifloxysulfuron), trifluralin, anti-fall ester, trifloxysulfuron (tritosulfuron), high uniconazole and vernolate (vemolate) are (PPTC).

Insect-killing composition of the present invention also can with synergistic agent such as Piperonyl Butoxide, Safroxan, sulfoxide, N-(2-ethylhexyl)-8,9,10-trinorbornene-5-alkene (trinorborn-5-en)-2,3-dicarboximide (dicarboxyimide) (MGK 264), N-decyl imidazoles, (antiresistant) TBPT of the anti-tolerance of WARF-, TPP, IBP, PSCP, methyl iodide (CH ₃I), uncle-phenyl methylene acetone (butenone), toxilic acid diethyl ester, DMC, FDMC, the mixing such as ETP, ETN, and also can with safener such as benoxacor, cloquintocet, press down evil nitrile, vanilla grand, he presses down evil amine, ethyl fenchlorazole, fenclorim, flurazole, fluxofenim, solution grass furan, pyrroles's two diethyl phthalates, MG191, naphthalic anhydride and oxabetrinil and mix use.

And, compound of the present invention (I) or its salt can use with the arthropodan medicament mixed of control ectoparasitism together, (neotonin sample material if you would May Day five just like the IGR medicine for such medicine, ABG-6215 etc., chitinase inhibitor such as fluorine the third oxygen urea, flufenoxuron, Rimon, HEXAFLUMURON, Teflubenzuron, diflubenzuron, desinsection is grand etc., insect growth regulator(IGR) such as cyromazine, pyriproxyfen etc.), and anabasine (neonicotinoid) compound (nitenpyram etc.), or can with control volume in parasitic medicine (IGR medicine described above, as the medicine that gives animal in the body), medicine (Macrocyclic lactone compounds such as the selamectin of control Filaria, ivermectin, milbemycin, Moxidectin etc.) etc. mix use, and the antimicrobial drug that also is used for animal, vaccine, therapeutical agent, nutritious supplementary and food mix use.

The activated insect example of compound (I) or its tool of its salt pair comprises harmful arthropods such as insect pest, acarid insect etc., and nematode pests.Below list concrete example:

Hemiptera :-

Delphacidae (Delphacidae), for example small brown rice planthopper (Laodelphax striatellus), brown paddy plant hopper (Nilaparvata lugens), white backed planthopper (Sogatella furcifera); Angle top Cicadidae (Deltocephalidae), such as rice green leafhopper (Nephotettix cincticeps) and nephotettix bipunctatus (Nephotettix virescens) etc.; Aphidiadae (Aphididae), such as cotten aphid (Aphisgossypii), black peach aphid (Myzus persicae) etc.; Vegetable aphid (Brevicoryne brassicae), eggplant Macrosiphus spp (Macrosiphum euphorbiae), foxglove is without net Macrosiphus spp (Aulacorthumsolani), oat-cherry knurl volume flies aphid (Rhopalosiphum padi), and tropical citrus aphid (Toxoptera citricidus); The green stinkbug of Pentatomiddae (Pentatomidae) Ru Huajiao (Nezaraantennata), excellent honeybee coried (Riptortus clavetus), rice spot abdomen spider coried (Leptocorisachinensis), wedge angle two star stinkbugs (Eysarcoris parvus) and mixed tea wing stinkbug (Halyomorphamista); Aleyrodidae is such as greenhouse whitefly (Trialeurodes vaporariorum), whitefly in bt cotton (Bemisia tabaci) and Bemisia argentifolii (Bemisia argentifolii); A red-spotted lizard section (Coccidae) is such as red kidney Aspidiotus (Aonidiella aurantii), Sheng Qiongsikang armored scale (Comstockaspisperniciosa), citrus point armored scale (Unaspis citri), red ceroplastes floridensis (Ceroplastes rubens), Australia icerya purchasi (Icerya purchasi); Tingidae (Tingidae); Psyllidae (Psyllidae) etc.

Lepidopteran (Lepidoptera):

Pyralidae (Pyralidae), such as striped rice borer (Chilo suppressalis), cnaphalocrocis medinalls guenee (Cnaphalocrocis medinalis), the wild snout moth's larva (Notarcha derogata) of lap leaf, India paddy phycitid (Plodia interpunctella) etc., east Pyrausta nubilalis (Hubern). (Ostrinia furnacalis), Caulis et Folium Brassicae capitatae web spinner (Hellula undalis), and precocious dogstail set (Pediasia teterrellus); Noctuidae (Noctuidae), for example prodenia litura (Spodoptera litura), beet armyworm (Spodoptera exigua), mythimna separata (Pseudaletia separata), lopper worm (Mamestrabrassicae), black cutworm (Agrotis ipsilon), sweet cabbage caterpillar (semi-looper) (Plusianigrisigna), Thoricoplusia spp., real noctuid (Heliothis spp.), noctuid (Helicoverpaspp.); Sulfur butterfly (Pieridae), for example small white (Pieris rapae); Tortricidae (Tortricidae) is for example rolled up moth (Adoxophyes spp.), oriental fruit months (Grapholita molesta), large flat heart-eating worm (Leguminivora glycinivorella), azuki eating-core bean worm (Matsumuraesesazukivora), fruit leaf roller in summer (Adoxophyes orana fasciata), volume moth (Adoxophyes sp.), oriental tea leaf roller (Homona magnanima), apple skin worm (Archips fuscocupreanus), Pericarpium Mali pumilae steinernema (Cydia pomonella); The thin moth of leaf mining (Gracillariidae) is such as the thin moth of tea (Caloptilia theivora), and narrow wing lyonetid (Phyllonorycter ringoneella); Carposinidae (Carposinidae), for example peach fruit moth (Carposina niponensis); Lyonetid section (Lyonetiidae), for example lyonetid (Lyonetia spp.); Lymantriidae (Lymantriidae), for example poison moth (Lymantria spp.) and pornography and drug moth (Euproctisspp.); Yponomeutidae (Yponomeutidae), for example small cabbage moth (Plutella xylostella); Gelechidae (Gelechiidae), for example Pectinophora gossypiella (Pectinophora gossypiella) and phthorimaea operculella (Phthorimaea operculella); Tiger moth and; Arctiidae (Arctiidae), for example fall webworms (Hyphahtria cunea); Rain moth section (Tineidae) is for example according to moth (Tinea translucens), curtain rain moth (Tineola bisselliella);

Thysanoptera (Thysanoptera):

Thripidae (Thripidae) is such as Frankliniella occidentalis (Frankliniella occidentalis), palm thrips (Thrips parmi), onion thrips (Thrips tabaci), onion thrips (Thrips tabaci), flower thrips (Frankliniella intonsa) etc.

Diptera (Diptera):

Housefly (Musca domestica), common culex (Culex popiens pallens), horse botfly (Tabanus trigonus), onion fly (Hylemya antiqua), Chrysomyia megacephala (Fabricius) (Hylemya platura), Anopheles sinensis (Anopheles sinensis), the rice fly (Agromyza oryzae) of diving, the rice fly (Hydrellia griseola) of diving, ricestem-fly (chlorops oryzae), melon trypetid (Dacuscucurbitae), Mediterranean Sea fruit fly (Ceratitis capitata), African chrysanthemum liriomyza bryoniae (Liriomyzatrifolii) etc.

Coleoptera (Coleoptera):

Potato ladybug (Epilachna vigintioctopunctata), aulacophora femoralis (Aulacophorafemoralis), Phyllotreta striolata (Phyllotreta striolata), rice leaf beetles (Oulemaoryzae), Lissorhoptrus oryzophilus Kuschel (Echinocnemus squameus), rice water resembles (Lissorhoptrusoryzophilus), cotton sandfly weevil worm (Anthonomus grandis), red bean resembles (Callosobruchuschinensis), Sphenophorus venatus, Japanese beetle (Popillia japonica), large green rutelian (Anomala cuprea), corn rootworm (Diabrotica spp.), Colorado beetle (Leptinotarsa decemlineata), click beetle (Agriotes spp.), cigarette beetle (Lasioderma serricorne), little garden khapra beetle (Anthrenus verbasci), red flour beetle (Tribolium castaneum), lyctus (Lyctus brunneus), spot longicorn beetle (Anoplophora malasiaca), pine bark beetle (Tomicus piniperda) etc.

Orthoptera (Orthoptera):

East Asia moth (Locusta migratoria), African mole cricket (Gryllotalpa africana), etc. divergent sugarcane locust (Oxya yezoensis), etc. divergent sugarcane locust (Oxya japonica) etc.

Hymenoptera (Hymenoptera):

Cabbage sawfly (Athalia rosae), leaf cutting ant (Acromyrmex spp.), fiery ant (Solenopsisspp.) etc.

Threadworms :-

The white sharp pathogenic nematode of paddy rice (Aphelenchoides besseyi), strawberry leaf bud nematode (strawberry bud nematode (Nothotylenchus acris) etc.

Dictyoptera :-

Groton bug (Blattella germanica)), Peroplaneta fluligginosa (Periplaneta fuliginosa), periplaneta americana (Periplaneta americana), the large Lian of foxiness (Periplaneta brunnea), oriental cockroach (Blatta orientalis) etc.

Acarina (Acarina):

Tetranychidae (Tetranychidae), for example Tetranychus urticae (Tetranychus urticae); Eriophyidae (Eriophyidae), for example tangerine peronium goitre mite (Aculops pelekassi); Tarsonemidae (Tarsonemidae), for example Polyphagotarsonemus latus Banks (Polyphagotarsonemus latus); Tenuipalpidae (Tenuipalpidae); Du Ke Tetranychidae (Tuckerellidae); Hard tick section (Iodidae), for example haemaphysalis longicornis (Haemaphysalis longicornis), haemaphysalis flava (Haemaphysalisflava), Taiwan epidermis tick (Dermacentor taiwanicus), ixodes ovatus (Ixodes ovatus), ixodes persulcatus (Ixodes persulcatus), boophilus microplus (Boophilus microplus) and brown dog tick (Rhipicephalus sanguineus); Tyroglyphidae (Acaridae), for example tyrophagus putrescentiae (Tyrophagus putrescentiae); House dust mite (Pyroglyphidae) is such as dust mite (Dermatophagoides farinae) and Dermatophagoides (Dermatophagoidesptrenyssnus); Cheyletidae (Cheyletidae), for example Cheyletus eruditus (Cheyletuseruditus), Malacca cheyletid mite (Cheyletus malaccensis) and Cheyletus (Cheyletusmoorei); Dermanyssidae (Dermanyssidae) is such as Dermanyssus gallinae (Dermahyssus gallinae) etc.

In addition, the preparation that contains compound (I) or its salt can be used for treating in the field of disease of livestock and livestock industry domestic animal, and also be used for parasitizing in vertebrates (such as people, ox, horse, sheep, goat, pig, poultry, dog, cat, the fish etc.) body and/or external arthropods and parasite kept public health by elimination.The example of insect comprises, for example, true tick (Ixodes spp.), boophilus microplus (such as Boophilus microplus), flower tick (Amblyomma spp.), glass eye tick (Hyalomma spp.), fan head tick (such as Rhipicephalus appendiculatus), brown dog tick (Haemaphysalis spp.), leather tick (dermacentor spp.), Africa pure garden tick (such as Ornithodoros moubata), cock skin thorn tick (Dermahyssus gallinae), fowl thorn mite (Ornithonyssus sylviarum), itch mite (such as itch mite (Sarcoptes scabiei)), itch mite (Psoroptes spp.), skin mite (Chorioptes spp.), demodicid mite (Demodex spp.), Eutrombicula spp., yellow-fever mosquito (such as text of an annotated book yellow-fever mosquito (Aedes albopictus)), anopheles (Anopheles spp.), culex (Culex spp), kitchen fly (Culicodes spp), fly (Muscaspp.), torsalo (Hypoderma spp.), stomach fly (Gasterophilus spp.), lick blood fly (Haematobia spp), horsefly (Tabanus spp), buffalo gnat (Simulium spp.), cone nose worm (Triatoma spp.), the hair Anoplura (as is bitten lice (Damalinia spp.), sour jujube lice (Linognathusspp.), sucking louse (Haematopinus spp)), a furuncle flea (Ctenocephalides spp.), visitor flea (Xenosylla spp), (monomorium pharaonis_ and threadworms are (for example for MonomoriumMayr, trichostrongylus is (such as ancylostoma braziliense (Nippostrongylus brasiliensis), trichostrongylus axei, trichostrongylus colubriformis), Trichinella (such as Trichinella spiralis (Trichinella spiralis)), haemonchus contortus (Haemonchus contortus), Turbatrix (such as ancylostoma duodenale (Nematodirus battus)), ox digitellium worm (Ostertagia circumcincta), ancient cypressCypressus filaria (Cooperia spp.), Diplacanthus nanus, dwarf tapeworm) etc.

For the method for Control pests of the present invention, compound (I) or its salt can be used as it is.But compound (I) or its salt are configured to above-mentioned insect-killing composition of the present invention usually, and for example, it is applied to insect lives and to be applied to the habitat of insect in the mode that is similar to conventional insect-killing composition, then make activeconstituents contact work with insect with the described insect of its feeding.

The example of insect of the present invention habitat comprises rice field, wild country, orchard, unreclamined field, household etc.

As the method for using, for example can mention that spraying processing, soil treatment, seed treatment and water culture are processed.

It is by processing plant surface or insect itself with activeconstituents (compound (I) or its salt), particularly for example, being applied to leaf, to the treatment process of the expression control effects such as trunk spraying that spraying of the present invention is processed.The treatment process that soil treatment protection farm crop avoid insect to damage; it is by processing soil with activeconstituents; irrigate solution etc.; so that from infiltrations such as roots be delivered to the inside plants of farm crop; with the infringement of avoiding insect as nibbling etc.; and particularly; for example; the processing of the implant hole (spraying of implant hole; soil fusion after implant hole is processed); plant root is processed (plant root spraying; the soil fusion of plant root; the plant root pouring; the plant root of second half section in sowing time is processed); the processing of plantation ditch dug with a plow (plantation ditch dug with a plow spraying; the soil fusion of plantation ditch dug with a plow); plantation row row's processing (plantation row row spraying; the fusion of plantation row casting earth; the plantation row row spraying of planting season); the plantation row row in sowing time processes (the plantation row row spraying in sowing time; the plantation row casting earth fusion in sowing time); overall process (total spray body; overall soil fusion); (the granular spraying in the blade face in vegetative period is processed in other spraying; spraying around trunk or the stem; the soil surface spraying; the soil surface fusion; the spraying of sowing hole; the field spraying; the plant internal spraying); (irrigation soils are processed in other irrigation; irrigate in sowing time; the injection treatment of insecticidal solution; the irrigating plant root; the drip irrigation insecticidal solution; chemigation (chemigation)); the nursery case is processed (nursery case spraying; nursery case pouring); the artificial incubation pallet is processed (artificial incubation pallet spraying; the pouring of artificial incubation pallet); (nursery spraying is processed in the nursery; the nursery pouring; the nursery spraying in rice field; the dipping of nursery plant); (nursery soil fusion is processed in the nursery soil fusion; nursery soil fusion before the sowing), other processing (growth medium fusion; turn over; the surface soil fusion; soil mixes in the raindrop; the plantation point is processed; the granular spraying of flowers; pasty state fertilizer mixes) etc. can be used as example.Seed treatment represents to control the treatment process of effect for the antagonism insect, the seed of the method by processing farm crop with activeconstituents, seed tubers, napiform root etc. or infringement of avoiding insect to cause around it are carried out as directly nibbling, and particularly, for example, processing, dip treating, immersion treatment are processed, are coated with in air blast, wiping is deposited processes, and film coating and particle coating are processed and be can be used as example.Water culture is treated to the treatment process that the protection farm crop avoid the insect infringement; it is undertaken by solution that process to cultivate with activeconstituents etc.; so that from infiltrations such as roots be delivered to the inside plants of farm crop; with the infringement of avoiding insect as nibbling etc.; and particularly; for example, the mixing of the solution of the solution blending of cultivation, cultivation can be used as example.

The amount that compound (I) or its salt are used in the method for Control pests of the present invention can be according to the time of using, use place, application process etc. changes, but in general, with the about 0.3-3000g of per hectare, preferably the amount of the activeconstituents of about 50-3000g (compound (I) or its salt) is used.In addition, when insect-killing composition of the present invention is wettable powder etc., use behind its dilutable water, so that the ultimate density of activeconstituents reaches about 0.1-1000ppm, the preferred scope of about 10-500ppm

As alternative approach, for example, by insect-killing composition of the present invention being given (inside of health) or external (surface) in the above-mentioned vertebrate body, can integral body or non-integral ground eliminate arthropods and the parasite that lives in the described vertebrates.The method that gives in the body comprises oral processing; Anus is processed; Inter-planting; Process with subcutaneous injection, intramuscularly processing or intravenous injection are processed.In addition, the sanitary insect pest that is produced by animal excrements can be eliminated to the livestock animals medicine by feeding.

When insect-killing composition of the present invention is applied to the animal of insect parasitism such as domestic animal and pet, the amount of using is enclosed interior variation according to application process wide in range, but in general, the amount of the activeconstituents of preferred every 1kg the weight of animals (compound (I) or its salt) is about 0.1mg-2000mg, more preferably about 0.5mg-1000mg.

The present invention will further be obtained explanation by following synthetic example, reference example, example of formulations and test example; Yet the present invention is not limited to these embodiment.

Carry out for embodiment with reference to being eluted under the monitoring of TLC (thin-layer chromatography) of column chromatography of Preparation Example.Under the TLC monitoring, by Merck﹠amp; Co., the kieselgel 60F of Inc. production ₂₅₄(70-230 order) is used as the TLC flat board; The solvent that is used as eluting solvent at column chromatography is used as developing solvent; Be used to detect with the UV detector.By Merck﹠amp; Co., the Kieselgel 60 (70-230 order) of Inc. production is used as the silica gel for column chromatography.When compacting is for the type high performance liquid chromatography in the conduct, use by Yamazen Co., Ltd. (filter: the Ultrapack that silica gel) produces.When mixed solvent is used as developing solvent, the ratio of mixture of the numeric representation solvent volume in the bracket.The NMR spectrum is proton N MR, and with JEOL AL-400 (400MHz) spectrograph and AVANCE 400 (400MHz) spectrophotometer, uses tetramethylsilane as interior mark.All δ values represent with ppm.The temperature of measuring is 25 ℃, and unless otherwise indicated, and the temperature of measuring represents the temperature that leaves standstill.

In addition, be used for following examples and have following meaning with reference to the abbreviation of Preparation Example:

S: unimodal, br: broad peak, brs: wide unimodal, d: bimodal, t: triplet, q: quartet, quint: quintet, sext: sextet, sept: septet, Me: methyl, Et: ethyl, Ph: phenyl, Pr-n (or n-Pr): n-propyl, Pr-i (or i-Pr or ⁱPr): sec.-propyl, the Pr-ring (or ring-Pr): cyclopropyl, Bu-n (or n-Bu): normal-butyl, Bu-i (or i-Bu): isobutyl-, Bu-s (or s-Bu): sec-butyl, Bu-t (or t-Bu): the tertiary butyl, DMF: dimethyl formamide, m-CPBA: a chloro peroxybenzoic acid.In addition, room temperature refers to about 15-25 ℃.

Embodiment 1

Compound (1): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

N-phenyl-3-phenyl sulfo-acrylimide (thioacrylamide) (0.75g) is suspended in the toluene (10ml), then under room temperature, to wherein adding thionyl chloride (0.40ml), 1 DMF and triethylamine (0.80ml).In 60 ℃ of oil baths, stirred this mixture 3 hours.Then make it cooling and filtering insoluble substance.Concentrating under reduced pressure filtrate.Make residue be dissolved in DMF (15ml).Ice-cooled lower, to wherein add sodium hydride (55% in oil: 0.217g), then with being added dropwise to thiophene (0.40ml) in 3 minutes.It was stirred 2.5 hours.Saturated sodium-chloride water solution (10ml) and water (5ml) are joined in the reaction mixture, and extract (15ml) 3 times with t-butyl methyl ether.Merge organic layer, and with saturated sodium-chloride water solution (15ml) washing 3 times, dry through anhydrous sodium chlorate, filtering organic salt, concentrating under reduced pressure obtains black oil (1.0g).Make it through silica gel column chromatography (hexane: ethyl acetate=15: 1), obtain phenyl N-phenyl-3-(thiophenyl) sulfo-acryloyl imido-ester (thioacrylimidate) (0.41g), be faint yellow oily thing.

¹H-NMR (CDCl ₃) δ (ppm): 5.68 (d J=15.1Hz), 5.81 (d J=10.3Hz), the total 1H of 6.08 (d J=15.1Hz), 6.66-7.58 (16H, m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (2)-(34) are synthetic in the mode that is similar to embodiment 1.

Embodiment 2

Compound (2): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-chlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.46-5.84(1H，m)，6.67-7.52(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 3

Compound (3): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 3-chlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.55-5.87(1H，m)，6.67-7.63(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 4

Compound (4): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2-chlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.62-5.87(1H，m)，6.83-7.59(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 5

Compound (5): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.31(2H，s)，6.08(1H，d J＝15.6Hz)，6.74(2H，d J＝7.3Hz)，7.05(1H，t J＝7.4Hz)，7.22-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 6

Compound (6): N-phenyl-3-(benzylthio-) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.82(2H，s)，4.30(2H，s)，6.07(1H，dJ＝15.6Hz)，6.73(2H，d J＝7.6Hz)，7.07(1H，t J＝7.4Hz)，7.14-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 7

Compound (7): N-phenyl-3-(cyclohexyl sulfenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-2.00(10H，m)，2.66-2.92(1H，m)，5.71(0.33H，d J＝12.0Hz)，5.77(0.66H，d J＝15.1Hz)，6.92-7.51(11H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 8

Compound (8): N-phenyl-3-(benzylthio-) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.75(1H，m)，3.86(1H，m)，5.70(0.5H，d，J＝12.0Hz)，5.79(0.5H，d，J＝16.0Hz)，6.62-7.52(16H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 9

Compound (9): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.81(1H，d J＝10.1Hz)，6.84(1H，dJ＝10.1Hz)，7.08-7.52(15H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 10

Compound (10): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-pyridyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.87(0.7H，d J＝15.0Hz)，6.09(0.3H，dJ＝15.2Hz)，6.73(0.6H，d J＝7.7Hz)，6.84(1.4H，d J＝7.7Hz)，7.08-7.66(11H，m)，8.43(1.4H，d J＝5.8Hz)，8.54(0.6H，d J＝4.8H)。

The stereochemistry of-CH=CH-key is E.

Embodiment 11

Compound (11): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 3,4-dichlorophenyl ester

m.p.：99.5-100.5℃

¹H-NMR(CDCl ₃)δ(ppm)：5.38(0.8H，d J＝14.7Hz)，6.06(0.2H，dJ＝15.5Hz)，6.67(0.4H，d J＝7.6Hz)，6.87(1.6H，d J＝7.6Hz)，6.99-7.64(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 12

Compound (12): N-(2-p-methoxy-phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.90(3H，s)，5.86(1H，d J＝10.2Hz)，6.86(1H，d J＝10.2Hz)，6.95-7.03(4H，m)，7.09-7.16(1H，m)，7.22-7.38(4H，m)，7.40-7.52(5H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 13

Compound (13): N-phenyl-3-(4-chloro benzylthio-) sulfo-acryloyl imido acid 4-chloro benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.78(2H，s)，4.24(2H，s)，6.00(1H，dJ＝16.0Hz)，6.67(2H，dJ＝7.7Hz)，7.00-7.75(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 14

Compound (14): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.50-5.70(0.7H，m)，5.80-5.90(0.3H，m)，6.81-7.87(18H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 15

Compound (15): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 3,4-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.37(0.1H，dJ＝14.6Hz)，5.81(0.9H，dJ＝10.2Hz)，6.86-7.59(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 16

Compound (16): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 3,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.46(0.7H，d J＝14.6Hz)，6.06(0.3H，dJ＝15.4Hz)，6.68-7.66(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 17

Compound (17): N-(4-chlorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.66(1H，d J＝14.85Hz)，6.84(2H，dJ＝8.45Hz)，7.24-7.38(12H，m)，7.56(1H，dJ＝14.85Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 18

Compound (18): N-(4-chlorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.80(1H，d J＝10.14Hz)，6.86(1H，dJ＝10.14Hz)，6.99-7.05(2H，m)，7.22-7.53(12H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 19

Compound (19): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2,4 dichloro benzene base ester

¹H-NMR(CDCl ₃)δ(ppm)：5.44(0.5H，d J＝14.2Hz)，5.74(0.3H，dJ＝10.1Hz)，6.05(0.2H，d J＝15.9Hz)，6.66-7.63(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 20

Compound (20): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.60(0.7H，d J＝14.7Hz)，5.79(0.1H，dJ＝10.4Hz)，6.05(0.2H，d J＝15.0Hz)，6.68-7.65(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 21

Compound (21): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-bromo phenylester

m.p.：93-95℃

¹H-NMR(CDCl ₃)δ(ppm)：5.49(0.83H，d J＝14.4Hz)，6.06(0.17H，dJ＝16.1Hz)，6.65-7.59(15H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 22

Compound (22): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-bromo phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.49(0.1H，d J＝14.7Hz)，5.79(0.9H，dJ＝9.9Hz)，6.87-7.59(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 23

Compound (23): N-(3-chlorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.65(0.63H，d J＝14.73Hz)，5.80(0.29H，d J＝10.63Hz)，6.00(0.08H，d J＝14.97Hz)，6.73-7.17(3H，m)，7.17-7.63(11.92H，m)，7.78(0.08H，d J＝14.97Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 24

Compound (24): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.68(1H，d J＝14.5Hz)，6.88-6.94(2H，m)，7.05-7.40(13H，m)，7.55(1H，d J＝14.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 25

Compound (25): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-trifluoromethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.58(0.42H，d J＝14.7Hz)，5.79(0.42H，dJ＝9.9Hz)，6.08(0.16H，d J＝15.5Hz)，6.67-7.64(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 26

Compound (26): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-p-methoxy-phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.85(3H，s)，5.59(0.83H，d J＝14.6Hz)，6.06(0.17H，d J＝15.6Hz)，6.64-7.56(15H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 27

Compound (27): N-phenyl-3-(4-anisole sulfenyl) sulfo-acryloyl imido acid 4-p-methoxy-phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.83(3H，s)，3.84(3H，s)，5.40(0.83H，d J＝14.2Hz)，5.85(0.17H，d J＝15.5Hz)，6.60-7.52(14H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 28

Compound (28): N-(4-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.37(3H，s)，5.80(1H，d J＝9.9Hz)，6.82(1H，d J＝9.9Hz)，7.00(2H，d J＝8.2Hz)，7.18-7.53(12H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 29

Compound (29): N-(4-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.37(3H，s)，5.68(0.36H，d J＝14.7Hz)，6.01(0.64H，d J＝14.6Hz)，6.83(2H，d J＝8.2Hz)，7.12-7.55(12.36H，m)，7.85(0.64H，d J＝14.6Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 30

Compound (30): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-Trifluoromethoxyphen-l ester

¹H-NMR(CDCl ₃)δ(ppm)：5.58(0.5H，d J＝14.7Hz)，5.79(0.5H，dJ＝10.1Hz)，6.88-7.54(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 31

Compound (31): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 1-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.31(0.38H，d J＝14.6Hz)，5.56(0.38H，dJ＝10.2Hz)，5.68(0.24H，d J＝14.9Hz)，6.61-8.34(18H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 32

Compound (32): N-(3-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.40(3H，s)，5.81(1H，d J＝9.9Hz)，6.83(1H，d J＝9.9Hz)，6.86-6.92(2H，m)，6.94-7.00(1H，m)，7.20-7.55(11H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 33

Compound (33): N-(3-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.35(2.5H，s)，2.40(0.5H，s)，5.68(0.84H，d J＝14.5Hz)，5.81(0.16H，d J＝9.9Hz)，6.69-6.75(3H，m)，6.83(0.16H，d J＝9.9Hz)，6.89-6.94(2H，m)，7.18-7.57(9.84H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 34

Compound (34): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2,3-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.54(0.5H，d J＝14.6Hz)，5.77(0.38H，dJ＝10.2Hz)，6.05(0.12H，d J＝15.4Hz)，6.67-7.62(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 35

Compound (35): N-phenyl-3-(phenoxy group) sulfo-acryloyl imido acid phenylester

N-phenyl-3-phenoxy group acrylamide (1.5g) is suspended in the toluene (80ml), then under room temperature, to wherein adding thionyl chloride (0.82ml), triethylamine (1.8ml) and 1 DMF.In 60 ℃ of oil baths, stirred this mixture 3 hours.Then make it cooling and filtering insoluble substance.Concentrating under reduced pressure filtrate.Make residue be dissolved in DMF (80ml).Ice-cooled lower, to the sodium salt that wherein adds thiophenol (0.82g), and stirred 2 hours.T-butyl methyl ether (250ml) is joined in the reaction mixture.It is used the 1N aqueous sodium hydroxide solution, and water and saturated sodium-chloride water solution sequentially wash, and be dry through anhydrous sodium chlorate, filtering organic salt, concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=20: 1), obtain N-phenyl-3-(phenoxy group) sulfo-acryloyl imido acid phenylester (0.28g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：5.64(0.7H，d，J＝12.0Hz)，5.98(0.3H，d，J＝12.0Hz)，6.75(0.6H，d，J＝7.6Hz)，6.91-7.44(13.8H，m)，7.59(0.6H，d，J＝6.6Hz)，7.68(1H，d，J＝12.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 36

Compound (36): N-phenyl sulfonyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

N-phenyl sulfonyl-3-phenyl sulfo-acrylimide (0.50g) is suspended in the toluene (10ml), then under room temperature, to wherein adding thionyl chloride (0.20ml), triethylamine (0.40ml) and 1 DMF.In 60 ℃ of oil baths, stirred this mixture 3 hours.Then make it cooling, the filtering insoluble substance.Concentrating under reduced pressure filtrate.Make residue be dissolved in DMF (8ml).Ice-cooled lower, to the DMF that wherein adds thiophenol sodium salt (0.30g) (2ml) solution, and it was stirred under room temperature 1.5 hours.Ethyl acetate (80ml) is joined in the reaction mixture, it is sequentially washed with 1N aqueous sodium hydroxide solution, water and saturated sodium-chloride water solution, dry through anhydrous sodium chlorate, filtering organic salt, concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain N-phenyl sulfonyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester (0.14g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：6.01(0.67H，d J＝14.7Hz)，6.35(0.33H，dJ＝9.9Hz)，7.20(0.33H，d J＝9.9Hz)，7.31-7.51(15H，m)，7.85(0.67H，d J＝14.7Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 37

Compound (37): N-phenyl-3-(thiophenyl) acryloyl imido acid phenylester

N-phenyl-3-phenyl sulfo-acrylimide (0.766g) is suspended in the toluene (15ml), then under room temperature, to wherein adding thionyl chloride (0.33ml) and triethylamine (0.62ml).In 60 ℃ of oil baths, stirred this mixture 3 hours.Then it is removed by filter insoluble thing.Concentrating under reduced pressure filtrate.Make residue be dissolved in DMF (15ml).Ice-cooled lower, (55% in oil: 0.226g), then add phenol (0.303g) to wherein adding sodium hydride.It ice-cooled lower stirring 2.5 hours, and is stirred under room temperature and spend the night.Saturated sodium-chloride water solution (15ml) and water (5ml) are joined in the reaction mixture, extract twice with ethyl acetate (20ml) and t-butyl methyl ether (15ml).Merge organic layer, and with saturated sodium-chloride water solution (15ml) washing 3 times, dry through anhydrous sodium chlorate, filtering organic salt, concentrating under reduced pressure obtains black oil (0.88g).Make it through silica gel column chromatography (hexane: ethyl acetate=15: 1), obtain phenyl N-phenyl-3-(thiophenyl) acryloyl imido-ester (acrylimidate) (0.2g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：5.65-5.90(1H，m)，6.72-7.72(16H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (38)-(98) are synthetic in the mode that is similar to embodiment 37.

Embodiment 38

Compound (38): 3-(phenoxy group)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.74(1H，d，J＝12.4Hz)，6.78-6.81(2H，m)，7.00-7.44(13H，m)，7.80(1H，d，J＝12.4Hz)

The stereochemistry of-CH=CH-key is E.

Embodiment 39

Compound (39): N-(2-chlorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.69(0.83H，d J＝15.2Hz)，5.81(0.17H，dJ＝15.0Hz)，6.73(0.83H，d J＝7.7Hz)，6.88-7.00(0.83H，m)，7.05-7.55(12.34H，m)，7.74(0.83H，d J＝15.2Hz)，8.00(0.17H，d J＝15.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 40

Compound (40): N-(3-chlorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.75(0.83H，d J＝15.0Hz)，5.81(0.17H，dJ＝15.0Hz)，6.56-6.63(0.83H，m)，6.71-6.77(0.83H，m)，6.92-7.54(12.34H，m)，7.74(0.83H，d J＝15.0Hz)，8.00(0.17H，d J＝15.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 41

Compound (41): N-(4-chlorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.76(1H，d J＝15.1Hz)，6.64(2H，dJ＝8.5Hz)，7.05-7.56(12H，m)，7.72(1H，d J＝15.1Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 42

Compound (42): N-(2-p-methoxy-phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.75(3H，s)，5.82(1H，d J＝15.1Hz)，6.69(1H，d J＝6.5Hz)，6.78-7.03(5H，m)，7.21-7.50(8H，m)，7.66(1H，d J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 43

Compound (43): N-(4-chlorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

m.p.：98-100℃

¹H-NMR(CDCl ₃)δ(ppm)：5.70(1H，d，J＝12.0Hz)，6.72-6.74(2H，m)，7.05-7.41(12H，m)，7.83(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 44

Compound (44): N-(3-p-methoxy-phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.75(3H，s)，5.91(1H，d J＝15.0Hz)，6.27-6.35(2H，m)，6.53-6.60(1H，m)，6.82(2H，d J＝7.5Hz)，6.92(1H，d J＝7.5Hz)，7.07-7.52(8H，m)，7.70(1H，d J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 45

Compound (45): N-(3-chlorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.71(1H，d，J＝12.0Hz)，6.68(1H，d，J＝8.0Hz)，6.81(1H，s)，6.99-7.41(12H，m)，7.83(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 46

Compound (46): N-(4-p-methoxy-phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.77(3H，s)，5.94(1H，d J＝15.1Hz)，6.67(2H，d J＝8.7Hz)，6.74-6.86(6H，m)，6.92(2H，t J＝7.5Hz)，7.17-7.54(4H，m)，7.68(1H，d J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 47

Compound (47): N-(4-pyridyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.81(0.83H，d J＝15.2Hz)，6.13(0.17H，dJ＝9.9Hz)，7.08(1H，d J＝8.5Hz)，7.32-7.57(12.17H，m)，8.00(0.83H，d J＝15.2Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 48

Compound (48): N-(2-difluorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.78 (d, J=15.5Hz), the total 1H of 5.81 (d, J=15.5Hz), 6.72-6.80 (0.67H, m), 6.91-7.58 (13.33H, m), 7.75 (0.67H, d, J=15.0Hz), 8.00 (0.33H, d, J=15.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 49

Compound (49): N-(3-pyridyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.72 (d J=15.2Hz), the total 1H of 5.82 (d J=10.9Hz), 7.08-7.53 (12.3H, m), 7.79 (0.7H, d J=15.2Hz), 8.03-8.08 (1H, m), 8.22-8.31 (1H, m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 50

Compound (50): N-(4-difluorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.80 (d, J=15.5Hz), 5.81 (d, J=15.5Hz) total 1H, 6.63-6.68 (2H, m), (6.86-6.93 2H, m), 7.18-7.56 (10H, m), (7.71 0.8H, d, J=15.5Hz) 8.00 (0.2H, d, J=15.5Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 51

Compound (51): N-(3-difluorophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.78 (d, J=15.2Hz), 5.81 (d, J=14.7Hz) total 1H, 6.40-6.53 (2H, m), (6.65-6.73 1H, m), 7.05-7.55 (11H, m), (7.73 0.7H, d, J=15.2Hz) 8.00 (0.3H, d, J=14.7Hz).

The stereochemistry of-CH=CH-key is E.

Embodiment 52

Compound (52): N-(4-trifluoromethyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.60(0.77H，d，J＝15.0Hz)，5.75(0.15H，d，J＝10.6Hz)，5.81(0.04H，d，J＝14.7Hz)，5.82(0.04H，d，J＝10.4Hz)，6.73-6.82(2H，m)，7.13-7.62(12.19H，m)，7.75(0.77H，d，J＝15.0Hz)8.00(0.04H，d，J＝15.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 53

Compound (53): N-(4-bromo phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.74 (d, J=14.5Hz), the total 0.95H of 5.81 (d, J=15.2Hz), (6.13 0.05H, d, J=10.1Hz), 6.59 (1H, d, J=8.5Hz), 7.06-7.11 (0.57H, m), 7.14-7.56 (12.48H, m), (7.72 0.63H, d, J=15.2Hz), (8.00 0.32H, d, J=14.5Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 54

Compound (54): N-(4-aminomethyl phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.29(3H，s)，5.81(0.17H，dJ＝15.2Hz)，5.94(0.83H，d J＝15.2Hz)，6.63(2H，d J＝8.2Hz)，6.98-7.57(12H，m)，7.67(0.83H，d J＝15.2Hz)，8.00(0.17H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 55

Compound (55): N-(4-nitrophenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR (CDCl ₃) δ (ppm): 5.57 (0.77H, d J=15.2Hz), 5.67 (dJ=15.2Hz), (5.72 d J=10.3Hz) total 0.23H, 6.79 (2H, d J=8.7Hz), 7.13-7.54 (10.23H, m), 7.81 (0.77H, d J=15.2Hz), 8.03-8.12 (1.54H, m), 8.12-8.21 (0.46H, m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 56

Compound (56): N-(4-aminomethyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

m.p.：73-74℃

¹H-NMR(CDCl ₃)δ(ppm)：2.29(3H，s)，5.78(1H，d J＝12.1Hz)，6.70(2H，d J＝7.7Hz)，7.05-7.07(4H，m)，7.12-7.25(4H，m)，7.33-7.40(4H，m)，7.79(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 57

Compound (57): N-(4-p-methoxy-phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.77(3H，s)，5.80(1H，d J＝12.1Hz)，6.72-6.97(4H，m)，7.05-7.07(2H，m)，7.12-7.24(4H，m)，7.33-7.39(4H，m)，7.80(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 58

Compound (58): N-(2-chlorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.59(1H，d J＝12.0Hz)，6.81(1H，dJ＝7.5Hz)，6.93-6.97(1H，m)，7.06-7.07(2H，m)，7.13-7.21(3H，m)，7.30-7.42(7H，m)，7.84(1H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 59

Compound (59): N-(3,4-dichlorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.67(1H，d J＝11.8Hz)，6.64(1H，dd J＝8.5，2.4Hz)，6.91(1H，d J＝2.4Hz)，7.07(2H，d J＝8.0Hz)，7.15-7.41(9H，m)，7.85(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 60

Compound (60): N-phenyl-3-(thiophenyl) acryloyl imido acid benzyl ester

m.p.：77-81℃

¹H-NMR(CDCl ₃)δ(ppm)：5.29(1.67H，s)，5.43(0.33H，s)，5.75(0.16H，d J＝10.9Hz)，5.81(0.84H，d J＝15.2Hz)，6.75-7.62(16H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 61

Compound (61): N-phenyl-3-(thiophenyl) acryloyl imido acid 3-methyl-benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.37(2.25H，s)，2.39(0.75H，s)，5.25(1.5H，s)，5.39(0.5H，s)，5.75(0.25H，d J＝10.9Hz)，5.80(0.75H，d J＝15.2Hz)，6.75-7.47(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 62

Compound (62): N-(4-cyano-phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.58(0.91H，d J＝14.9Hz)，5.71(0.09H，dJ＝10.9Hz)，6.72-6.96(3H，m)，7.10-7.61(11.09H，m)，7.79(0.91H，d J＝14.9Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 63

Compound (63): N-(4-ethylphenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(3H，t J＝7.5Hz)，2.58(2H，q J＝7.5Hz)，5.81(0.21H，d J＝15.0Hz)，5.93(0.79H，d J＝15.4Hz)，6.65(2H，dJ＝8.0Hz)，7.01-7.57(12H，m)，7.67(0.79H，d J＝15.4Hz)，8.00(0.21H，d J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 64

Compound (64): N-(3,5-dichlorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.66(1H，d J＝12.0Hz)，6.71(2H，s)，7.02-7.25(6H，m)，7.36-7.39(5H，m)，7.86(1H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 65

Compound (65): N-(3,4,5-trichloro-benzene base)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.65(1H，d J＝11.8Hz)，6.85(2H，s)，7.08-7.10(2H，m)，7.16-7.23(4H，m)，7.36-7.42(4H，m)，7.87(1H，d J＝11.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 66

Compound (66): N-phenyl-3-(phenoxy group) acryloyl imido acid 3-pyridyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.88(1H，d J＝15.0Hz)，6.69-6.75(2H，m)，6.98-7.05(1H，m)，7.18-7.61(9H，m)，7.72(1H，d J＝15.0Hz)，8.40-8.55(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 67

Compound (67): N-phenyl-3-(thiophenyl) acryloyl imido acid 4-chloro benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.25(1.6H，s)，5.38(0.4H，s)，5.74(0.2H，d J＝11.1Hz)，5.79(0.8H，d J＝15.2Hz)，6.72-7.55(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 68

Compound (68): N-phenyl-3-(thiophenyl) acryloyl imido acid 2-chloro-pyridine-5-ylmethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.29(1.6H，s)，5.41(0.4H，s)，5.74(0.2H，d J＝11.1Hz)，5.78(0.8H，d J＝15.2Hz)，6.71-7.44(12H，m)，7.73(0.8H，d J＝8.2Hz)，7.91(0.2H，d J＝8.1Hz)，8.47(0.8H，s)，8.64(0.2H，s)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 69

Compound (69): N-(3-aminomethyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.29(3H，s)，5.77(1H，d J＝11.8Hz)，6.59-6.62(2H，m)，6.83(1H，d J＝7.5Hz)，7.05-7.24(7H，m)，7.35-7.40(4H，m)，7.80(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 70

Compound (70): N-(3,4-3,5-dimethylphenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(6H，s)，5.81(1H，d J＝11.8Hz)，6.53-6.59(2H，m)，7.00-7.07(3H，m)，7.12-7.18(2H，m)，7.23-7.25(2H，m)，7.33-7.39(4H，m)，7.78(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 71

Compound (71): N-[3-(1-methylethyl) phenyl]-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.76(1H，d J＝11.8Hz)，6.60-6.66(2H，m)，6.88(1H，dJ＝7.5Hz)，7.06(2H，d J＝7.7Hz)，7.14-7.25(5H，m)，7.33-7.40(4H，m)，7.79(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 72

Compound (72): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.81(0.07H，d J＝15.4Hz)，5.92(0.93H，d J＝15.4Hz)，6.65(2H，d J＝8.2Hz)，7.01-7.58(12H，m)，7.68(0.93H，d J＝15.4Hz)，8.01(0.07H，d J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 73

Compound (73): N-(4-propyl group phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：0.91(3H，t J＝7.2Hz)，2.22(2H，septJ＝7.2Hz)，2.52(2H，t J＝7.2Hz)，5.81(0.09H，d J＝15.2Hz)，5.92(0.91H，d J＝15.3Hz)，6.64(2H，d J＝8.5Hz)，6.97-7.56(12H，m)，7.68(0.91H，d J＝15.3Hz)，8.01(0.09H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 74

Compound (74): N-[4-(1-methylethyl) phenyl]-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.23(6H，d J＝6.9Hz)，2.85(1H，septJ＝6.9Hz)，5.81(1H，d J＝12.1Hz)，6.71-6.73(2H，m)，7.05-7.18(6H，m)，7.22-7.25(2H，m)，7.33-7.39(4H，m)，7.79(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 75

Compound (75): N-(4-difluorophenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.72(1H，d J＝11.8Hz)，6.71-6.77(2H，m)，6.92-6.97(2H，m)，7.05-7.08(2H，m)，7.14-7.23(4H，m)，7.33-7.41(4H，m)，7.82(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 76

Compound (76): N-[4-(1,1-dimethyl ethyl) phenyl]-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.59(9H，s)，5.81(0.33H，d J＝15.0Hz)，5.92(0.67H，d J＝15.0Hz)，6.65(2H，d J＝8.5Hz)，7.06-7.57(12H，m)，7.67(0.67H，d J＝15.0Hz)，8.00(0.33H，d J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 77

Compound (77): N-(4-bromo phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.69(1H，d J＝11.8Hz)，6.68(2H，dJ＝8.7Hz)，7.05-7.07(2H，m)，7.14-7.22(4H，m)，7.34-7.41(6H，m)，7.82(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 78

Compound (78): N-(3-p-methoxy-phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.77(3H，s)，5.77(1H，d J＝12.1Hz)，6.31-6.39(2H，m)，6.57-6.59(1H，m)，7.06(2H，d J＝7.7Hz)，7.14-7.24(5H，m)，7.33-7.41(4H，m)，7.80(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 79

Compound (79): 3-benzylthio--N-phenyl-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.89(2H，s)，5.84(1H，d J＝15.2Hz)，6.72(2H，d J＝7.2Hz)，7.01-7.05(1H，m)，7.14-7.31(10H，m)，7.34-7.38(2H，m)，7.58(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 80

Compound (80): N-(4-iodine substituted phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.69(1H，d J＝12.0Hz)，6.57(2H，dJ＝8.5Hz)，7.06(2H，d J＝8.0Hz)，7.11-7.21(4H，m)，7.34-7.41(4H，m)，7.55(2H，d J＝8.5Hz)，7.81(1H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 81

Compound (81): N-(indane-5-yl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.01-2.09(2H，m)，2.83-2.86(4H，m)，5.83(1H，d J＝12.0Hz)，6.55-6.57(1H，m)，6.67(1H，brs)，7.05-7.24(7H，m)，7.33-7.39(4H，m)，7.78(1H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 82

Compound (82): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 2,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.87(1H，d J＝15.1Hz)，6.64-7.48(12H，m)，7.73(1H，dJ＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 83

Compound (83): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.8Hz)，2.83(1H，septJ＝6.8Hz)，5.96(1H，d J＝15.0Hz)，6.66-7.82(17H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 84

Compound (84): N-(4-methylthio group phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.45(3H，s)，5.75(1H，d J＝11.8Hz)，6.57(2H，d，J＝8.5Hz)，7.06(2H，d，J＝7.7Hz)，7.13-7.23(6H，m)，7.34-7.41(4H，m)，7.81(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 85

Compound (85): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 5,6,7,8-tetrahydrochysene-2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝7.0Hz)，1.72-1.82(4H，m)，2.67-2.90(5H，m)，5.89(1H，d J＝14.9Hz)，6.61-6.67(2H，m)，6.85-7.52(10H，m)，7.64(1H，d J＝19.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 86

Compound (86): N-(phendioxin-6-yl)-3-(phenoxy group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：4.17-4.25(4H，m)，5.83(1H，d J＝12.0Hz)，6.28-6.35(2H，m)，6.75(1H，d J＝8.5Hz)，7.06-7.08(2H，m)，7.15-7.21(4H，m)，7.33-7.39(4H，m)，7.78(1H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 87

Compound (87): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝7.0Hz)，2.34(3H，s)，2.83(1H，sept J＝7.0Hz)，5.91(1H，d J＝15.2Hz)，6.64-7.47(13H，m)，7.65(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 88

Compound (88): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.9Hz)，2.31(3H，s)，2.83(1H，sept J＝6.9Hz)，5.90(1H，d J＝15.2Hz)，6.62-7.44(13H，m)，7.66(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 89

Compound (89): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-(1-methylethyl) phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.23(12H，m)，2.85(2H，m)，5.91(1H，d J＝15.2Hz)，6.64-7.43(13H，m)，7.66(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 90

Compound (90): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-(1,1-dimethyl ethyl) phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.8Hz)，1.31(9H，s)，2.83(1H，sept J＝6.8Hz)，5.91(1H，d J＝15.1Hz)，6.64-7.47(13H，m)，7.65(1H，d J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 91

Compound (91): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 2,3-3,5-dimethylphenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20(6H，d J＝7.2Hz)，2.16(3H，s)，2.29(3H，s)，2.77-2.88(1H，m)，5.90(1H，d J＝15.6Hz)，6.56-7.54(12H，m)，7.70(1H，d J＝15.6Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 92

Compound (92): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 2,5-difluorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20(6H，d J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.86(1H，d J＝15.2Hz)，6.64-7.48(12H，m)，7.69(1H，dJ＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 93

Compound (93): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 2,4,5-trichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝7.0Hz)，2.84(1H，septJ＝7.0Hz)，5.85(1H，d J＝15.2Hz)，6.63-7.48(11H，m)，7.73(1H，dJ＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 94

Compound (94): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 1-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.19(6H，d J＝7.0Hz)，2.81(1H，septJ＝7.0Hz)，6.00(1H，d J＝15.2Hz)，6.58(1H，d J＝8.2Hz)，7.01-7.97(15H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 95

Compound (95): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-cyano-phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d J＝7.1Hz)，2.85(1H，septJ＝7.1Hz)，5.89(1H，d J＝15.1Hz)，6.64(2H，d J＝8.3Hz)，7.07-7.69(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 96

Compound (96): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-nitrophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d J＝7.2Hz)，2.85(1H，septJ＝7.2Hz)，5.90(1H，d J＝15.2Hz)，6.65(2H，d J＝8.2Hz)，7.08-7.45(9H，m)，7.69(1H，d J＝15.2Hz)，8.24(2H，d J＝8.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 97

Compound (97): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid phendioxin, 3-dioxole-5-base ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.88(1H，d J＝15.2Hz)，5.95(2H，s)，6.61-7.44(12H，m)，7.64(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 98

Compound (98): 3-(phenoxy group)-N-(4-thiophenyl phenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.74(1H，d J＝12.0Hz)，6.78(2H，dJ＝8.5Hz)，7.06-7.24(11H，m)，7.34-7.41(6H，m)，7.84(0.83H，dJ＝12.0Hz)，7.99(0.17H，d J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 99

Compound (99): N-phenyl-3-(phenyl sulfonyl) acryloyl imido acid phenylester

Make N-phenyl-3-(thiophenyl) acryloyl imido acid phenylester (3.65g) be dissolved in chloroform (50ml), ice-cooled lower, divide 5 parts to wherein adding m-CPBA (70%:5.42g), then under identical temperature, it was stirred 2 hours.Then add chloroform (50ml) and saturated sodium bicarbonate aqueous solution (75ml) and extraction.Organic layer washs with saturated sodium-chloride water solution (50ml), drying, distillation desolventizing.Residue is through silica gel column chromatography (hexane: ethyl acetate=3: 1), obtain N-phenyl-3-(phenyl sulfonyl) acryloyl imido acid phenylester (2.08g), be faint yellow crystallization.

m.p.：110-116℃

¹H-NMR(CDCl ₃)δ(ppm)：6.73-6.75H(2H，m)，7.04(1H，d，J＝15.0Hz)，7.10-7.91(14H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 100

Compound (100): 3-(2-bromobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

Sodium hydride (60%in oil:0.026g) is suspended among the DMF (2ml), and ice-cooled lower to wherein adding 2-bromo thiophene (0.10g).In addition, to wherein adding N-phenyl-3-(phenyl sulfonyl) acryloyl imido acid phenylester (0.20g), and ice-cooled lower stirring 1 hour.After the reaction, water and ethyl acetate are joined in the reaction mixture, and extract.Organic layer washs with saturated sodium-chloride water solution, drying, and distillation desolventizing.Residue is through silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain 3-(2-bromobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester (0.19g).

¹H-NMR(CDCl ₃)δ(ppm)：5.90(1H，d，J＝15.1Hz)，6.74(2H，d，J＝7.6Hz)，6.98-7.64(13H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (101)-(130) are synthetic in the mode that is similar to embodiment 100.

Embodiment 101

Compound (101): 3-(3-bromobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.92(1H，d，J＝15.2Hz)，6.73(2H，d，J＝7.7Hz)，6.98-7.67(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 102

Compound (102): 3-(4-bromobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.85(1H，d，J＝15.4Hz)，6.71(2H，d，J＝7.8Hz)，7.02-7.46(12H，m)，7.62(1H，d，J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 103

Compound (103): 3-(4-fluorobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.76(1H，d，J＝15.2Hz)，6.70(2H，d，J＝7.2Hz)，6.98-7.42(12H，m)，7.61(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 104

Compound (104): 3-(2-fluorobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.81(1H，d，J＝14.9Hz)，6.72(2H，d，J＝7.3Hz)，6.97-7.46(12H，m)，7.58(1H，d，J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 105

Compound (105): 3-(2-methylbenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.38(3H，s)，5.65(1H，d，J＝15.0Hz)，6.69(2H，d，J＝7.5Hz)，6.95-7.42(12H，m)，7.61(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 106

Compound (106): 3-(3-methylbenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，5.87(1H，d，J＝15.2Hz)，6.73(2H，d，J＝7.2Hz)，6.98-7.39(12H，m)，7.69(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 107

Compound (107): 3-(3-anisole sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.79(3H，s)，5.91(1H，d，J＝15.2Hz)，6.73(2H，d，J＝7.5Hz)，6.83-7.39(12H，m)，7.70(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 108

Compound (108): 3-(4-nitrophenylsulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：6.15(1H，d，J＝15.2Hz)，6.76(2H，d，J＝7.2Hz)，7.03-7.53(10H，m)，7.70(1H，d，J＝15.2Hz)，8.19(2H，d，J＝8.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 109

Compound (109): N-phenyl-3-(4-pyridyl sulfenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：6.23(1H，d，J＝15.4Hz)，6.78(2H，d，J＝7.3Hz)，7.04-7.42(10H，m)，7.74(1H，d，J＝15.4Hz)，8.52(2H，d，J＝6.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 110

Compound (110): N-phenyl-3-(2-trifluoromethyl thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.88(1H，d，J＝15.0Hz)，6.72(2H，d，J＝7.5Hz)，6.98-7.70(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 111

Compound (111): N-phenyl-3-(3-trifluoromethyl thiophenyl) acryloyl imido acid phenylester

m.p.：79-81℃

¹H-NMR(CDCl ₃)δ(ppm)：5.90(1H，d，J＝15.2Hz)，6.72(2H，d，J＝7.5Hz)，6.98-7.68(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 112

Compound (112): 3-(3,5-dichlorobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

m.p.：126-131℃

¹H-NMR(CDCl ₃)δ(ppm)：5.97(1H，d，J＝15.2Hz)，6.74(2H，d，J＝7.2Hz)，7.01-7.41(11H，m)，7.60(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 113

Compound (113): 3-(3-fluorobenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.94(1H，d，J＝15.2Hz)，6.74(2H，d，J＝7.7Hz)，6.97-7.40(12H，m)，7.66(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 114

Compound (114): N-phenyl-3-(2-pyrimidine-based sulfur-base) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：6.26(1H，d，J＝15.9Hz)，6.80(2H，d，J＝8.0Hz)，7.04-7.43(9H，m)，8.59-8.63(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 115

Compound (115): N-phenyl-3-(2-pyridyl sulfenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：6.21(1H，d，J＝15.7Hz)，6.79(2H，d，J＝7.2Hz)，7.02-7.59(11H，m)，8.49-8.53(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 116

Compound (116): 3-(1-methyl-2-imidazolyl sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.63(3H，s)，5.71(1H，d，J＝15.2Hz)，6.71(2H，d，J＝7.5Hz)，6.95-7.39(10H，m)，7.61(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 117

Compound (117): 3-(4-chlorinated benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

m.p.：75.5℃

¹H-NMR(CDCl ₃)δ(ppm)：5.84(1H，d J＝15.1Hz)，6.69-6.76(2H，m)，6.98-7.05(1H，m)，7.15-7.44(11H，m)，7.62(1H，d J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 118

Compound (118): 3-(4-methylbenzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，5.79(1H，d，J＝15.2Hz)，6.71(2H，d，J＝7.2Hz)，6.97-7.38(12H，m)，7.66(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 119

Compound (119): 3-(2,4-dimethyl benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.28(3H，s)，2.33(3H，s)，5.53(1H，d，J＝15.0Hz)，6.66(2H，d，J＝7.5Hz)，6.94-7.38(11H，m)，7.57(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 120

Compound (120): 3-(2,5-dimethyl benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.27(3H，s)，2.33(3H，s)，5.63(1H，d，J＝15.0Hz)，6.69(2H，d，J＝7.5Hz)，6.95-7.39(11H，m)，7.60(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 121

Compound (121): 3-(3,5-dimethyl benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.28(6H，s)，5.85(1H，d，J＝15.0Hz)，6.73(2H，d，J＝7.2Hz)，6.92-7.39(11H，m)，7.69(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 122

Compound (122): 3-[2-(1-methylethyl) thiophenyl]-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.18(6H，d，J＝7.5Hz)，3.36-3.43(1H，m)，5.65(1H，d，J＝15.0Hz)，6.67(2H，d，J＝7.2Hz)，6.93-7.42(12H，m)，7.64(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 123

Compound (123): N-phenyl-3-(4-trifluoromethyl thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.97(1H，d，J＝15.0Hz)，6.73(2H，d，J＝7.3Hz)，6.99-7.59(12H，m)，7.67(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 124

Compound (124): 3-(4,6-dimethyl-2-pyrimidine-based sulfur-base)-N-phenylacryloyl imido acid phenylester

m.p.：175-178℃

¹H-NMR(CDCl ₃)δ(ppm)：2.44(6H，s)，6.24(1H，d，J＝15.9Hz)，6.80(3H，d，J＝6.9Hz)，7.04-7.43(8H，m)，8.63(1H，d，J＝15.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 125

Compound (125): 3-(3-chlorinated benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

m.p.：85℃

¹H-NMR(CDCl ₃)δ(ppm)：5.92(1H，d，J＝15.2Hz)，6.73(2H，d，J＝7.5Hz)，7.01(1H，t，J＝7.5Hz)，7.15-7.45(11H，m)，7.64(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 126

Compound (126): 3-(2-chlorinated benzene sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.88(1H，d，J＝15.0Hz)，6.69-6.92(2H，m)，6.95-7.12(1H，m)，7.14-7.51(11H，m)，7.52(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 127

Compound (127): 3-(2-chloro-5-pyridyl methylthio group)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.85(2H，s)，5.77(1H，d，J＝15.2Hz)，6.70(2H，d，J＝6.7Hz)，7.02-7.52(11H，m)，8.23(1H，s)。

The stereochemistry of-CH=CH-key is E.

Embodiment 128

Compound (128): 3-(2-chloro-5-thiazolyl methylthio group)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：4.00(2H，s)，5.84(1H，d，J＝15.1Hz)，6.71-7.40(11H，m)，7.49(1H，d，J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 129

Compound (129): 3-(2-chloro-5-thienyl methylthio group)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：4.00(2H，s)，5.86(1H，d，J＝15.2Hz)，6.52-7.39(12H，m)，7.53(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 130

Compound (130): 3-(4-methylbenzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，5.58(1H，d，J＝14.5Hz)，6.90-7.56(15H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 131

Compound (131): N-phenyl-3-(N '-ethanoyl-N '-phenyl amino) acryloyl imido acid phenylester

Ice-cooled lower; (60% in oil: 0.043g), and be added dropwise to DMF (2ml) solution of N-phenyl-3-(phenyl sulfonyl) acryloyl imido acid phenylester (0.30g) to add sodium hydride in DMF (3ml) solution of acetanilide N (0.14g).Ice-cooled lower, it was stirred 2 hours, then at room temperature stirred 1 hour.Ethyl acetate (100ml) is joined in the reaction mixture, and water and saturated sodium-chloride water solution sequentially wash.Organic layer is through anhydrous magnesium sulfate drying, concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=3: 1), obtain N-phenyl-3-(N '-ethanoyl-N '-phenyl amino) acryloyl imido acid phenylester (0.050g), be yellow crystal.

m.p.：120℃

¹H-NMR(CDCl ₃)δ(ppm)：1.94(3H，s)，4.72(1H，d，J＝14.0Hz)，6.57(2H，d，J＝7.5Hz)，6.85-6.87(1H，m)，7.03-7.22(7H，m)，7.35-7.39(5H，m)，8.66(1H，d，J＝14.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 132

Compound (132): 3-(N '-methyl-N '-phenyl amino)-N-phenylacryloyl imido acid phenylester

Make 3-(phenoxy group)-N-phenylacryloyl imido acid phenylester (0.39g) be dissolved in acetonitrile (5ml), under room temperature, add the N of methylphenylamine (0.20g) and catalytic amount, the N-dimethyl aminopyridine.Under identical temperature, it was stirred 2 hours, then under reflux, stirred 8 hours.Concentrating under reduced pressure.Residue is through silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain 3-(N '-methyl-N '-phenyl amino)-N-phenylacryloyl imido acid phenylester (0.17g), be the light brown crystallization.

m.p.：130-132℃

¹H-NMR(CDCl ₃)δ(ppm)：3.11(3H，s)，4.92(1H，d，J＝16.0Hz)，6.86(2H，d，J＝8.0Hz)，6.99-7.38(13H，m)，7.95(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (133)-(135) are synthetic in the mode that is similar to embodiment 132.

Embodiment 133

Compound (133): 3-(N '-benzyl-N '-methylamino)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.65(3H，s)，4.28(2H，s)，4.51(0.25H，d，J＝4.0Hz)，4.59(0.75H，d，J＝16.0Hz)，6.76-7.46(15H，m)，7.62(0.75H，d，J＝16.0Hz)，8.93(0.25H，d，J＝4.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 134

Compound (134): N-phenyl-3-(piperidino-(1-position only)) acryloyl imido acid phenylester

m.p.：127-128℃

¹H-NMR(CDCl ₃)δ(ppm)：1.56(6H，brs)，3.07(4H，brs)，4.58(1H，d，J＝16.0Hz)，6.82(2H，d，J＝4.0Hz)，6.94-6.97(1H，m)，7.11-7.37(8H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 135

Compound (135): 3-(morpholino)-N-phenylacryloyl imido acid phenylester

m.p.：146-147℃

¹H-NMR(CDCl ₃)δ(ppm)：3.10(4H，t，J＝4.0Hz)，3.68(4H，t，J＝4.0Hz)，4.67(1H，d，J＝16.0Hz)，6.81(2H，d，J＝4.0Hz)，6.95-6.99(1H，m)，7.11-7.38(8H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 136

Compound (136): 3-ethylmercapto group-N-phenylacryloyl imido acid phenylester

Make sulfur alcohol (0.11ml) be dissolved in DMF (3ml), (60% in oil: 60mg), and stirred 30 minutes under identical temperature at ice-cooled lower adding sodium hydride.Make 3-phenoxy group-N-phenylacryloyl imido acid phenylester (0.30g) be dissolved in DMF (2ml), ice-cooled lower, the solution that obtains is joined in the above-mentioned thiolate solution, and under identical temperature, stirred 2 hours, then under room temperature, stirred 2 hours.Ethyl acetate (100ml) is joined in the reaction soln, and it is sequentially washed with 1N aqueous sodium hydroxide solution, water and saturated sodium-chloride water solution, through sal epsom (anhydrous) drying, concentrating under reduced pressure.Residue is through silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain 3-ethylmercapto group-N-phenylacryloyl imido acid phenylester (0.14g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：1.29(3H，t，J＝8.0Hz)，2.71(2H，q，J＝8.0Hz)，5.80(1H，d，J＝16.0Hz)，6.78(2H，d，J＝8.0Hz)，7.00-7.03(1H，m)，7.15-7.27(5H，m)，7.36-7.40(2H，m)，7.60(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (137)-(147) are synthetic in the mode that is similar to embodiment 136.

Embodiment 137

Compound (137): N-phenyl-3-(propyl group sulfenyl) acryloyl imido acid phenylester

¹H-MR(CDCl ₃)δ(ppm)：0.95(3H，t，J＝8.0Hz)，1.60-1.69(2H，m)，2.66(2H，t，J＝8.0Hz)，5.80(1H，d，J＝16.0Hz)，6.78(2H，d，J＝8.0Hz)，7.00-7.03(1H，m)，7.15-7.27(5H，m)，7.36-7.40(2H，m)，7.59(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 138

Compound (138): 3-hexyl sulfenyl-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：0.88(3H，t，J＝8.0Hz)，1.23-1.34(6H，m)，1.55-1.64(2H，m)，2.67(2H，t，J＝8.0Hz)，5.79(1H，d，J＝16.0Hz)，6.78(2H，d，J＝8.0Hz)，7.00-7.03(1H，m)，7.15-7.27(5H，m)，7.36-7.40(2H，m)，7.60(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 139

Compound (139): 3-(1-methyl ethylmercapto group)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.32(6H，d，J＝8.0Hz)，3.19(1H，sept.，J＝8.0Hz)，5.85(1H，d，J＝16.0Hz)，6.79(2H，d，J＝8.0Hz)，6.99-7.03(1H，m)，7.16-7.26(5H，m)，7.36-7.40(2H，m)，7.62(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 140

Compound (140): 3-(1,1-dimethyl ethylmercapto group)-N-phenylacryloyl imido acid phenylester

m.p.：134-136℃

¹H-NMR(CDCl ₃)δ(ppm)：1.42(9H，s)，5.97(1H，d，J＝16.0Hz)，6.77(2H，d，J＝8.0Hz)，6.99-7.03(1H，m)，7.16-7.26(5H，m)，7.37-7.41(2H，m)，7.72(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 141

Compound (141): N-phenyl-3-(2-phenyl ethylmercapto group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.85-2.97(4H，m)，5.87(1H，d，J＝16.0Hz)，6.80(2H，d，J＝8.0Hz)，7.01-7.06(3H，m)，7.16-7.29(8H，m)，7.37-7.41(2H，m)，7.58(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 142

Compound (142): 3-dodecane sulfenyl-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：0.88(3H，t，J＝6.8Hz)，1.22-1.34(18H，m)，1.56-1.64(2H，m)，2.67(2H，t，J＝7.5Hz)，5.79(1H，d，J＝15.2Hz)，6.78(2H，d，J＝7.5Hz)，6.99-7.03(1H，m)，7.16-7.26(5H，m)，7.36-7.40(2H，m)，7.60(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 143

Compound (143): 3-allyl group sulfenyl-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.33(2H，d，J＝7.0Hz)，5.00(1H，d，J＝10.9Hz)，5.12(1H，d，J＝10.1Hz)，5.70-5.80(1H，m)，5.89(1H，d，J＝15.6Hz)，6.76(2H，d，J＝7.5Hz)，7.02(1H，t，J＝7.4Hz)，7.15-7.26(5H，m)，7.35-7.39(2H，m)，7.54(1H，d，J＝15.6Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 144

Compound (144): 3-(2-naphthyl alkyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.93(1H，d，J＝15.2Hz)，6.72(2H，d，J＝7.5Hz)，6.92-6.94(1H，m)，7.13-7.22(5H，m)，7.35-7.39(2H，m)，7.45-7.53(3H，m)，7.75-7.83(4H，m)，7.92(1H，brs)。

The stereochemistry of-CH=CH-key is E.

Embodiment 145

Compound (145): N-phenyl-3-(1-phenyl ethylmercapto group) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.60(3H，d，J＝7.0Hz)，4.14-4.20(1H，m)，5.80(1H，d，J＝15.2Hz)，6.68(2H，d，J＝7.2Hz)，7.03(1H，t，J＝7.4Hz)，7.13-7.37(12H，m)，7.49(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 146

Compound (146): 3-(4-anisole sulfenyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.79(3H，s)，5.69(1H，d，J＝16.0Hz)，6.69(1H，d，J＝8.0Hz)，6.84(2H，d，J＝8.0Hz)，6.95-7.38(11H，m)，7.62(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 147

Compound (147): 3-benzyloxy-N-phenylacryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.73(2H，s)，5.27(1H，d，J＝12.4Hz)5.30(2H，s)，6.78-6.80(2H，m)，7.01-7.06(1H，m)，7.22-7.48(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 148

Compound (148): 3-methylthio group-N-phenylacryloyl imido acid phenylester

Make 3-phenoxy group-N-phenylacryloyl imido acid phenylester (0.30g) be dissolved in THF (5ml), stirred 4 hours to the sodium salt that wherein adds methyl mercaptan (0.075g) and under room temperature.Ethyl acetate (50ml) is joined in the reaction soln, and its water and saturated sodium-chloride water solution are sequentially washed, through sal epsom (anhydrous) drying, concentrating under reduced pressure.Residue is through silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain 3-methylthio group-N-phenylacryloyl imido acid phenylester (0.20g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：2.22(3H，s)，5.72(1H，d，J＝16.0Hz)，6.79(2H，d，J＝8.0Hz)，7.00-7.04(1H，m)，7.17-7.27(5H，m)，7.36-7.40(2H，m)，7.65(1H，d，J＝16.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 149

Compound (149): N-benzyl-N-methyl-N '-phenyl-3-thiophenyl acrylamidine

Make N-phenyl-3-phenyl sulfo-acrylimide (0.77g) be suspended in toluene (15ml), then under room temperature, to wherein adding 1 DMF and thionyl chloride (0.52ml).This mixture was stirred 1 hour in 60 ℃ of oil baths.Then make it cooling and concentrating under reduced pressure. make residue be dissolved in THF (15ml).Under room temperature to wherein adding benzyl methylamine (0.77ml) and stirring 4.5 hours.The insoluble thing of filtering is also concentrated, obtains brown oil (1.39g).Make its activated alumina column chromatography (hexane: ethyl acetate=20: 1), obtain N-benzyl-N-methyl-N '-phenyl-3-(thiophenyl) acrylamidine (acrylamidine) (0.22g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：2.95(3H，s)，4.59(1.4H，s)，4.62(0.6H，s)，5.94(0.7H，d，J＝16.2Hz)，6.01(0.3H，d，J＝10.6Hz)，6.45(0.3H，d，J＝10.6Hz)，6.53(0.7H，d，J＝16.2Hz)，6.67-6.90(2H，m)，7.13-7.38(13H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 150

Compound (150): N-phenyl-3-(thiophenyl) acryloyl imido acid ethyl ester

Make N-phenyl-3-(thiophenyl) acrylamide (2.0g) be dissolved in chloroform (10ml), ice-cooled lower, to wherein being added dropwise to 7.8ml Tetrafluoroboric acid triethyl oxygen-methylene dichloride 1mol/L solution.It was stirred under room temperature 1 hour, stirred 2 hours and reflux 5 hours in 50 ℃.After the cooling, will ice-water joins in the reaction soln, then separates chloroform layer.Wash chloroform layer with water, dry and distillation desolventizing.Residue obtains N-phenyl-3-(thiophenyl) acryloyl imido acid ethyl ester (0.15g) through silica gel column chromatography (hexane/ethyl acetate=15/1), is oily matter.

¹H-NMR(CDCl ₃)δ(ppm)：1.35(1.8H，t，J＝8.4Hz)，1.51(1.2H，t，J＝8.4Hz)，4.28(1.2H，q，J＝8.4Hz)，4.39(0.8H，q，J＝8.4Hz)，5.72(0.4H，d，J＝11.1Hz)，5.78(0.6H，d，J＝15.2Hz)，6.71-7.48(11H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 151

Compound (151): 3-ethylmercapto group-N-phenylacryloyl imido acid ethyl ester

Ice-cooled lower, add the sodium salt (0.10g) of ethanethio to DMF (5ml) solution of N-phenyl-3-phenoxy group acryloyl imido acid phenylester (0.30g), and under identical temperature, stirred 3 hours.Ethyl acetate (80ml) is joined in the reaction soln, and water and saturated sodium-chloride water solution sequentially wash, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.The sodium salt (0.1g) of DMF (5ml) and ethanethio is joined in the residue, and under room temperature, stirred 3 hours.Ethyl acetate (80ml) is joined in the reaction soln, and water and saturated sodium-chloride water solution sequentially wash, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=10: 1), obtain N-phenyl-3-(ethylmercapto group) acryloyl imido acid ethyl ester (0.14g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：1.24(3H，t，J＝7.3Hz)，1.34(3H，t，J＝7.3Hz)，2.65(2H，q，J＝7.3Hz)，3.07(2H，q，J＝7.3Hz)，6.01(1H，d，J＝15.6Hz)，6.78(2H，d，J＝7.6Hz)，7.03-7.06(1H，m)，7.23-7.31(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 152

Compound (152): N-methyl-N-phenyl-N '-phenyl-3-(4-chlorinated benzene sulfenyl) acrylamidine

Make N-methyl-N-phenyl-N '-phenyl the third amidine (propynamidine) (0.23g) be dissolved in chloroform (5ml), descend to be added dropwise to chloroform (5ml) solution of 4-chloro thiophene (0.14g) and under room temperature, stirred 14 hours ice-cooled.The concentrating under reduced pressure reaction soln.Residue is through purification by silica gel column chromatography (hexane: ethyl acetate=7: 1), get N-methyl-N-phenyl-N '-phenyl-3-(4-chlorinated benzene sulfenyl) acrylamidine (0.22g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：3.41(3H，s)，5.72(0.8H，d，J＝15.9Hz)，5.92(0.2H，d，J＝10.3Hz)，6.52-7.41(15H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (153) is with synthetic with embodiment 152 similar modes.

Embodiment 153

Compound (153): N, N-dimethyl-N '-phenyl-3-(4-methylbenzene sulfenyl) acrylamidine

¹H-NMR(CDCl ₃)δ(ppm)：2.30(2.4H，s)，2.32(0.6H，s)，2.98(4.8H，s)，3.08(1.2H，s)，5.77(0.8H，d，J＝15.8Hz)，5.83(0.2H，d，J＝10.7Hz)，6.42(0.2H，d，J＝10.7Hz)，6.45(0.8H，d，J＝15.8Hz)，6.68-7.73(2H，m)，6.81-7.29(7H，m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 154

Compound (154): N-(4-hydroxy phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

Ice-cooled lower, in chloroform (80ml) solution of N-(4-p-methoxy-phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (2.4g), be added dropwise to boron tribromide dichloromethane solution (1.0M: 14.0ml), and under identical temperature, stirred 1 hour, under room temperature, stirred 2.5 hours.Chloroform (200ml) is joined in the reaction soln, its water and saturated sodium-chloride water solution are sequentially washed, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=3: 1), obtain N-(4-hydroxy phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.46g), be white crystals.

m.p.：110℃

¹H-NMR(CDCl ₃)δ(ppm)：4.73(1H，brs)，5.79(1H，d J＝11.8Hz)，6.66-6.72(4H，m)，7.06-7.39(10H，m)，7.79(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 155

Compound (155): N-(4-acetoxyl group phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

Under room temperature, salt of wormwood (0.075g) and Acetyl Chloride 98Min. (0.035ml) are joined in DMF (3ml) solution of N-(4-hydroxy phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.15g) and under identical temperature and stirred 2 hours, stirred 3 hours in 50 ℃.T-butyl methyl ether (80ml) is joined in the reaction soln, and its water and saturated sodium-chloride water solution are sequentially washed, through anhydrous magnesium sulfate drying, concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=4: 1), obtain N-(4-acetoxyl group phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.11g), be colorless oil.

¹H-NMR(CDCl ₃)δ(ppm)：2.27(3H，s)，5.79(1H，d J＝11.8Hz)，6.78-6.80(2H，m)，6.98-7.00(2H，m)，7.06-7.08(2H，m)，7.15-7.23(4H，m)，7.34-7.40(4H，m)，7.82(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 156

Compound (156): N-(4-ethynyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

Make N-(4-iodine substituted phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.40g), two (acetonitrile) dichloro palladium (II) (0.016g) and cupric iodide (I) (0.006g) be suspended in dioxane (5ml).Ice-cooled lower, (10wt% is in hexane: 0.24g) and trimethyl silyl acetylene (0.12g), and stirred 8 hours under room temperature to wherein adding diisopropylamine (0.090ml), tri-butyl phosphine.T-butyl methyl ether (50ml) is joined in the reaction soln, and water and saturated sodium-chloride water solution sequentially wash, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=4: 1) obtain white crystals (0.15g).

Make above-mentioned crystallization be dissolved in methyl alcohol (5ml), adding salt of wormwood (0.010g) also stirred 4 hours under room temperature.The concentrating under reduced pressure reaction soln.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=5: 1), obtain N-(4-ethynyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.12g), be yellow solid.

¹H-NMR(CDCl ₃)δ(ppm)：3.02(1H，s)，5.68(1H，d J＝11.8Hz)，6.75(2H，d J＝8.2Hz)，7.06(2H，d J＝7.7Hz)，7.14-7.22(4H，m)，7.34-7.41(6H，m)，7.82(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 157

Compound (157): N-(4-ethenylphenyl)-3-(phenoxy group) acryloyl imido acid phenylester

Make N-(4-iodine substituted phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.50g), two (benzylidene-acetone) palladium (0) (0.023g) and cesium carbonate (0.82g) be suspended in the dioxane (15ml).(10wt% is in hexane: 0.24g) and tributyl (vinyl) tin (0.44g) and it was stirred 4 hours under room temperature, stirred 5 hours in 60 ℃ to wherein adding tri-butyl phosphine.The insoluble thing of filtering, and concentrating under reduced pressure filtrate.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=30: 1), obtain N-(4-ethenylphenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.29g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：5.15(1H，d J＝11.6Hz)，5.65(1H，dJ＝18.4Hz)，5.76(1H，d J＝12.1Hz)，6.63-6.70(1H，m)，6.76(2H，dJ＝8.2Hz)，7.06(2H，d J＝7.7Hz)，7.13-7.22(4H，m)，7.31-7.41(6H，m)，7.80(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 158

Compound (158): N-(4-phenylbenzene)-3-(phenoxy group) acryloyl imido acid phenylester

Make N-(4-iodine substituted phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.30g), phenyl-boron dihydroxide (0.091g), two (benzylidene-acetone) palladium (0) (0.015g) and cesium carbonate (0.26g) be suspended among the THF (15ml).(10wt% is in hexane: 0.11g) and under room temperature stirred 16 hours to wherein adding tri-butyl phosphine.The insoluble thing of filtering, and concentrating under reduced pressure filtrate.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=20: 1), obtain N-(4-xenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.06g), be faint yellow crystallization.

¹H-NMR(CDCl ₃)δ(ppm)：5.82(1H，d J＝12.1Hz)，6.88(2H，dJ＝8.2Hz)，7.07(2H，d J＝7.7Hz)，7.13-7.43(11H，m)，7.50-7.52(2H，m)，7.56-7.58(2H，m)，7.83(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (159) is with synthetic with embodiment 158 similar modes.

Embodiment 159

Compound (159): 3-phenoxy group-N-(4-(3-thienyl) phenyl) acryloyl imido acid phenylester

m.p.：117℃

¹H-NMR(CDCl ₃)δ(ppm)：5.80(1H，d J＝11.8Hz)，6.84(2H，dJ＝8.2Hz)，7.07(2H，d J＝8.0Hz)，7.13-7.23(4H，m)，7.33-7.42(7H，m)，7.50-7.52(2H，m)，7.82(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 160

Compound (160): N-(4-methylsulfinyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester

Compound (161): phenyl N-(4-methyl sulphonyl phenyl)-3-(phenoxy group) acryloyl imido-ester

Make N-(4-methylthio group phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.50g) be dissolved in chloroform (15ml), then descend to be added dropwise to chloroform (10ml) solution of m-chloro benzoic acid (0.55g) and under room temperature, stirred 5 hours ice-cooled.To wherein adding chloroform (50ml), and it is used the 1N aqueous sodium hydroxide solution, water and saturated sodium-chloride water solution sequentially wash, through anhydrous magnesium sulfate drying, and concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=1: 1); obtain N-(4-methylsulfinyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.30g); be yellow oil; and N-(4-methyl sulphonyl phenyl)-3-(phenoxy group) acryloyl imido acid phenylester (0.18g), be yellow oil.

Compound (160):

¹H-NMR(CDCl ₃)δ(ppm)：2.70(3H，s)，5.65(1H，d J＝11.8Hz)，6.94(2H，d J＝8.2Hz)，7.06-7.08(2H，m)，7.15-7.23(4H，m)，7.34-7.42(4H，m)，7.56(2H，d J＝8.2Hz)，7.85(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (161):

¹H-NMR(CDCl ₃)δ(ppm)：3.30(3H，s)，5.59(1H，dJ＝11.8Hz)，6.95(2H，d J＝8.2Hz)，7.06-7.08(2H，m)，7.17-7.21(4H，m)，7.35-7.40(4H，m)，7.83(2H，d J＝8.2Hz)，7.87(1H，d J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 161

Compound (162): N-phenyl-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid methyl ester

Make N-phenyl rosickyite base imido acid methyl ester (0.30g) be dissolved in chloroform (5ml), be added dropwise to 4-thiotolene (0.19g) under ice-cooled and under room temperature, stirred 15 hours.The concentrating under reduced pressure reaction soln.Residue is through purification by silica gel column chromatography (hexane: ethyl acetate=15: 1), obtain N-phenyl-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid methyl ester (0.20g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，2.43(3H，s)，5.99(1H，d，J＝15.1Hz)，6.68-6.75(2H，m)，7.00-7.35(8H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (163)-(169) are synthetic in the mode that is similar to embodiment 161.

Embodiment 162

Compound (163): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.44(3H，s)，6.09(1H，d，J＝15.6Hz)，6.73(2H，d，J＝7.3Hz)，7.00-7.39(9H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 163

Compound (164): 3-(4-chlorinated benzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.44(3H，s)，6.04(1H，d，J＝16.1Hz)，6.71(2H，d，J＝7.7Hz)，7.06(1H，br)，7.22-7.31(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 164

Compound (165): 3-(4-chlorinated benzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.41(3H，brs)，6.40(1H，br)，6.90-7.48(10H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 165

Compound (166): 3-(4-fluorobenzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.30(2H，s)，5.94(1H，d，J＝15.6Hz)，6.67-6.73(1H，m)，6.93-7.09(3H，m)，7.20-7.42(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 166

Compound (167): 3-(4-chlorinated benzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.31(2H，s)，6.03(1H，d，J＝15.5Hz)，6.72(2H，d，J＝7.5Hz)，7.04-7.10(1H，m)，7.21-7.41(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 167

Compound (168): 3-(3-methylbenzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.30(3H，s)，4.31(2H，s)，6.06(1H，d，J＝15.3Hz)，6.73(2H，d，J＝8.2Hz)，7.00-7.42(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 168

Compound (169): N-phenyl-3-(3-trifluoromethyl thiophenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.33(2H，s)，6.09(1H，d，J＝15.6Hz)，6.73(2H，d，J＝8.2Hz)，7.02-7.10(1H，def.t)，7.21-7.63(12H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (170)-(173) are synthetic in the mode that is similar to embodiment 37.

Embodiment 169

Compound (170): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-methylthio group phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d，J＝6.8Hz)，2.45(3H，s)，2.84(1H，sept J＝6.8Hz)，5.90(1H，d，J＝15.2Hz)，6.64(2H，d，J＝8.2Hz)，7.05-7.41(11H，m)，7.66(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 170

Compound (171): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-methyl sulphonyl phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d，J＝7.0Hz)，2.85(1H，septJ＝7.0Hz)，3.04(3H，s)，5.90(1H，d，J＝15.0Hz)，6.66(2H，d，J＝8.5Hz)，7.08-7.45(9H，m)，7.69(1H，d，J＝15.0Hz，CH)，7.94(2H，d，J＝8.7Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 171

Compound (172): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-cyclohexyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝6.8Hz)，1.26-1.40(6H，m)，1.84(4H，m)，2.47(1H，m)，2.84(1H，sept J＝6.8Hz)，5.91(1H，d，J＝15.2Hz)，6.64(2H，d，J＝8.2Hz)，7.04-7.45(11H，m)，7.65(1H，d，J＝15.2Hz，CH)。

The stereochemistry of-CH=CH-key is E.

Embodiment 172

Compound (173): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 3-biphenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.94(1H，d，J＝15.1Hz)，6.67(2H，d，J＝8.0Hz)，7.05-7.59(16H，m)，7.70(1H，d，J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (174) is with synthetic with embodiment 161 similar modes.

Embodiment 173

Compound (174): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 1-methylethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.38(6H，d，J＝7.8Hz)，3.82-3.94(1H，m)，6.06(1H，d，J＝15.6Hz)，6.73(2H，d，J＝8.0Hz)，7.03(1H，t，J＝7.4Hz)，7.22-7.40(8H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (175) and (176) are synthetic in the mode that is similar to embodiment 37.

Embodiment 174

Compound (175): N-(4-cyclohexyl phenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.29-1.45(4H，m)，1.68-1.91(6H，m)，2.38-2.49(1H，m)，5.81(0.21H，d J＝15.0Hz)，5.93(0.75H，d，J＝15.2Hz)，6.13(0.04H，d，J＝9.9Hz)，6.64(1H，d，J＝8.2Hz)，7.01-7.56(13.04H，m)，7.67(0.75H，d J＝15.2Hz)，8.00(0.21H，d J＝15.0Hz)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 175

Compound (176): N-(4-cyclohexyl sulfenyl phenyl)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：0.87-0.90(2H，m)，1.23-1.33(4H，m)，1.74-1.76(2H，m)，1.92-1.94(2H，m)，2.98-3.00(1H，m)，5.74(1H，d，J＝12.0Hz)，6.73(2H，d，J＝8.3Hz)，7.07(2H，d，J＝8.0Hz)，7.13-7.22(4H，m)，7.33-7.40(6H，m)，7.82(1H，d，J＝12.0Hz，CH)。

The stereochemistry of-CH=CH-key is E.

Embodiment 176

Compound (177): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-(1,1-dimethyl ethyl) phenylester

Make N-phenyl-3-(thiophenyl) acrylamide (0.77g) be suspended in toluene (15ml), then under room temperature, to wherein adding thionyl chloride (0.52ml) and 1 DMF.In 60 ℃ of oil baths, stirred this mixture 1 hour.The concentrating under reduced pressure reaction mixture.Make residue be dissolved in THF (15ml).

Ice-cooled lower, (55% in oil: 0.25g) be suspended among the THF (5ml), and ice-cooled lower to wherein adding 4-(tertiary butyl) thiophene (0.57ml) to make sodium hydride.Ice-cooled lower, this suspension is joined in the THF solution of above-mentioned residue, and under identical temperature, stirred 15 minutes. then to wherein adding methyl-iodide (0.1ml).Saturated sodium-chloride water solution (20ml) and water (10ml) are joined in the reaction mixture, and extract twice with ethyl acetate (20ml).Merge organic layer and use saturated sodium-chloride water solution (20ml) washing, dry through anhydrous sodium chlorate, the filtering inorganic salt, concentrating under reduced pressure obtains brown oil (1.36g).Make it through silica gel column chromatography (hexane: ethyl acetate=20: 1) obtain faint yellow oily thing, the standby type high performance liquid chromatography purifying (hexane: ethyl acetate=99: 1) of compacting in the warp, obtain N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 4-(1,1-dimethyl ethyl) phenylester (0.20g).

¹H-NMR(CDCl ₃)δ(ppm)：1.33(9H，s)，5.83(1H，d J＝15.0Hz)，6.90-7.58(15H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (178) and (179) are synthetic in the mode that is similar to embodiment 176.

Embodiment 177

Compound (178): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) sulfo-acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.24(6H，d J＝7.0Hz)，2.85-2.92(1H，m)，5.55(1H，d J＝15.0Hz)，6.62-8.05(17H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 178

Compound (179): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) sulfo-acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.28(6H，d J＝7.0Hz)，2.90-2.97(1H，m)，5.83(1H，d J＝10.1Hz)，6.78(1H，d J＝9.9Hz)，7.07(2H，d J＝8.2Hz)，7.25-7.32(5H，m)，7.43(2H，d J＝6.7Hz)，7.53(3H，d J＝7.2Hz)，7.82(3H，d J＝8.5Hz)，8.04(1H，s)。

The stereochemistry of-CH=CH-key is Z.

Compound (180)-(185) are synthetic in the mode that is similar to embodiment 37.

Embodiment 179

Compound (180): N-(4-Phenoxyphenyl)-3-(thiophenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.81(0.29H，d J＝15.1Hz)，5.90(0.71H，d，J＝15.1Hz)，6.70(2H，d，J＝8.7Hz)，7.13-7.56(17H，m)，7.72(0.71H，d J＝15.1Hz)，8.00(0.29H，d J＝15.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 180

Compound (181): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-biphenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d，J＝6.8Hz)，2.84(1H，septJ＝6.8Hz)，5.93(1H，d，J＝15.2Hz)，6.67(2H，d，J＝8.2Hz)，7.06-7.58(16H，m)，7.70(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 181

Compound (182): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-methoxycarbonyl phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d，J＝7.0Hz)，2.84(1H，septJ＝7.0Hz)，3.89(3H，s)，5.91(1H，d，J＝15.2Hz)，6.65(2H，d，J＝8.2Hz)，7.07(2H，d，J＝8.2Hz)，7.14-7.44(7H，m)，7.67(1H，d，J＝15.2Hz)，8.05(2H，d，J＝8.7Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 182

Compound (183): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-(1H-imidazoles-1-yl) phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝6.9Hz)，2.83(1H，sept)，5.90(1H，d，J＝15.2Hz)，6.62-7.44(16H，m)，7.66(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 183

Compound (184): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-p-methoxy-phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝6.8Hz)，2.83(1H，septJ＝6.8Hz)，3.77(3H，s)，5.90(1H，d，J＝15.0Hz)，6.64(2H，d，J＝8.5Hz)，6.86-7.46(11H，m)，7.66(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 184

Compound (185): N-[4-(1,1-dimethyl oxyethyl group) phenyl]-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.30(9H，s)，5.76(1H，d，J＝12.1Hz)，6.68-6.70(2H，m)，6.88-6.90(2H，m)，7.07(2H，d，J＝8.7Hz)，7.13-7.23(4H，m)，7.33-7.40(4H，m)，7.81(1H，d，J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (186) and (187) are synthetic in the mode that is similar to embodiment 161.

Embodiment 185

Compound (186): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2-propenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.73(2H，d，J＝7.1Hz)，5.12(1H，d，J＝17.0Hz)，5.27(1H，brs)，5.87-6.01(1H，m)，6.08(1H，d，J＝15.8Hz)，6.72(2H，d，J＝7.8Hz)，7.00-7.43(9H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 186

Compound (187): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.26-1.63(6H，m)，1.65-1.78(2H，m)，2.02-2.12(2H，m)，3.70-3.81(1H，m)，6.06(1H，d，J＝16.0Hz)，6.68-6.75(2H，d)，6.98-7.07(1H，m)，7.20-7.43(8H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (188)-(190) are synthetic in the mode that is similar to embodiment 37.

Embodiment 187

Compound (188): N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acryloyl imido acid 4-aminophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝7.0Hz)，2.83(1H，septJ＝7.0Hz)，5.89(1H，d，J＝15.2Hz)，6.65-7.43(15H，m)，7.65(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 188

Compound (189): N-phenyl-3-(thiophenyl) acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.93(1H，d，J＝15.2Hz)，6.74(2H，d，J＝7.5Hz)，6.97-7.83(16H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 189

Compound (190): N-phenyl-3-phenyl sulfo-acryloyl imido acid 2,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.84(1H，d，J＝15.2Hz)，6.73(2H，d，J＝7.5Hz)，6.99-7.44(11H，m)，7.76(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (191) is with synthetic with embodiment 161 similar modes.

Embodiment 190

Compound (191): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 2-propynyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(1H，t，J＝2.5Hz)，3.86(2H，d，J＝2.7Hz)，6.10(1H，d，J＝15.4Hz)，6.74(2H，d，J＝7.5Hz)，7.03-7.60(9H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (192) and (193) are synthetic in the mode that is similar to embodiment 37.

Embodiment 191

Compound (192): N-phenyl-3-phenoxy group acryloyl imido acid 2,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.71(1H，d，J＝12.0Hz)，6.80(2H，d，J＝7.8Hz)，6.90-7.43(11H，m)，7.85(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 192

Compound (193): N-phenyl-3-phenoxy group acryloyl imido acid 2-naphthyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.79(1H，d，J＝12.0Hz)，6.82(2H，d，J＝7.3Hz)，6.97-7.90(16H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (194) is with synthetic with embodiment 161 similar modes.

Embodiment 193

Compound (194): N-phenyl-3-(thiophenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d，J＝7.7Hz)，4.96-5.06(1H，m)，6.04(1H，d，J＝15.7Hz)，6.70(2H，d，J＝7.5Hz)，7.00-7.46(14H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (195) is with synthetic with embodiment 100 similar modes.

Embodiment 194

Compound (195): 3-(1-naphthyl alkyl)-N-phenylacryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.58(1H，d，J＝15.0Hz)，6.52(2H，d，J＝7.2Hz)，6.85-6.89(1H，m)，6.99-7.03(2H，m)，7.12-7.17(3H，m)，7.32-7.42(3H，m)，7.54-7.62(2H，m)，7.66(1H，d，J＝15.0Hz)，7.71-7.73(1H，m)，7.83-7.88(2H，m)，8.27-8.29(1H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (196) and (197) are synthetic in the mode that is similar to embodiment 37.

Embodiment 195

Compound (196): 3-phenoxy group-N-(4-piperidino-(1-position only) phenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.53-1.57(2H，m)，1.68-1.73(4H，m)，3.05-3.08(4H，m)，5.84(1H，d，J＝12.1Hz)，6.71-6.73(2H，m)，6.86-6.88(2H，m)，7.05-7.07(2H，m)，7.14-7.23(4H，m)，7.33-7.39(4H，m)，7.78(1H，d，J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 196

Compound (197): N-[4-(1-methylethyl) phenyl]-3-phenoxy group acryloyl imido acid 2,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝7.0Hz)，2.85(1H，septJ＝7.0Hz)，5.78(1H，d，J＝11.8Hz)，6.73(2H，d，J＝8.2Hz)，7.05-7.37(10H，m)，7.84(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (198) and (199) are synthetic in the mode that is similar to embodiment 161.

Embodiment 197

Compound (198): N-phenyl-3-(phenoxy group) sulfo-acryloyl imido acid 1-methylethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.40(6H，d，J＝7.3Hz)，3.90-4.02(1H，m)，5.94(1H，d，＝12.6Hz)，6.95-7.40(10H，m)，7.52(1H，d，J＝12.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 198

Compound (199): 3-(4-methyl benzylthio-)-N-(phenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，3.79(2H，s)，4.29(2H，s)，6.07(1H，d，J＝15.4Hz)，6.78(2H，d，J＝7.3Hz)，7.00-7.40(13H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (200)-(204) are synthetic in the mode that is similar to embodiment 37.

Embodiment 199

Compound (200): N-[4-(1-methylethyl) phenyl]-3-phenoxy group acryloyl imido acid 2,3-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝7.4Hz)，2.85(1H，septJ＝7.4Hz)，5.78(1H，d，J＝12.0Hz)，6.72(2H，d，J＝8.3Hz)，7.05-7.38(10H，m)，7.85(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 200

Compound (201): N-[4-(1-methylethyl) phenyl]-3-phenoxy group acryloyl imido acid 3,5-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.23(6H，d，J＝6.8Hz)，2.87(1H，septJ＝6.8Hz)，5.78(1H，d，J＝12.0Hz)，6.74(2H，d，J＝8.3Hz)，7.03-7.37(10H，m)，7.73(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 201

Compound (202): N-[4-(1-methylethyl) phenyl]-3-phenoxy group acryloyl imido acid 2,4 dichloro benzene base ester

¹H-NMR(CDCl ₃)δ(ppm)：1.21(6H，d，J＝6.8Hz)，2.85(1H，septJ＝6.8Hz)，5.77(1H，d，J＝12.0Hz)，6.71(2H，d，J＝8.3Hz)，7.05-7.43(10H，m)，7.84(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 202

Compound (203): N-(3,4-3,5-dimethylphenyl)-3-phenyl sulfo-acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.34(3H，s)，5.96(1H，d，J＝15.0Hz)，6.47-6.53(2H，m)，6.95-7.43(10H，m)，7.65(1H，d，J＝15.0Hz，CH)。

The stereochemistry of-CH=CH-key is E.

Embodiment 203

Compound (204): N-(4-benzyl phenyl)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.93(2H，s)，5.78(1H，d，J＝12.1Hz)，6.72(2H，d，J＝8.5Hz)，7.05-7.09(4H，m)，7.11-7.40(13H，m)，7.79(1H，d，J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (205) is with synthetic with embodiment 161 similar modes.

Embodiment 204

Compound (205): N-phenyl-3-(phenoxy group) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.36(2H，s)，5.96(1H，d，J＝12.3Hz)，6.77-7.54(16H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (206) is with synthetic with embodiment 99 similar modes.

Embodiment 205

Compound (206): N-phenyl-3-(phenyl sulfonyl) sulfo-acryloyl imido acid phenylester

m.p.：69-70℃

¹H-NMR(CDCl ₃)δ(ppm)：6.86-7.74(m)

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (207) is with synthetic with embodiment 37 similar modes.

Embodiment 206

Compound (207): N-(4-Trifluoromethoxyphen-l)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.69(1H，d，J＝11.8Hz)，6.79(2H，d，J＝8.7Hz)，7.06-7.22(8H，m)，7.34-7.41(4H，m)，7.84(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (208) is with synthetic with embodiment 161 similar modes.

Embodiment 207

Compound (208): N-phenyl-3-(thiophenyl 9 sulfo-acryloyl imido acid cyclohexyl esters

¹H-NMR(CDCl ₃)δ(ppm)：1.26-2.15(8H，m)，3.22(2H，brs)，3.95(1H，Br)，6.42(1H，d，J＝10.1Hz)，6.90-7.55(11H，m)。

The stereochemistry of-CH=CH-key is Z.

Compound (209) is with synthetic with embodiment 37 similar modes.

Embodiment 208

Compound (209): N-(3,4-3,5-dimethylphenyl)-3-phenoxy group acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，5.80(1H，d，J＝11.8Hz)，6.54-6.60(2H，m)，6.96-7.37(10H，m)，7.76(1H，d，J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (210) is with synthetic with embodiment 100 similar modes.

Embodiment 209

Compound (210): N-(3,4-3,5-dimethylphenyl)-3-benzyloxy acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，4.80(2H，s)，5.42(1H，d，J＝12.3Hz)，6.52-7.21(12H，m)，7.62(1H，d，J＝12.3Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (211)-(234) are synthetic in the mode that is similar to embodiment 161.

Embodiment 210

Compound (211): 3-(2-fluorobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.30(2H，s)，6.00(1H，d J＝15.7Hz)，6.73(2H，d J＝7.3Hz)，7.02-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 211

Compound (213): 3-(3-fluorobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.00(1H，d J＝15.7Hz)，6.73(2H，d J＝7.3Hz)，7.02-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 212

Compound (215): 3-(2-chlorinated benzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.08(1H，d J＝15.4Hz)，6.75(2H，d J＝7.3Hz)，7.03-7.40(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 213

Compound (217): 3-(3-chlorinated benzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.11(1H，d J＝15.7Hz)，6.74(2H，d J＝7.3Hz)，7.06(1H，t J＝7.5Hz)，7.21-7.34(10H，m)，7.39(2H，d J＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 214

Compound (219): 3-(4-chlorinated benzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.31(2H，s)，6.03(1H，d J＝15.7Hz)，6.72(2H，d J＝7.3Hz)，7.07(1H，t J＝7.5Hz)，7.22-7.32(10H，m)，7.38(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 215

Compound (221): 3-(3-bromobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.10(1H，d J＝15.7Hz)，6.74(2H，d J＝7.3Hz)，7.07(1H，t J＝7.5Hz)，7.16(1H，t J＝8.0Hz)，7.23-7.32(8H，m)，7.39(2H，d J＝7.3Hz)，7.49(1H，s)。

The stereochemistry of-CH=CH-key is E.

Embodiment 216

Compound (223): 3-(4-bromobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.31(2H，s)，6.04(1H，d J＝15.7Hz)，6.72(2H，d J＝7.3Hz)，7.08(1H，t J＝7.3Hz)，7.18(2H，d J＝8.6Hz)，7.22-7.32(6H，m)，7.40(4H，t J＝8.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 217

Compound (225): 3-(4-nitrophenylsulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.34(2H，s)，6.33(1H，d J＝15.7Hz)，6.77(2H，d J＝7.3Hz)，7.10(1H，t J＝7.3Hz)，7.24-7.43(10H，m)，8.15(2H，d J＝8.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 218

Compound (226): 3-(2-methylbenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.30(3H，s)，4.30(2H，s)，5.83(1H，dJ＝15.4Hz)，6.69(2H，d J＝7.3Hz)，7.02(1H，t J＝7.5Hz)，7.09-7.39(10H，m)，7.38(2H，d J＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 219

Compound (228): 3-(4-methylbenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.31(3H，s)，4.30(2H，s)，5.98(1H，dJ＝15.4Hz)，6.72(2H，d J＝7.3Hz)，7.02-7.33(11H，m)，7.38(2H，dJ＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 220

Compound (230): N-phenyl-3-(4-trifluoromethyl thiophenyl)-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.17(1H，d J＝15.7Hz)，6.74(2H，d J＝7.3Hz)，7.07(1H，t J＝7.5Hz)，7.25-7.32(6H，m)，7.41(4H，t J＝8.8Hz)，7.54(2H，d J＝8.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 221

Compound (232): 3-(3-anisole sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.77(3H，s)，4.31(2H，s)，6.10(1H，dJ＝15.4Hz)，6.74(2H，d J＝7.3Hz)，6.81(1H，d J＝8.1Hz)，6.87(1H，s)，6.92(1H，d J＝7.8Hz)，7.03-7.40(10H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 222

Compound (234): 3-(4-anisole sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.78(3H，s)，4.29(2H，s)，5.87(1H，dJ＝15.4Hz)，6.70(2H，d J＝7.3Hz)，6.80(2H，d J＝7.2Hz)，7.02(1H，t J＝7.3Hz)，7.22-7.31(8H，m)，7.38(2H，d J＝6.6Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 223

Compound (235): 3-(4-fluoro benzylthio-)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

Make N-phenyl proyl imido acid benzyl ester (propynthioimidate) (0.30g) be dissolved in chloroform (15ml) with 4-fluoro benzyl mercaptan, ice-cooled lower, stirred 14 hours to the potassium tert.-butoxide that wherein adds catalytic amount and under room temperature.The concentrating under reduced pressure reaction mixture.Residue is through purification by silica gel column chromatography (hexane: ethyl acetate=15: 1), obtain 3-(4-fluoro benzylthio-)-N-phenyl-sulfo-acryloyl imido acid benzyl ester (0.15g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：3.79(2H，s)，4.29(2H，s)，6.03(1H，d J＝15.7Hz)，6.71(2H，d J＝7.3Hz)，6.94(2H，t J＝8.7Hz)，7.05-7.12(3H，m)，7.20(1H，d J＝15.4Hz)，7.24-7.32(5H，m)，7.38(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (236)-(246) and (257) are synthetic in the mode that is similar to embodiment 223.

Embodiment 224

Compound (237): 3-(4-methyl benzylthio-)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，3.78(2H，s)，4.29(2H，s)，6.07(1H，d J＝15.7Hz)，6.73(2H，d J＝7.3Hz)，7.02-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 225

Compound (239): 3-(4-chloro benzylthio-)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.78(2H，s)，4.29(2H，s)，6.01(1H，d J＝15.4Hz)，6.70(2H，d J＝7.3Hz)，7.02-7.32(11H，m)，7.38(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 226

Compound (241): 3-(2,4-benzyl dichloride sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.90(2H，s)，4.30(2H，s)，6.01(1H，dJ＝15.7Hz)，6.70(2H，dJ＝7.3Hz)，7.06(2H，t J＝7.5Hz)，7.15-7.34(8H，m)，7.38(2H，d J＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 227

Compound (243): 3-(2-methyl benzylthio-)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.27(3H，s)，3.82(2H，s)，4.30(2H，s)，6.07(1H，d J＝15.4Hz)，6.75(2H，d J＝7.3Hz)，7.06(1H，t J＝7.3Hz)，7.13-7.32(10H，m)，7.39(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 228

Compound (245): 3-(4-methoxybenzyl sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.77(2H，s)，3.78(3H，s)，4.29(2H，s)，6.07(1H，dJ＝15.4Hz)，6.73(2H，d J＝7.3Hz)，6.79(2H，d J＝8.6Hz)，7.05-7.39(9H，m)，7.38(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (247)-(256) and (258) are synthetic in the mode that is similar to embodiment 161.

Embodiment 229

Compound (248): 3-(2,4 dichloro benzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.03(1H，d J＝15.4Hz)，6.73(2H，d J＝7.3Hz)，7.07(1H，t J＝7.3Hz)，7.16-7.40(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 230

Compound (250): 3-(3,5-dichlorobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.03(1H，d J＝15.4Hz)，6.75(2H，d J＝7.3Hz)，7.08(2H，t J＝7.5Hz)，7.20-7.34(8H，m)，7.40(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 231

Compound (252): 3-(2,4-dimethyl benzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.25(3H，s)，2.26(3H，s)，4.32(2H，s)，5.71(1H，d J＝15.4Hz)，6.67(2H，d J＝7.3Hz)，6.90-7.04(4H，m)，7.18-7.31(6H，m)，7.38(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 232

Compound (254): N-phenyl-3-(2-pyridyl sulfenyl)-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.35(2H，s)，6.40(1H，d J＝16.2Hz)，6.81(2H，d J＝7.3Hz)，7.09(2H，t J＝7.3Hz)，7.18(1H，d J＝7.8Hz)7.26(1H，d J＝7.3Hz)，7.32(4H，t J＝7.8Hz)，7.43(2H，d J＝7.3Hz)，7.55(1H，t J＝7.8Hz)，8.21(1H，d J＝16.2Hz)，8.50(1H，d J＝5.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 233

Compound (256): N-phenyl-3-(2-pyrimidine-based sulfur-base)-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.36(2H，s)，6.44(1H，d J＝16.4Hz)，6.81(2H，d J＝7.3Hz)，7.05-7.12(2H，m)，7.24-7.35(5H，m)，7.44(2H，d J＝7.1Hz)，8.30(1H，d J＝16.4Hz)，8.57(2H，d J＝5.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 234

Compound (258): 3-(3,4-dichlorobenzene sulfenyl)-N-phenyl-sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：4.32(2H，s)，6.06(1H，d，J＝15.5Hz)，6.73(2H，d，J＝7.5Hz)，7.10-7.43(12H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (259) is with synthetic with embodiment 176 similar modes.

Embodiment 235

Compound (259): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-(1-methylethyl) phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.23(6H，d J＝7.0Hz)，2.29(3H，s)，2.82(1H，sept.J＝7.0Hz)，5.93(1H，d J＝15.0Hz)，6.63(2H，d J＝7.8Hz)，7.02(2H，d J＝8.0Hz)，7.11(2H，d J＝8.3Hz)，7.20-7.42(7H，m)，7.66(1H，d J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (260) is with synthetic with embodiment 161 similar modes.

Embodiment 236

Compound (260): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，4.30(2H，s)，6.13(1H，d，J＝15.7Hz)，6.65(2H，d，J＝8.0Hz)，7.21-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 237

Compound (261): N-benzyloxy-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

Under room temperature, the sodium salt (0.14g) of thiophenol is joined ethanol (5ml) solution of N-benzyloxy-3-thiophenyl acryloyl imido acid bromide (acrylimidoyl bromide) (0.30g), then with its reflux 3 hours.Make it cooling, chloroform (50ml) is joined in the reaction mixture.It is sequentially washed with 1N aqueous sodium hydroxide solution, pure water, saturated sodium-chloride water solution.Organic layer is through anhydrous magnesium sulfate drying, concentrating under reduced pressure. residue is through purification by silica gel column chromatography (hexane: ethyl acetate=20: 1), obtain N-benzyloxy-3-(thiophenyl) sulfo-acryloyl imido acid phenylester (0.14g), be colorless oil.

¹H-NMR(CDCl ₃)δ(ppm)：5.21(2H，s)，5.49(1H，d，J＝15.0Hz)，6.99(1H，d，J＝15.0Hz)，7.14-7.18(2H，m)，7.21-7.39(13H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (262) is with synthetic with embodiment 36 similar modes.

Embodiment 238

Compound (262): N-(N '-methyl-N '-phenyl amino)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.17(3H，s)，5.53(1H，d，J＝14.7Hz)，6.90-6.96(3H，m)，7.20-7.42(13H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (263)-(265) are synthetic in the mode that is similar to embodiment 176.

Embodiment 239

Compound (263): N-(4-difluorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.80(1H，d J＝10.2Hz)，6.84(1H，dJ＝10.2Hz)，7.05-7.11(4H，m)，7.25-7.51(10H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 240

Compound (264): N-(4-difluorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.67(0.77H，d J＝14.6Hz)，5.80(0.08H，dJ＝10.0Hz)，5.99(0.15H，d J＝15.4Hz)，6.62(0.3H，br.m)，6.82-6.61(1.7H，m)，6.99-7.09(2H，m)，7.25-7.57(11H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 241

Compound (265): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 1,1-dimethyl ethyl ester

¹H-NMR (CDCl ₃) δ (ppm): 1.38 (2.1H, s), 1.56 (6.9H, s), 2.31 (0.7H, s), (2.32 2.3H, s), 6.07 (0.77H, d J=15.5Hz), 6.15 (0.23H, d J=15.7Hz), (6.64 d J=8.5Hz), the total 2H of 6.67 (d J=8.2Hz), 7.06-7.09 (2H, m), 7.27-7.38 (6H, m).

The stereochemistry of-CH=CH-key is E.

Compound (266) and (267) are synthetic in the mode that is similar to embodiment 161.

Embodiment 242

Compound (266): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid ethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.33(3H，t J＝7.4Hz)，2.32(3H，s)，2.89(2H，sept)，6.13(1H，d，J＝15.5Hz)，6.63(2H，d，J＝8.2Hz)，7.05-7.38(8H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 243

Compound (267): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid ethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.28-1.33(3H，m)，2.34(3H，s)，2.91-2.93(2H，m)，6.39(1H，d，J＝10.0Hz)，6.89-7.49(10H，m)。

The stereochemistry of-CH=CH-key is Z.

Compound (268)-(277) are synthetic in the mode that is similar to embodiment 100.

Embodiment 244

Compound (268): N-(3,4-3,5-dimethylphenyl)-3-(4-fluorobenzene sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.18(3H，s)，2.19(3H，s)，2.35(3H，s)，5.80(1H，d J＝15.2Hz)，6.45(1H，d J＝7.8Hz)，6.50(1H，brs)，6.94-7.04(7H，m)，7.34-7.42(2H，m)，7.55(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 245

Compound (269): N-(3,4-3,5-dimethylphenyl)-3-(4-chlorinated benzene sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.35(3H，s)，5.88(1H，d J＝15.2Hz)，6.46(1H，d J＝7.8Hz)，6.50(1H，brs)，6.96-7.00(3H，m)，7.22-7.36(6H，m)，7.56(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 246

Compound (270): N-(3,4-3,5-dimethylphenyl)-3-(4-methylbenzene sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.18(3H，s)，2.19(3H，s)，2.33(3H，s)，2.34(3H，s)，5.87(1H，d J＝14.9Hz)，6.47(1H，d J＝7.8Hz)，6.51(1H，brs)，6.94-6.99(4H，m)，7.12-7.14(2H，m)，7.21-7.23(1H，m)，7.30-7.32(2H，m)，7.61(1H，d J＝14.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 247

Compound (271): N-(3,4-3,5-dimethylphenyl)-3-(4-anisole sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.17(3H，s)，2.18(3H，s)，2.34(3H，s)，3.80(3H，s)，5.76(1H，d J＝15.2Hz)，6.45(1H，d J＝7.8Hz)，6.49(1H，brs)，6.83-6.86(2H，m)，6.93-6.98(4H，m)，7.20-7.24(1H，m)，7.34-7.36(2H，m)，7.56(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 248

Compound (272): N-(3,4-3,5-dimethylphenyl)-3-(2-pyridyl sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(6H，s)，2.37(3H，s)，6.25(1H，dJ＝15.7Hz)，6.53(1H，d J＝7.8Hz)，6.59(1H，brs)，6.97-7.14(7H，m)，7.55-7.59(1H，m)，8.45(1H，d J＝15.9Hz)，8.49-8.53(1H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 249

Compound (273): N-(3,4-3,5-dimethylphenyl)-3-(2-pyrimidine-based sulfur-base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(6H，s)，2.38(3H，s)，6.29(1H，d J＝15.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.98-7.09(6H，m)，8.55(1H，d J＝15.9Hz)，8.58-8.60(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 250

Compound (274): N-(3,4-3,5-dimethylphenyl)-3-(benzylthio-) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.35(3H，s)，3.90(2H，s)，5.90(1H，d J＝15.2Hz)，6.47(1H，d J＝7.8Hz)，6.54(1H，brs)，6.95-7.00(4H，m)，7.20-7.28(6H，m)，7.53(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 251

Compound (275): N-(3,4-3,5-dimethylphenyl)-3-(4-fluoro benzylthio-) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.35(3H，s)，3.87(2H，s)，5.87(1H，d J＝15.2Hz)，6.46(1H，d J＝8.1Hz)，6.53(1H，brs)，6.89-6.99(7H，m)，7.15-7.18(2H，m)，7.50(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 252

Compound (276): N-(3,4-3,5-dimethylphenyl)-3-(4-methyl benzylthio-) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.33(3H，s)，2.35(3H，s)，3.86(2H，s)，5.90(1H，d J＝14.9Hz)，6.47(1H，d J＝7.8Hz)，6.54(1H，brs)，6.95-7.00(4H，m)，7.09(4H，brs)，7.21-7.23(1H，m)，7.54(1H，d J＝14.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 253

Compound (277): N-(3,4-3,5-dimethylphenyl)-3-(4-methoxybenzyl sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.35(3H，s)，3.80(3H，s)，3.86(2H，s)，5.90(1H，d J＝15.2Hz)，6.48(1H，d J＝7.8Hz)，6.55(1H，brs)，6.80-6.82(2H，m)，6.95-7.00(4H，m)，7.12-7.14(2H，m)，7.21-7.23(1H，m)，7.55(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (278) and (279) are synthetic in the mode that is similar to embodiment 176.

Embodiment 254

Compound (278): N-(4-difluorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-difluorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：5.46(0.83H，d J＝14.4Hz)，5.97(0.17H，dJ＝15.6Hz)，6.59(0.51H，Br)，6.84-7.06(4.49H，m)，7.25-7.32(7H，m)，7.49-7.59(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 255

Compound (279): N-(4-difluorophenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-p-methoxy-phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.80(0.30H，s)，3.83(1.29H，s)，3.85(1.41H，s)，5.57(0.47H，d J＝14.9Hz)，5.80(0.43H，d J＝10.0Hz)，5.97(0.10H，d J＝15.4Hz)，6.59(0.2H，Br)，6.78-6.91(3.8H，m)，7.00-7.11(3H，m)，7.21-7.56(7H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (280)-(284) are synthetic in the mode that is similar to embodiment 161.

Embodiment 256

Compound (280): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid propyl diester

¹H-NMR(CDCl ₃)δ(ppm)：1.01(3H，t J＝7.3Hz)，1.70(2H，m)，2.31(3H，s)，3.04(2H，t J＝7.2Hz)，6.13(1H，d，J＝15.6Hz)，6.63(2H，d，J＝8.0Hz)，7.05-7.49(8H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 257

Compound (281): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid propyl diester

¹H-NMR(CDCl ₃)δ(ppm)：0.99(3H，m)，1.63(2H，m)，2.34(3H，s)，2.86(2H，m)，6.39(1H，d，J＝9.8Hz)，6.89-7.49(10H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 258

Compound (282): N-(4-aminomethyl phenyl)-3-(4-chloro benzylthio-) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.34(3H，s)，3.79(2H，s)，4.28(2H，s)，6.05(1H，d，J＝15.5Hz)，6.60(2H，d，J＝8.2Hz)，7.07-7.38(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 259

Compound (283): N-(4-aminomethyl phenyl)-3-(4-chloro benzylthio-) sulfo-acryloyl imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.30(3H，s)，3.85(2H，brs)，4.06(2H，brs)，6.29(1H，brs)，6.70-7.30(14H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 260

Compound (284): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.92(3H，t J＝7.4Hz)，1.38-1.50(2H，m)，1.62-1.75(2H，m)，2.31(3H，s)，3.06(2H，t J＝7.4Hz)，6.13(1H，d，J＝15.5Hz)，6.63(2H，d，J＝8.2Hz)，6.75-7.38(8H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (285) is synthetic in the mode that is similar to embodiment 61.

Embodiment 261

Compound (285): N-(4-aminomethyl phenyl)-3-(thiophenyl) acryloyl imido acid 4-biphenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.29(3H，s)，5.95(1H，d J＝15.4Hz)，6.66(2H，d J＝8.0Hz)，7.03(2H，d J＝8.0Hz)，7.26-7.59(14H，m)，7.70(1H，d J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (286)-(320) are synthetic in the mode that is similar to embodiment 100.

Embodiment 262

Compound (286): N-(3,4-3,5-dimethylphenyl)-3-(2-fluorinated phenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.36(3H，s)，5.81(1H，d J＝12.1Hz)，6.53(1H，d J＝7.8Hz)，6.54(1H，brs)，6.96-7.03(4H，m)，7.08-7.16(4H，m)，7.23-7.27(1H，m)，7.68(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 263

Compound (287): N-(3,4-3,5-dimethylphenyl)-3-(3-fluorinated phenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.83(1H，d J＝11.9Hz)，6.53(1H，d J＝7.8Hz)，6.59(1H，brs)，6.76-6.80(1H，m)，6.83-6.87(2H，m)，6.97-7.04(4H，m)，7.23-7.33(2H，m)，7.71(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 264

Compound (288): N-(3,4-3,5-dimethylphenyl)-3-(4-fluorinated phenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.36(3H，s)，5.76(1H，d J＝12.1Hz)，6.53(1H，d J＝7.8Hz)，6.58(1H，brs)，6.97-7.03(8H，m)，7.23-7.27(1H，m)，7.67(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 265

Compound (289): 3-(2-chloro phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ³)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.36(3H，s)，5.83(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.96-7.03(6H，m)，7.07-7.13(2H，m)，7.39-7.42(1H，m)，7.66(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 266

Compound (290): 3-(3-chloro phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.82(1H，d J＝12.1Hz)，6.53(1H，d J＝7.8Hz)，6.59(1H，brs)，6.93-7.06(6H，m)，7.11-7.13(1H，m)，7.24-7.29(2H，m)，7.69(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 267

Compound (291): 3-(4-chloro phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，5.80(1H，d J＝12.1Hz)，6.53(1H，d J＝7.8Hz)，6.58(1H，brs)，6.97-7.03(6H，m)，7.23-7.31(3H，m)，7.68(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 268

Compound (292): N-(3,4-3,5-dimethylphenyl)-3-(2-methylphenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.24(3H，s)，2.36(3H，s)，5.73(1H，d J＝12.1Hz)，6.55(1H，d J＝7.8Hz)，6.60(1H，brs)，6.96-7.06(6H，m)，7.17-7.18(2H，m)，7.22-7.26(1H，m)，7.71(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 269

Compound (293): N-(3,4-3,5-dimethylphenyl)-3-(3-methylphenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.35(3H，s)，2.36(3H，s)，5.77(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.84-6.86(2H，m)，6.94-7.04(5H，m)，7.19-7.27(2H，m)，7.74(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 270

Compound (294): N-(3,4-3,5-dimethylphenyl)-3-(4-methylphenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.32(3H，s)，2.36(3H，s)，5.75(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.92-7.03(6H，m)，7.12-7.14(2H，m)，7.23-7.27(1H，m)，7.72(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 271

Compound (295): N-(3,4-3,5-dimethylphenyl)-3-(3-methoxyphenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，3.79(3H，s)，5.79(1H，d J＝12.1Hz)，6.54(1H，d J＝7.8Hz)，6.59(2H，brs)，6.64-6.70(2H，m)，6.96-7.03(4H，m)，7.22-7.27(2H，m)，7.74(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 272

Compound (296): N-(3,4-3,5-dimethylphenyl)-3-(4-methoxyphenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.36(3H，s)，3.78(3H，s)，5.72(1H，d J＝12.1Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.84-6.86(2H，m)，6.96-7.02(6H，m)，7.22-7.26(1H，m)，7.68(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 273

Compound (297): N-(3,4-3,5-dimethylphenyl)-3-(3-4-trifluoromethylphenopendant) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.85(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.98-7.04(4H，m)，7.23-7.29(3H，m)，7.39-7.41(1H，m)，7.46-7.50(1H，m)，7.72(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 274

Compound (298): 3-(4-bromo phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，5.80(1H，d J＝11.9Hz)，6.53(1H，d J＝7.8Hz)，6.58(1H，brs)，6.92-7.03(6H，m)，7.23-7.27(1H，m)，7.44-7.46(2H，m)，7.68(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 275

Compound (299): 3-(3,4-difluoro phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，5.80(1H，d J＝11.9Hz)，6.52(1H，d J＝7.8Hz)，6.58(1H，brs)，6.77-6.81(1H，m)，6.87-6.92(1H，m)，6.97-7.02(4H，m)，7.10-7.17(1H，m)，7.23-7.28(1H，m)，7.63(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 276

Compound (300): 3-(3,4-dichlorophenoxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.83(1H，d J＝11.9Hz)，6.53(1H，d J＝7.8Hz)，6.58(1H，brs)，6.90-6.93(1H，m)，6.98-7.03(4H，m)，7.16-7.17(1H，m)，7.24-7.28(1H，m)，7.39-7.41(1H，m)，7.64(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 277

Compound (301): N-(3,4-3,5-dimethylphenyl)-3-(3,4-dimethyl phenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.21(3H，s)，2.24(3H，s)，2.36(3H，s)，5.74(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.78(1H，d J＝7.8Hz)，6.82(1H，brs)，6.96-7.08(4H，m)，7.23-7.27(1H，m)，7.22-7.26(1H，m)，7.72(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 278

Compound (302): N-(3,4-3,5-dimethylphenyl)-3-(6-benzo [1,3] dioxolyl oxygen base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.36(3H，s)，5.71(1H，d J＝11.9Hz)，5.96(2H，s)，6.48-6.54(2H，m)，6.58-6.59(2H，m)，6.72-6.74(1H，m)，6.96-7.02(4H，m)，7.22-7.27(1H，m)，7.63(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 279

Compound (303): N-(3,4-3,5-dimethylphenyl)-3-(4-methoxycarbonyl phenoxy group) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，3.91(3H，s)，5.88(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.98-7.04(4H，m)，7.07-7.10(2H，m)，7.24-7.28(1H，m)，7.78(1H，d J＝11.9Hz)，8.03-8.05(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 280

Compound (304): 3-(4-ethanoyl phenoxy group)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，2.58(3H，s)，5.90(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.98-7.04(4H，m)，7.10-7.12(2H，m)，7.24-7.29(1H，m)，7.79(1H，d J＝11.9Hz)，7.97-7.99(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 281

Compound (305): N-(3,4-3,5-dimethylphenyl)-3-(4-cyano-benzene oxygen) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.92(1H，d J＝11.9Hz)，6.53(1H，d J＝7.8Hz)，6.58(1H，brs)，6.99-7.03(4H，m)，7.12-7.15(2H，m)，7.24-7.29(1H，m)，7.65-7.67(2H，m)7.79(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 282

Compound (306): N-(3,4-3,5-dimethylphenyl)-3-(4-nitrophenoxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(3H，s)，2.22(3H，s)，2.38(3H，s)，5.96(1H，d J＝11.9Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.99-7.04(4H，m)，7.15-7.17(2H，m)，7.25-7.27(2H，m)，7.77(1H，d J＝11.9Hz)，8.25-8.27(1H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 283

Compound (307): N-(3,4-3,5-dimethylphenyl)-3-(4-methylthio group phenoxy group) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.36(3H，s)，2.46(3H，s)，5.77(1H，d J＝12.1Hz)，6.54(1H，d J＝7.8Hz)，6.59(1H，brs)，6.97-7.03(6H，m)，7.23-7.27(3H，m)，7.70(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 284

Compound (308): N-(3,4-3,5-dimethylphenyl)-3-(4-phenyl phenoxy group) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(3H，s)，2.21(3H，s)，2.37(3H，s)，5.83(1H，d J＝11.9Hz)，6.56(1H，d J＝7.8Hz)，6.61(1H，brs)，6.99-7.05(4H，m)，7.11-7.13(2H，m)，7.24-7.26(1H，m)，7.34-7.36(1H，m)，7.41-7.45(2H，m)，7.53-7.57(4H，m)，7.80(1H，d J＝11.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 285

Compound (309): 3-(2-fluorinated benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，4.88(2H，s)，5.43(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.56(1H，brs)，6.93-7.01(5H，m)，7.11-7.16(2H，m)，7.28-7.36(2H，m)，7.61(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 286

Compound (310): 3-(3-fluorinated benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.35(3H，s)，4.80(2H，s)，5.40(1H，d J＝12.4Hz)，6.49(1H，d J＝7.8Hz)，6.56(1H，brs)，6.95-7.01(7H，m)，7.22-7.24(1H，m)，7.29-7.32(1H，m)，7.60(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 287

Compound (311): 3-(4-fluorinated benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(6H，s)，2.35(3H，s)，4.77(2H，s)，5.39(1H，d J＝12.4Hz)，6.49(1H，d J＝7.8Hz)，6.55(1H，brs)，6.95-7.06(6H，m)，7.22-7.28(3H，m)，7.59(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 288

Compound (312): 3-(2-chloro benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，4.94(2H，s)，5.45(1H，d J＝12.1Hz)，6.51(1H，d J＝8.3Hz)，6.56(1H，brs)，6.91-7.01(3H，m)，7.19-7.29(4H，m)，7.34-7.49(2H，m)，7.62(1H，d J＝12.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 289

Compound (313): 3-(3-chloro benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.35(3H，s)，4.78(2H，s)，5.39(1H，d J＝12.4Hz)，6.49(1H，d J＝7.8Hz)，6.56(1H，brs)，6.91-7.00(4H，m)，7.22-7.32(5H，m)，7.59(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 290

Compound (314): 3-(4-chloro benzyloxy)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.35(3H，s)，4.77(2H，s)，5.38(1H，d J＝12.4Hz)，6.49(1H，d J＝7.8Hz)，6.55(1H，brs)，6.95-7.00(3H，m)，7.20-7.24(3H，m)，7.29-7.34(3H，m)，7.59(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 291

Compound (315): N-(3,4-3,5-dimethylphenyl)-3-(2-methyl benzyloxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.29(3H，s)，2.35(3H，s)，4.81(2H，s)，5.42(1H，d J＝12.4Hz)，6.52(1H，d J＝7.8Hz)，6.57(1H，brs)，6.87-7.01(4H，m)，7.17-7.24(5H，m)，7.61(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 292

Compound (316): N-(3,4-3,5-dimethylphenyl)-3-(3-methyl benzyloxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(6H，s)，4.77(2H，s)，5.41(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.57(1H，brs)，6.91-7.00(3H，m)，7.07-7.15(3H，m)，7.21-7.26(3H，m)，7.61(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 293

Compound (317): N-(3,4-3,5-dimethylphenyl)-3-(4-methyl benzyloxy) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(6H，s)，4.76(2H，s)，5.40(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.56(1H，brs)，6.94-7.00(4H，m)，7.16-7.18(3H，m)，7.20-7.23(2H，m)，7.60(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 294

Compound (318): N-(3,4-3,5-dimethylphenyl)-3-(2-methoxyl group benzyloxy base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，3.79(3H，s)，4.89(2H，s)，5.41(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.56(1H，brs)，6.86-6.88(1H，m)，6.94-7.00(5H，m)，7.21-7.33(3H，m)，7.62(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 295

Compound (319): N-(3,4-3,5-dimethylphenyl)-3-(3-methoxyl group benzyloxy base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.20(3H，s)，2.35(3H，s)，3.80(3H，s)，4.79(2H，s)，5.41(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.56(1H，brs)，6.83-6.88(3H，m)，6.95-7.00(4H，m)，7.21-7.29(2H，m)，7.61(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 296

Compound (320): N-(3,4-3,5-dimethylphenyl)-3-(4-methoxyl group benzyloxy base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，3.81(3H，s)，4.74(2H，s)，5.39(1H，d J＝12.4Hz)，6.50(1H，d J＝7.8Hz)，6.56(1H，brs)，6.87-6.89(2H，m)，6.95-7.00(4H，m)，7.20-7.23(3H，m)，7.60(1H，d J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (321)-(324) are synthetic in the mode that is similar to embodiment 161.

Embodiment 297

Compound (321): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.5Hz)，1.93(1H，sept.J＝6.7Hz)，2.31(3H，s)，2.99(2H，d，J＝6.8Hz)，6.12(1H，d，J＝15.5Hz)，6.62(2H，d，J＝8.0Hz)，7.06(2H，d，J＝8.0Hz)，7.29-7.39(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 298

Compound (322): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.97(6H，brs)，1.57(2H，s)，2.34(3H，s)，2.77(1H，brs)，6.38(1H，d，J＝9.7Hz)，6.91-7.49(10H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 299

Compound (323): N-phenyl-3-(cyclohexyl sulfenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.23-2.10(20H，m)，2.84-2.89(1H，m)，3.76-3.81(1H，m)，6.03(1H，d，J＝15.7Hz)，6.75-7.29(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 300

Compound (324): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 1-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01(3H，t J＝7.4Hz)，1.36(3H，d，J＝7.0Hz)，1.63-1.74(2H，m)，2.34(3H，s)，3.79(1H，m)，6.12(1H，d，J＝15.5Hz)，6.63(2H，d，J＝8.2Hz)，7.06(2H，d，J＝8.0Hz)，7.29-7.38(6H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (325) is synthetic in the mode that is similar to embodiment 37.

Embodiment 301

Compound (325): N-(3-xenyl)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.70(1H，d，J＝11.8Hz)，6.80-7.78(19H，m)，7.85(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 302

Compound (326): N-phenoxy group-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

N-phenoxy group-3-(thiophenyl) acrylamide (0.50g) is suspended in the toluene (5ml), then ice-cooled lower, to wherein adding phosphorus pentachloride (0.42g) and under identical temperature, stirring 2.5 hours.The concentrating under reduced pressure reaction mixture.Make residue be dissolved in ethanol (15ml).Ice-cooled lower, join the sodium salt (0.73g) of thiophenol in this solution and reflux 2.5 hours.T-butyl methyl ether (100ml) is joined in the reaction mixture, sequentially wash with 1N aqueous sodium hydroxide solution, water and saturated sodium-chloride water solution, dry through anhydrous sodium chlorate, filtering inorganic salt and concentrating under reduced pressure. the standby type high performance liquid chromatography (hexane: ethyl acetate=30: 1) purifying of compacting in the residue warp, obtain N-(phenoxy group)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester (0.14g), be yellow oil.

¹H-NMR(CDCl ₃)δ(ppm)：5.45(1H，d，J＝15.0Hz)，7.00-7.04(1H，m)，7.18-7.46(15H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (327) is with synthetic with embodiment 302 similar modes.

Embodiment 303

Compound (327): N-(phenyl amino)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：6.07(0.41H，d，J＝9.0Hz)，6.55(0.41H，d，J＝9.0Hz)，6.68(0.59H，d，J＝16.3Hz)，6.88-6.94(1H，m)，7.00(0.59H，d，J＝16.3Hz)，7.03-7.07(1H，m)，7.19-7.37(12H，m)7.52-7.54(1H，m)，8.68(0.41H，brs，NH)，8.74(0.59H，brs，NH)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (328)-(330) are synthetic in the mode that is similar to embodiment 176.

Embodiment 304

Compound (328): N-(4-aminomethyl phenyl)-3-(thiophenyl) acryloyl imido acid isopropylidene (Isopropyridene) amino ester

¹H-NMR(CDCl ₃)δ(ppm)：2.06(3H，s)，2.11(3H，s)，2.30(3H，s)，5.80(1H，d J＝15.4Hz)，6.73(2H，d J＝7.8Hz)，7.03(2H，d J＝8.5Hz)，7.30-7.52(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 305

Compound (329): N-(4-aminomethyl phenyl)-3-(thiophenyl) acryloyl imido acid 2,3,5, the 6-tetrafluoro is for phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.29(3H，s)，5.86(1H，d J＝15.2Hz)，6.64(2H，d J＝8.2Hz)，6.90-6.95(1H，m)，7.04(2H，d J＝7.7Hz)，7.32-7.38(3H，m)，7.43-7.46(2H，m)，7.74(1H，d J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 306

Compound (330): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2,6-dichlorophenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.28(0.39H，s)，2.31(1.86H，s)，2.36(0.75H，s)，5.56(0.62H，d J＝14.9Hz)，5.67(0.25H，d J＝10.0Hz)，6.10(0.13H，d J＝15.4Hz)，6.57(0.26H，d J＝7.3Hz)，6.82-7.57(12.74H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (331) and (332) are synthetic in the mode that is similar to embodiment 100.

Embodiment 307

Compound (331): 3-cyclohexyl sulfenyl-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.90(8H，m)，2.19(6H，s)，2.36(3H，s)，2.88-2.99(1H，brs)，6.51(1H，d，J＝8.4Hz)，6.57(1H，s)，6.92-7.02(1H，m)，7.20-7.28(1H，m)，7.55(1H，d，J＝15.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 308

Compound (332): N-(3,4-3,5-dimethylphenyl)-3-(4-4-trifluoromethylphenopendant) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(6H，s)，2.37(3H，s)，5.89(1H，d，J＝11.8Hz)，6.54(1H，d，J＝8.0Hz)，6.59(1H，s)，6.59-7.07(4H，m)，7.14(2H，d，J＝8.5Hz)，7.23-7.30(1H，m)，7.62(2H，d，J＝8.7Hz)，7.76(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (333)-(338) are synthetic in the mode that is similar to embodiment 161.

Embodiment 309

Compound (333): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid cyclopentyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.59-1.73(6H，m)，2.16(2H，brs)，2.31(3H，s)，3.95(1H，q，J＝7.0Hz)，6.12(1H，d，J＝15.6Hz)，6.63(2H，d，J＝8.0Hz)，7.06(2H，d，J＝8.0Hz)，7.25-7.52(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 310

Compound (334): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid cyclopentyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.57-1.71(6H，m)，2.07(2H，brs)，2.34(3H，s)，3.63(1H，brs)，6.47(1H，d，J＝10.1Hz)，6.90(2H，d，J＝7.7Hz)，6.99(1H，d，J＝9.9Hz)，7.15(2H，d，J＝7.7Hz)，7.30-7.51(5H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 311

Compound (335): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-methyl-benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.31(3H，s)，2.32(3H，s)，4.27(2H，s)，6.13(1H，d，J＝15.7Hz)，6.65(2H，d，J＝8.2Hz)，7.07-7.35(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 312

Compound (336): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-methyl-benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(6H，s)，4.11(2H，brs)，6.38(1H，d，J＝10.4Hz)，6.91-7.47(14H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 313

Compound (337): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-chloro benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，4.25(2H，s)，6.11(1H，d，J＝15.5Hz)，6.62(2H，d，J＝8.2Hz)，7.08(2H，d，J＝8.0Hz)，7.24-7.36(10H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 314

Compound (338): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2,4-dichloro benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，4.37(2H，s)，6.09(1H，d，J＝15.5Hz)，6.62(2H，d，J＝8.2Hz)，7.07-7.48(11H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (339)-(340) are synthetic in the mode that is similar to embodiment 37.

Embodiment 315

Compound (339): N-(4-benzoylphenyl)-3-phenoxy group acryloyl imido acid phenylester

The stereochemistry of-CH=CH-key is E.

Embodiment 316

Compound (340): N-(4-acetylphenyl)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.57(3H，s)，5.63(0.75H，d，J＝12.0Hz)，5.68(0.25H，d，J＝12.0Hz)，6.85-7.90(14H，m)，7.58(0.25H，d，J＝12.0Hz)，7.84(0.75H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (341)-(370) are synthetic in the mode that is similar to embodiment 161.

Embodiment 317

Compound (341): 3-(2-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00-1.25(5H，m)，1.57-1.86(6H，m)，2.31(3H，s)，2.99(2H，d J＝6.8Hz)，6.05(1H，d J＝15.7Hz)，6.61(2H，dJ＝8.1Hz)，7.04-7.40(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 318

Compound (343): 3-(3-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.59-1.87(6H，m)，2.32(3H，s)，3.00(2H，d J＝6.8Hz)，6.16(1H，d J＝15.4Hz)，6.63(2H，dJ＝8.3Hz)，6.96-7.33(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 319

Compound (345): 3-(2-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.66-1.87(6H，m)，2.31(3H，s)，3.00(2H，d J＝6.6Hz)，6.15(1H，d J＝15.4Hz)，6.63(2H，dJ＝8.3Hz)，7.06(2H，d J＝8.1Hz)，7.21-7.41(5H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 320

Compound (347): 3-(3-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.66-1.87(6H，m)，2.31(3H，s)，3.00(2H，d J＝6.8Hz)，6.13(1H，d J＝15.7Hz)，6.62(2H，dJ＝8.1Hz)，7.07(2H，d J＝7.8Hz)，7.23-7.36(5H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 321

Compound (349): 3-(4-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.66-1.86(6H，m)，2.31(3H，s)，3.00(2H，d J＝6.8Hz)，6.04(1H，d J＝15.7Hz)，6.59(2H，dJ＝8.1Hz)，7.06(2H，d J＝7.8Hz)，7.21-7.29(5H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 322

Compound (351): 3-(3-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.63-1.87(6H，m)，2.32(3H，s)，3.00(2H，d J＝6.8Hz)，6.13(1H，d J＝15.4Hz)，6.62(2H，dJ＝8.1Hz)，7.08(2H，d J＝8.1Hz)，7.18(1H，t J＝7.8Hz)，7.26-7.31(2H，m)，7.41(1H，d J＝7.8Hz)，7.52(1H，s)。

The stereochemistry of-CH=CH-key is E.

Embodiment 323

Compound (353): 3-(4-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.66-1.86(6H，m)，2.33(3H，s)，2.99(2H，d J＝6.6Hz)，6.06(1H，d J＝15.7Hz)，6.59(2H，dJ＝8.1Hz)，7.06(2H，d J＝8.1Hz)，7.21-7.44(5H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 324

Compound (354): N-(4-aminomethyl phenyl)-3-(4-nitrophenylsulfenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.02-1.27(5H，m)，1.64-1.88(6H，m)，2.33(3H，s)，3.03(2H，d J＝6.8Hz)，6.37(1H，d J＝15.7Hz)，6.65(2H，dJ＝8.1Hz)，7.10(2H，d J＝8.1Hz)，7.33(1H，dJ＝15.7Hz)，7.45(2H，dJ＝8.8Hz)，8.17(2H，d J＝8.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 325

Compound (356): N-(4-aminomethyl phenyl)-3-(2-methylbenzene sulfenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.25(5H，m)，1.62-1.86(6H，m)，2.30(3H，s)，2.32(3H，s)，2.98(2H，d J＝6.8Hz)，5.88(1H，d J＝15.4Hz)，6.57(2H，d J＝8.1Hz)，7.02(2H，d J＝7.8Hz)，7.12-7.29(4H，m)，7.35(1H，d J＝7.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 326

Compound (357): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.25(5H，m)，1.60-1.85(6H，m)，2.31(3H，s)，2.33(3H，s)，2.98(2H，d J＝6.8Hz)，6.03(1H，d J＝15.4Hz)，6.60(2H，d J＝8.1Hz)，7.04(2H，d J＝8.1Hz)，7.09-7.34(4H，m)，7.38(1H，d J＝8.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 327

Compound (359): N-(4-aminomethyl phenyl)-3-(4-trifluoromethyl thiophenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.66-1.87(6H，m)，2.32(3H，s)，3.01(2H，d J＝6.8Hz)，6.21(1H，d J＝15.7Hz)，6.62(2H，dJ＝8.3Hz)，7.07(2H，d J＝7.8Hz)，7.33(1H，d J＝15.7Hz)，7.45(2H，dJ＝8.1Hz)，7.56(2H，d J＝8.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 328

Compound (361): 3-(3-anisole sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00-1.25(5H，m)，1.66-1.86(6H，m)，2.31(3H，s)，2.99(2H，d J＝6.8Hz)，3.79(3H，s)，6.14(1H，dJ＝15.7Hz)，6.62(2H，d J＝8.1Hz)，6.83(1H，d J＝8.3Hz)，6.95(1H，dJ＝7.6Hz)，7.06(2H，d J＝8.1Hz)，7.23(2H，m)，7.37(1H，d J＝15.7Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 329

Compound (363): 3-(4-anisole sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.02-1.21(5H，m)，1.65-1.85(6H，m)，2.31(3H，s)，2.97(2H，d J＝6.6Hz)，3.79(3H，s)，5.92(1H，d J＝15.4Hz)，6.58(2H，d J＝8.3Hz)，6.82(2H，d J＝8.8Hz)，7.03(2H，d J＝8.1Hz)，7.26-7.30(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 330

Compound (365): 3-(2,4 dichloro benzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.26(5H，m)，1.70-1.84(6H，m)，2.33(3H，s)，3.00(2H，d J＝6.8Hz)，6.05(1H，d J＝15.4Hz)，6.60(2H，dJ＝8.1Hz)，7.02(2H，d J＝8.1Hz)，7.18-7.40(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 331

Compound (366): 3-(3,5-dichlorobenzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.05-1.26(5H，m)，1.63-1.84(6H，m)，2.34(3H，s)，3.01(2H，d J＝6.8Hz)，6.17(1H，d J＝15.4Hz)，6.63(2H，dJ＝8.1Hz)，7.08-7.23(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 332

Compound (367): 3-(2,4-dimethyl benzene sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00-1.25(5H，m)，1.60-1.85(6H，m)，2.28(6H，s)，2.30(3H，s)，2.97(2H，d J＝6.8Hz)，5.76(1H，d J＝15.4Hz)，6.55(2H，d J＝8.3Hz)，6.92-7.26(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 333

Compound (368): N-(4-aminomethyl phenyl)-3-(2-pyridyl sulfenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.03-1.28(5H，m)，1.64-1.87(6H，m)，2.33(3H，s)，3.03(2H，d J＝6.8Hz)，6.43(1H，d J＝15.9Hz)，6.68(2H，d J＝8.1Hz)，7.10(3H，d J＝8.1Hz)，7.20(1H，d J＝7.8Hz)，7.56(1H，d J＝7.8Hz)，8.18(1H，d J＝15.9Hz)，8.54(1H，d J＝7.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 334

Compound (370): N-(4-aminomethyl phenyl)-3-(2-pyrimidine-based sulfur-base)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.04-1.26(5H，m)，1.64-1.88(6H，m)，2.33(3H，s)，3.04(2H，d J＝6.8Hz)，6.46(1H，d J＝16.4Hz)，6.68(2H，dJ＝8.1Hz)，7.08(1H，t J＝4.8Hz)，7.11(2H，d J＝8.1Hz)，8.28(1H，dJ＝16.4Hz)，8.60(2H，d J＝5.1Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (371)-(384) are synthetic in the mode that is similar to embodiment 223.

Embodiment 335

Compound (371): 3-benzylthio--N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.25(5H，m)，1.66-1.86(6H，m)，2.32(3H，s)，2.97(2H，d J＝6.8Hz)，3.85(2H，s)，6.10(1H，d J＝15.4Hz)，6.61(2H，d J＝8.3Hz)，7.07(2H，d J＝8.1Hz)，7.19(2H，d J＝7.8Hz)，7.25-7.29(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 336

Compound (373): 3-(4-fluoro benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.02-1.25(5H，m)，1.66-1.85(6H，m)，2.33(3H，s)，2.97(2H，d J＝6.8Hz)，3.82(2H，s)，6.06(1H，d J＝15.4Hz)，6.59(2H，d J＝8.1Hz)，6.95(2H，t J＝8.7Hz)7.06(2H，d J＝7.8Hz)，7.12-7.16(2H，m)，7.23(1H，d J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 337

Compound (375): 3-(4-methyl benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.02-1.26(5H，m)，1.70-1.83(6H，m)，2.32(3H，s)，2.33(3H，s)，2.97(2H，d J＝6.8Hz)，3.81(2H，s)，6.10(1H，d J＝15.4Hz)，6.61(2H，d J＝8.1Hz)，7.07-7.08(6H，m)，7.27(1H，dJ＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 338

Compound (377): 3-(4-chloro benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.02-1.25(5H，m)，1.70-1.85(6H，m)，2.33(3H，s)，2.97(2H，d J＝6.6Hz)，3.81(2H，s)，6.04(1H，d J＝15.4Hz)，6.58(2H，d J＝8.1Hz)，7.06(2H，d J＝8.1Hz)，7.10(2H，d J＝8.3Hz)，7.14-7.30(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 339

Compound (379): 3-(2,4-benzyl dichloride sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.01-1.23(5H，m)，1.70-1.86(6H，m)，2.32(3H，s)，2.98(2H，d J＝6.8Hz)，3.92(2H，s)，6.03(1H，d J＝15.4Hz)，6.57(2H，d J＝8.1Hz)，7.04(2H，d J＝8.1Hz)，7.19-7.35(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 340

Compound (381): 3-(2-methyl benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00-1.26(5H，m)，1.66-1.86(6H，m)，2.30(3H，s)，2.31(3H，s)，2.98(2H，d J＝6.8Hz)，3.85(2H，s)，6.10(1H，d J＝15.7Hz)，6.63(2H，d J＝8.1Hz)，7.06(2H，dJ＝8.1Hz)7.13-7.18(4H，m)，7.30(1H，d J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 341

Compound (383): 3-(4-methoxybenzyl sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00-1.25(5H，m)，1.66-1.86(6H，m)，2.32(3H，s)，2.97(2H，d J＝6.8Hz)，3.80(3H，s)，3.81(2H，s)，6.10(1H，d J＝15.4Hz)，6.62(2H，d J＝8.3Hz)，6.81(2H，d J＝8.8Hz)，7.07(2H，d J＝8.1Hz)，7.11(2H，d J＝8.6Hz)，7.27(1H，d J＝15.7Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (385) is with synthetic with embodiment 176 similar modes.

Embodiment 342

Compound (385): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 1-phenyl ethidine amino ester

¹H-NMR(CDCl ₃)δ(ppm)：2.17(0.96H，s)，2.31(3H，s)，2.45(2.04H，s)，5.88(0.83H，d J＝15.4Hz)，6.59(0.17H，d J＝15.1Hz)，6.76(2H，dJ＝8.0Hz)，6.98-7.08(3H，m)，7.32-7.54(8H，m)，7.74-7.78(2H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (386) is with synthetic with embodiment 161 similar modes.

Embodiment 343

Compound (386): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2-phenylethylester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(3H，s)，2.98(2H，t J＝7.7Hz)，3.30(2H，t J＝7.7Hz)，6.14(1H，d，J＝15.6Hz)，6.64(2H，d，J＝8.0Hz)，7.07(2H，d，J＝8.0Hz)，7.18-7.37(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 344

Compound (387): N-ethoxy carbonyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

Make N-ethoxy carbonyl-3-(thiophenyl) acrylamide (1.20g) be dissolved in acetonitrile (30ml), then to wherein adding carbon tetrabromide (2.83g) and triphenyl phosphine (2.23g) and reflux 3 hours.The concentrating under reduced pressure reaction mixture.Residue is through silica gel column chromatography (hexane: ethyl acetate 20: 1), obtain faint yellow oily thing.Make it be dissolved in DMF (10ml), then ice-cooled lower, stirred 2 hours to the sodium salt that wherein adds thiophenol (0.63g) and under room temperature.T-butyl methyl ether (100ml) is joined in the reaction mixture, sequentially wash with 1N aqueous sodium hydroxide solution, water and saturated sodium-chloride water solution, dry through anhydrous sodium chlorate, filtering inorganic salt and concentrating under reduced pressure.The standby type high performance liquid chromatography purifying of compacting obtains N-ethoxy carbonyl-3-(thiophenyl) sulfo-acryloyl imido acid phenylester (0.40g) in the residue warp, is faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：1.28(2.3H，t，J＝7.2Hz)，1.40(0.70H，t，J＝7.1Hz)，4.15(1.5H，q，J＝7.2Hz)，4.30(0.50H，q，J＝7.1Hz)，5.67(0.75H，d，J＝14.5Hz)，5.82(0.25H，d，J＝10.1Hz)，7.00(0.25H，d，J＝10.1Hz)，7.29-7.58(10H，m)，7.78(0.75H，d，J＝14.5Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (388) and (389) are synthetic in the mode that is similar to embodiment 176.

Embodiment 345

Compound (388): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 3-methyl-2-butene base ester

¹H-NMR(CDCl ₃)δ(ppm)：1.71(3H，s)，1.73(3H，s)，2.32(3H，s)，3.71(2H，d，J＝8.0Hz)，5.32(1H，t J＝8.0Hz)，6.13(1H，d，J＝15.4Hz)，6.64(2H，d，J＝8.3Hz)，7.07(2H，d，J＝7.8Hz)，7.28-7.37(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 346

Compound (389): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 3,3-two chloro-2-propenyl esters

¹H-NMR(CDCl ₃)xδ(ppm)：2.32(3H，s)，3.80(2H，d，J＝7.7Hz)，6.11-6.15(2H，m)，6.64(2H，d，J＝8.2Hz)，7.08(2H，d，J＝8.0Hz)，7.30-7.38(6H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (390) is with synthetic with embodiment 100 similar modes.

Embodiment 347

Compound (390): N-(3,4-3,5-dimethylphenyl)-3-(cyclohexyl oxygen base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.92(10H，m)，2.18(6H，s)，2.35(3H，s)，3.77-3.89(1H，m)，5.37(1H，d，J＝12.0Hz)，6.48-6.58(2H，m)，6.92-7.02(4H，m)，7.20-7.27(1H，m)，7.48(1H，d，J＝12.2Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (391) is synthetic in the mode that is similar to embodiment 37.

Embodiment 348

Compound (391): N-(4-methoxycarbonyl phenyl)-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.79(3H，s)，5.64(1H，d，J＝12.0Hz)，6.81-7.36(12H，m)，7.82(1H，d，J＝12.0Hz)，7.94-7.96(2H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (392) to (418) is synthetic in the mode that is similar to embodiment 161.

Embodiment 349

Compound (392): 3-(2-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d J＝7.1Hz)，2.32(3H，s)，5.00(1H，q J＝7.1Hz)，6.02(1H，d J＝15.4Hz)，6.60(2H，d J＝8.1Hz)，7.06(2H，d J＝8.1Hz)，7.18(1H，d J＝15.4Hz)，7.23-7.26(2H，m)，7.29-7.37(5H，m)，7.41-7.42(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 350

Compound (393): 3-(3-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d J＝7.3Hz)，2.32(3H，s)，5.02(1H，q J＝7.3Hz)，6.12(1H，d J＝15.9Hz)，6.61(2H，d J＝8.3Hz)，6.94-6.99(1H，m)，7.03-7.06(3H，m)，7.08(2H，d J＝8.3Hz)，7.25(1H，d J＝15.9Hz)，7.29-7.33(3H，m)，7.41-7.43(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 351

Compound (394): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d J＝7.1Hz)，2.32(3H，s)，5.00(1H，q J＝7.1Hz)，5.93(1H，d J＝15.4Hz)，6.57(2H，d J＝8.1Hz)，6.95-7.03(3H，m)，7.05(2H，d J＝8.1Hz)，7.19(1H，d J＝15.4Hz)，7.29-7.32(4H，m)，7.40-7.42(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 352

Compound (396): 3-(2-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d J＝7.1Hz)，2.32(3H，s)，5.02(1H，q J＝7.1Hz)，6.12(1H，d J＝15.4Hz)，6.62(2H，d J＝8.3Hz)，7.06-7.08(2H，m)，7.19-7.23(4H，m)，7.29-7.38(4H，m)，7.42-7.43(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 353

Compound (397): 3-(3-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d J＝7.1Hz)，2.32(3H，s)，5.02(1H，q J＝7.1Hz)，6.09(1H，d J＝15.7Hz)，6.61(2H，d J＝8.1Hz)，7.08(2H，d J＝8.1Hz)，7.20-7.24(4H，m)，7.29-7.33(4H，m)，7.41-7.43(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 354

Compound (398): 3-(4-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d J＝7.1Hz)，2.33(3H，s)，5.01(1H，q J＝7.1Hz)，6.01(1H，d J＝15.7Hz)，6.58(2H，d J＝8.3Hz)，7.06(2H，d J＝8.3Hz)，7.14-7.23(4H，m)，7.29-7.33(4H，m)，7.41-7.42(2H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 355

Compound (400): 3-(3-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d J＝7.1Hz)，2.33(3H，s)，5.02(1H，q J＝7.1Hz)，6.09(1H，d J＝15.4Hz)，6.60(2H，d J＝8.1Hz)，7.07-7.24(5H，m)，7.29-7.33(3H，m)，7.39-7.43(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 356

Compound (402): 3-(4-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d J＝7.1Hz)，2.34(3H，s)，5.01(1H，q J＝7.1Hz)，6.03(1H，d J＝15.7Hz)，6.58(2H，d J＝8.1Hz)，7.06-7.19(2H，m)，7.22-7.24(3H，m)，7.29-7.34(4H，m)，7.40-7.42(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 357

Compound (404): N-(4-aminomethyl phenyl)-3-(4-nitrophenylsulfenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.76(3H，d，J＝7.0Hz)，2.33(3H，s)，5.03(1H，q，J＝7.0Hz)，6.32(1H，d，J＝15.4Hz)，6.63(2H，d，J＝8,0Hz)，7.11(2H，d，J＝7.8Hz)，7.21-7.47(8H，m)，8.15(2H，d，J＝8.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 358

Compound (405): N-(4-aminomethyl phenyl)-3-(2-methylbenzene sulfenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d，J＝7.0Hz)，2.30(3H，s)，2.31(3H，s)，5.00(1H，q，J＝7.0Hz)，5.85(1H，d，J＝15.4Hz)，6.56(2H，d，J＝8,3Hz)，7.00-7.43(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 359

Compound (407): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d，J＝7.0Hz)，2.32(6H，s)，5.00(1H，q，J＝7.0Hz)，5.99(1H，d，J＝15.4Hz)，6.59(2H，d，J＝8,0Hz)，7.01-7.44(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 360

Compound (408): N-(4-aminomethyl phenyl)-3-(4-trifluoromethyl thiophenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.74(3H，d，J＝7.0Hz)，2.32(3H，s)，5.02(1H，q，J＝7.0Hz)，6.18(1H，d，J＝15.6Hz)，6.60(2H，d，J＝8,0Hz)，7.03-7.70(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 361

Compound (409): 3-(3-anisole sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d，J＝7.0Hz)，2.32(3H，s)，3.77(3H，s)，5.02(1H，q，J＝7.0Hz)，6.10(1H，d，J＝15.4Hz)，6.61(2H，d，J＝8,0Hz)，6.73-7.45(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 362

Compound (410): 3-(4-anisole sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d，J＝7.0Hz)，2.32(3H，s)，3.78(3H，s)，4.99(1H，q，J＝7.0Hz)，5.89(1H，d，J＝15.6Hz)，6.57(2H，d，J＝8,0Hz)，6.80(2H，d，J＝8.8Hz)，7.00-7.45(10H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 363

Compound (411): 3-(2,4 dichloro benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d，J＝7.0Hz)，2.33(3H，s)，5.02(1H，q，J＝7.0Hz)，6.02(1H，d，J＝15.6Hz)，6.59(2H，d，J＝8,0Hz)，7.03-7.46(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 364

Compound (412): 3-(3,4-dichlorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d，J＝7.0Hz)，2.33(3H，s)，5.01(1H，q，J＝7.0Hz)，6.04(1H，d，J＝15.6Hz)，6.58(2H，d，J＝8,3Hz)，6.99-7.57(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 365

Compound (413): 3-(3,5-dichlorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.75(3H，d，J＝7.0Hz)，2.33(3H，d)，5.02(1H，q，J＝7.0Hz)，6.12(1H，d，J＝15.6Hz)，6.61(2H，d，J＝8,3Hz)，7.05-7.56(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 366

Compound (415): 3-(2,4-dimethyl benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d，J＝7.0Hz)，2.25(3H，s)，2.27(3H，s)，2.32(3H，s)，4.99(1H，q，J＝7.0Hz)，5.73(1H，d，J＝15.4Hz)，6.53(2H，d，J＝8.0Hz)，6.88-7.45(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 367

Compound (416): N-(4-aminomethyl phenyl)-3-(2-pyridyl sulfenyl) sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.77(3H，d J＝7.1Hz)，2.33(3H，s)，5.05(1H，q J＝7.1Hz)，6.39(1H，d J＝16.2Hz)，6.67(2H，d J＝8.1Hz)，7.11(2H，d J＝7.8Hz)，7.17(1H，d J＝8.1Hz)，7.25(1H，d J＝7.3Hz)，7.32(3H，t J＝7.5Hz)，7.46(2H，d J＝7.1Hz)，7.54(1H，t J＝7.7Hz)，8.12(1H，dJ＝16.2Hz)，8.51(1H，d J＝4.8Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 368

Compound (418): N-(4-aminomethyl phenyl)-3-(2-pyrimidine-based sulfur-base)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.78(3H，d J＝7.1Hz)，2.34(3H，s)，5.06(1H，q J＝7.1Hz)，6.42(1H，d J＝16.4Hz)，6.67(2H，d J＝8.1Hz)，7.06(1H，t J＝4.9Hz)，7.12(2H，d J＝7.8Hz)，7.26(1H，d J＝7.3Hz)，7.33(2H，t J＝7.5Hz)，7.47(2H，dJ＝7.1Hz)，8.22(1H，d J＝16.4Hz)，8.57(2H，d J＝4.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (419)-(425) are synthetic in the mode that is similar to embodiment 223.

Embodiment 369

Compound (419): 3-benzylthio--N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.33(3H，s)，3.81(2H，s)，4.99(1H，q J＝7.1Hz)，6.06(1H，d J＝15.4Hz)，6.58(2H，dJ＝8.3Hz)，7.07(2H，d J＝7.8Hz)，7.15-7.32(9H，m)，7.41(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 370

Compound (420): 3-(4-fluoro benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.33(3H，s)，3.78(2H，s)，4.99(1H，q J＝7.1Hz)，6.02(1H，d J＝15.4Hz)，6.57(2H，dJ＝8.1Hz)，6.93(2H，t 8.6Hz)，7.06-7.14(3H，m)，7.16(1H，d J＝15.7Hz)，7.24(1H，d J＝7.3Hz)，7.30(3H，t J＝7.5Hz)，7.41(2H，dJ＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 371

Compound (421): 3-(4-methyl benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.32(3H，s)，2.33(3H，s)，3.78(2H，s)，4.99(1H，q J＝7.3Hz)，6.05(1H，d J＝15.4Hz)，6.59(2H，d J＝8.3Hz)，7.06(5H，m)，7.20(1H，d J＝15.4Hz)，7.24(1H，d J＝7.3Hz)，7.30(3H，t J＝7.3Hz)，7.41(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 372

Compound (422): 3-(4-chloro benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.34(3H，s)，3.77(2H，s)，4.99(1H，q J＝7.1Hz)，6.00(1H，d J＝15.4Hz)，6.56(2H，dJ＝8.3Hz)，7.07(3H，d J＝8.3Hz)，7.14(1H，d J＝15.7Hz)，7.21(2H，d8.3Hz)，7.24(1H，d J＝7.3Hz)，7.30(3H，t J＝7.3Hz)，7.41(2H，dJ＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 373

Compound (423): 3-(2,4-benzyl dichloride sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.33(3H，s)，3.89(2H，s)，4.99(1H，q J＝7.1Hz)，5.98(1H，d J＝15.7Hz)，6.55(2H，dJ＝8.3Hz)，7.05(2H，d J＝8.1Hz)，7.16(3H，t J＝7.8Hz)，7.23-7.33(4H，m)，7.41(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 374

Compound (424): 3-(2-methyl benzylthio-)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d J＝7.3Hz)，2.27(3H，s)，2.32(3H，s)，3.81(2H，s)，5.00(1H，q J＝7.3Hz)，6.05(1H，d J＝15.7Hz)，6.60(2H，d J＝8.1Hz)，7.07(2H，d J＝8.1Hz)，7.13-7.25(5H，m)，7.31(3H，t J＝7.5Hz)，7.42(2H，d J＝7.1Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 375

Compound (425): 3-(4-methoxybenzyl sulfenyl)-N-(4-aminomethyl phenyl)-sulfo-acryloyl imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.72(3H，d J＝7.1Hz)，2.33(3H，s)，3.77(2H，s)，3.79(3H，s)，4.99(1H，q J＝7.1Hz)，6.05(1H，d J＝15.4Hz)，6.60(2H，d J＝8.1Hz)，6.79(2H，d J＝8.6Hz)，7.07-7.25(5H，m)，7.30(3H，t J＝7.5Hz)，7.41(2H，dJ＝7.3Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (426) and (427) are synthetic in the mode that is similar to embodiment 302.

Embodiment 376

Compound (426): N-(1-phenyl ethidine is amino)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.42(2.7H，s)，2.67(0.3H，s)，5.61(0.9H，d，J＝14.7Hz)，5.70(0.1H，d，J＝10.1Hz)，6.80(0.1H，d，J＝10.1Hz)，7.29-7.61(13.9H，m)，7.91-7.93(1.8H，m)，8.02-8.04(0.2H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 377

Compound (427): N-(2,2,2-trifluoroethyl)-3-(thiophenyl) sulfo-acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：3.99(1.5H，q，J＝9.5Hz)，4.08(0.5H，q，J＝9.5Hz)，5.63(0.75H，d，J＝14.7Hz)，5.68(0.25H，d，J＝10.1Hz)，6.78(0.25H，d，J＝10.1Hz)，7.20-7.53(10.75H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (428)-(455) are synthetic in the mode that is similar to embodiment 161.

Embodiment 378

Compound (428): 3-(2-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.88-2.00(1H，m)，2.31(3H，s)，2.98(2H，d，J＝6.8Hz)，6.05(1H，d，J＝15.6Hz)，6.61(2H，d，J＝8.5Hz)，7.02-7.42(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 379

Compound (429): 3-(3-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.88-2.00(1H，m)，2.32(3H，s)，3.00(2H，d，J＝6.8Hz)，6.16(1H，d，J＝16.4Hz)，6.62(2H，d，J＝8.5Hz)，7.05-7.33(6H，m)，7.32(1H，d，J＝16.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 380

Compound (431): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.5Hz)，1.88-1.99(1H，m)，2.32(3H，s)，2.98(2H，d，J＝7.3Hz)，5.95(1H，d，J＝16.6Hz)，6.57(2H，d，J＝8.3Hz)，6.96-7.47(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 381

Compound (432): N-(4-aminomethyl phenyl)-3-(4-fluorobenzene sulfenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：0.97(6H，d，J＝6.5Hz)，1.75-1.86(1H，m)，2.34(3H，s)，2.76(2H，d，J＝6.3Hz)，6.35(1H，d，J＝10.1Hz)，6.30-7.53(9H，m)。

The stereochemistry of-CH=CH-key is Z.

Embodiment 382

Compound (433): 3-(2-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.5Hz)，1.88-2.00(1H，m)，2.31(3H，s)，3.00(2H，d，J＝7.0Hz)，6.15(1H，d，J＝15.4Hz)，6.62(2H，d，J＝7.5Hz)，7.06(1H，d，J＝8.0Hz)，7.01-7.42(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 383

Compound (434): 3-(3-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.3Hz)，1.89-2.01(1H，m)，2.32(3H，s)，2.99(2H，d，J＝6.5Hz)，6.13(1H，d，J＝16.1Hz)，6.62(2H，d，J＝7.0Hz)，7.08(1H，d，J＝8.0Hz)，7.22-7.38(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 384

Compound (435): 3-(4-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.5Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.99(2H，d，J＝6.8Hz)，6.04(1H，d，J＝15.4Hz)，6.59(2H，d，J＝8.3Hz)，7.06(1H，d，J＝8.0Hz)，7.18-7.31(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 385

Compound (437): 3-(3-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.89-2.00(1H，m)，2.32(3H，s)，3.00(2H，d，J＝6.8Hz)，6.12(1H，d，J＝15.6Hz)，6.62(2H，d，J＝8.3Hz)，7.05-7.44(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 386

Compound (438): 3-(4-bromobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.89-1.99(1H，m)，2.33(3H，s)，2.99(2H，d，J＝6.8Hz)，6.06(1H，d，J＝15.6Hz)，6.59(2H，d，J＝7.8Hz)，7.01-7.46(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 387

Compound (440): N-(4-aminomethyl phenyl)-3-(4-nitrophenylsulfenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.03(6H，d，J＝6.8Hz)，1.91-2.02(1H，m)，2.32(3H，s)，3.02(2H，d，J＝6.5Hz)，6.37(1H，d，J＝16.1Hz)，6.65(2H，d，J＝8.0Hz)，7.01(2H，d，J＝8.3Hz)，7.33(1H，d，J＝15.6Hz)，7.45(2H，d，J＝8.3Hz)，8.13(2H，d，J＝8.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 388

Compound (441): N-(4-aminomethyl phenyl)-3-(2-methylbenzene sulfenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝7.0Hz)，1.88-1.99(1H，m)，2.30(3H，s)，2.32(3H.s)，2.98(2H，d，J＝6.5Hz)，5.88(1H，d，J＝15.6Hz)，6.57(2H，d，J＝8.3Hz)，7.02(1H，d，J＝8.0Hz)，7.10-7.38(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 389

Compound (443): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.98(1H，m)，2.31(3H，s)，2.32(3H.s)，2.98(2H，d，J＝6.5Hz)，6.02(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8.0Hz)，7.02-7.38(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 390

Compound (444): N-(4-aminomethyl phenyl)-3-(4-trifluoromethyl thiophenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.90-1.99(1H，m)，2.31(3H，s)，3.01(2H，d，J＝6.5Hz)，6.21(1H，d，J＝15.4Hz)，6.62(2H，d，J＝8.3Hz)，7.07(2H，d，J＝8.3Hz)，7.32(1H，d，J＝15.4Hz)，7.45(2H，d，J＝8.5Hz)，7.57(2H，d，J＝8.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 391

Compound (446): 3-(3-anisole sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ³)δ(ppm)：1.01(6H，d，J＝6.5Hz)，1.88-1.99(1H，m)，2.31(3H，s)，2.99(2H，d，J＝6.5Hz)，3.79(3H，s)，6.14(1H，d，J＝15.4Hz)，6.62(2H，d，J＝8.3Hz)，6.80-7.25(6H，m)，7.38(1H，d，J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 392

Compound (447): 3-(4-anisole sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.5Hz)，1.87-1.98(1H，m)，2.31(3H，s)，2.97(2H，d，J＝6.5Hz)，3.87(3H，s)，5.92(1H，d，J＝15.4Hz)，6.58(2H，d，J＝8.0Hz)，6.82(2H，d，J＝8.8Hz)，7.02(2H，d，J＝8.0Hz)，7.26-7.33(3H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 393

Compound (448): 3-(2,4 dichloro benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.5Hz)，1.89-2.00(1H，m)，2.32(3H，s)，3.00(2H，d，J＝6.3Hz)，6.05(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8.3Hz)，7.06(2H，d，J＝8.0Hz)，7.18-7.33(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 394

Compound (449): 3-(3,4-dichlorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝7.0Hz)，1.89-2.00(1H，m)，2.32(3H，s)，3.00(2H，d，J＝6.8Hz)，6.08(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8.3Hz)，7.03-7.47(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 395

Compound (450): 3-(3,5-dichlorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.89-2.01(1H，m)，2.32(3H，s)，3.01(2H，d，J＝6.8Hz)，6.17(1H，d，J＝15.4Hz)，6.62(2H，d，J＝8.0Hz)，7.06-7.28(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 396

Compound (451): 3-(2,4-dimethyl benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.5Hz)，1.87-1.99(1H，m)，2.28(6H，s)，2.31(3H，s)，2.97(2H，d，J＝6.8Hz)，5.77(1H，d，J＝15.4Hz)，6.55(2H，d，J＝7.8Hz)，6.90-7.28(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 397

Compound (452): N-(4-aminomethyl phenyl)-3-(2-pyridyl sulfenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.05(6H，d，J＝6.8Hz)，1.92-2.04(1H，m)，2.32(3H，s)，3.02(2H，d，J＝6.5Hz)，6.43(1H，d，J＝15.9Hz)，6.68(2H，d，J＝7.8Hz)，7.07-7.23(4H，m)，7.52-7.60(1H，m)，8.20(1H，d，J＝15.9Hz)，8.52-8.56(1H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 398

Compound (454): N-(4-aminomethyl phenyl)-3-(2-pyrimidine-based sulfur-base) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.06(6H，d，J＝6.5Hz)，1.93-2.05(1H，m)，2.32(3H，s)，3.03(2H，d，J＝6.5Hz)，6.47(1H，d，J＝16.6Hz)，6.68(2H，d，J＝8.3Hz)，7.08(1H，t，J＝4.8Hz)，7.11(2H，d，J＝7.5Hz)，8.29(1H，d，J＝16.6Hz)，2-7.60(1H，m)，8.20(1H，d，J＝16.6Hz)，8.60(1H，d，J＝5.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (456)-(467) are synthetic in the mode that is similar to embodiment 223.

Embodiment 399

Compound (456): 3-(benzylthio-)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.97(2H，d，J＝6.8Hz)，3.85(2H，s)，6.10(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8.0Hz)，7.04-7.31(8H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 400

Compound (458): 3-(4-fluoro benzylthio-)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.97(2H，d，J＝6.8Hz)，3.82(2H，s)，6.06(1H，d，J＝15.4Hz)，6.59(2H，d，J＝8.3Hz)，6.91-7.28(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 401

Compound (460): 3-(4-methyl benzylthio-)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.33(3H，s)，2.97(2H，d，J＝6.8Hz)，3.82(2H，s)，6.10(1H，d，J＝15.4Hz)，6.61(2H，d，J＝8.0Hz)，7.02-7.31(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 402

Compound (462): 3-(4-chloro benzylthio-)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.97(2H，d，J＝6.8Hz)，3.81(2H，s)，6.04(1H，d，J＝15.6Hz)，6.59(2H，d，J＝8.3Hz)，7.04-7.26(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 403

Compound (464): 3-(2,4-benzyl dichloride sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.98(2H，d，J＝6.8Hz)，3.92(2H，s)，6.03(1H，d，J＝15.6Hz)，6.58(2H，d，J＝8.3Hz)，7.02-7.39(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 404

Compound (465): 3-(2-methyl benzylthio-)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.02(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.30(3H，s)，2.31(3H，s)，2.98(2H，d，J＝6.8Hz)，3.85(2H，s)，6.10(1H，d，J＝15.6Hz)，6.62(2H，d，J＝8.0Hz)，7.03-7.20(6H，m)，7.30(1H，d，J＝15.6Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 405

Compound (467): 3-(4-methoxybenzyl sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid isobutyl

¹H-NMR(CDCl ₃)δ(ppm)：1.01(6H，d，J＝6.8Hz)，1.87-1.99(1H，m)，2.32(3H，s)，2.97(2H，d，J＝6.8Hz)，3.79(3H，s)，3.81(2H，s)，6.10(1H，d，J＝15.4Hz)，6.62(2H，d，J＝8.3Hz)，6.80(2H，d，J＝6.8Hz)，7.04-7.13(4H，m)，7.28(1H，d，J＝15.4Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (468) is synthetic in the mode that is similar to embodiment 37.

Embodiment 406

Compound (468): 3-phenoxy group-N-(6-quinolyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.73(1H，d，J＝12.0Hz)，7.04-8.80(16H，m)，7.87(1H，d，J＝12.0Hz，PHOC H＝CHR)。

The stereochemistry of-CH=CH-key is E.

Compound (469)-(476) are synthetic in the mode that is similar to embodiment 161.

Embodiment 407

Compound (469): 3-(4-fluorobenzene sulfenyl)-N-(phenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.90(8H，m)，2.00-2.21(2H，m)，2.70-2.81(1H，Br)，5.91(1H，d，J＝15.6Hz)，6.69(2H，d，J＝7.6Hz)，6.94-7.38(10H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 408

Compound (470): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.30(2H，brs)，1.37-1.51(4H，m)，1.71(2H，brs)，2.05(2H，brs)，2.31(3H，s)，3.77(1H，brs)，6.11(1H，d，J＝15.7Hz)，6.63(2H，d，J＝8.2Hz)，7.06(2H，d，J＝8.2Hz)，7.27-7.37(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 409

Compound (471): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.24-1.28(2H，m)，1.37-1.47(4H，m)，1.72(2H，brs)，2.04(2H，brs)，2.31(3H，s)，3.76(1H，brs)，5.94(1H，d，J＝15.6Hz)，6.59(2H，d，J＝8.3Hz)，6.97-7.35(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 410

Compound (472): 3-(4-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.77(8H，m)，2.02-2.12(2H，m)，2.32(3H，s)，3.70-3.82(1H，m)，6.03(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8,0Hz)，7.06(2H，d，J＝8,7Hz)，7.20-7.30(4H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 411

Compound (473): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.20-1.63(6H，m)，1.66-1.78(2H，m)，2.02-2.12(2H，m)，2.31(3H，s)，2.33(3H，s)，3.68-3.81(1H，m)，6.01(1H，d，J＝15.5Hz)，6.61(2H，d，J＝8,0Hz)，7.03-7.33(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 412

Compound (474): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.92(3H，t J＝7.3Hz)，1.34-1.50(2H，m)，1.54-1.68(2H，m)，2.31(3H，s)，3.05(2H，t J＝7.3Hz)，5.95(1H，d，J＝15.4Hz)，6.59(2H，d，J＝8.0Hz)，6.97-7.35(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 413

Compound (475): 3-(4-chlorinated benzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.85-0.96(3H，m)，1.35-1.70(4H，m)，2.32(3H，s)，3.07(2H，t，J＝7.3Hz)，6.09(1H，d，J＝15.4Hz)，6.60(2H，d，J＝8.0Hz)，7.05-7.30(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 414

Compound (476): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.85-1.80(7H，m)，2.31(3H，s)，2.32(3H，s)，3.05(2H，t，J＝7.5Hz)，6.03(1H，d，J＝15.4Hz)，6.61(2H，d，J＝8.3Hz)，7.01-7.35(7H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (477)-(480) are synthetic in the mode that is similar to embodiment 176.

Embodiment 415

Compound (477): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4,5-dimethylthiazole-2-base ester

¹H-NMR (CDCl ₃) δ (ppm): 2.29,2.31,2.33,2.34,2.36,2.37 (total 9H, s), 5.64 (0.52H, d J=15.5Hz), (5.94 0.37H, d J=9.9Hz), 6.16 (0.11H, d J=15.5Hz), 6.71-7.20 (4H, m), (7.28-7.63 6H, m).

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 416

Compound (478): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 5-methyl isophthalic acid, 3,4-thiadiazoles-2-base ester

¹H-NMR(CDCl ₃)δ(ppm)：2.35(3H，s)，2.73(3H，s)，6.19(1H，dJ＝15.9Hz)，6.73(2H，d J＝8.5Hz)，7.13(2H，d J＝7.8Hz)，7.35-7.40(5H，m)，7.55(1H，d J＝15.9Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 417

Compound (479): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 1-methyl isophthalic acid H-tetrazolium-5-base ester

¹H-NMR(CDCl ₃)δ(ppm)：2.24(1.3H，s)，2.35(1.7H，s)，3.77(1.3H，s)，3.92(1.7H，s)，6.19(0.56H，d J＝15.6Hz)，6.26(0.44H，d J＝15.4Hz)，6.66-7.16(4H，m)，7.32-7.54(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 418

Compound (480): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2-thienyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.34(2.3H，s)，2.37(0.7H，s)，5.70(0.77H，d J＝14.6Hz)，5.92(0.23H，d J＝10.2Hz)，6.83-7.58(13H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (481)-(487) are synthetic in the mode that is similar to embodiment 161.

Embodiment 419

Compound (481): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.92-1.90(10H，m)，2.30(3H，s)，2.89-3.02(3H，m)，6.12(1H，d，J＝15.2Hz)，6.62(2H，d，J＝7.9Hz)，7.06(2H，d，J＝8.2Hz)，7.26-7.40(6H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 420

Compound (482): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid cyclohexyl methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.94-1.90(10H，m)，2.32(3H，s)，2.85-3.01(3H，m)，5.95(1H，d，J＝15.5Hz)，6.68(2H，d，J＝7.9Hz)，6.95-7.38(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 421

Compound (483): N-(4-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid 1-phenylethylester

¹H-NMR(CDCl ₃)δ(ppm)：1.73(3H，d，J＝7.0Hz)，2.32(3H，s)，5.01(1H，q，J＝7.0Hz)，6.09(1H，d，J＝15.7Hz)，6.61(2H，d，J＝8，2Hz)，7.07(2H，d，J＝8.0Hz)，7.20-7.45(11H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 422

Compound (484): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid 1-phenyl propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.91(3H，t J＝7.3Hz)，1.93-2.17(2H，m)，2.31(6H，s)，4.78(1H，m)，5.97(1H，d，J＝15.4Hz)，6.54(2H，d，J＝8.0Hz)，7.03-7.37(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 423

Compound (485): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid 1-phenyl propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.92(3H，t J＝7.3Hz)，1.94-2.17(2H，m)，2.31(3H，s)，4.79(1H，m)，5.91(1H，d，J＝15.4Hz)，6.53(2H，d，J＝8.3Hz)，6.96-7.37(12H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 424

Compound (486): N-(4-aminomethyl phenyl)-3-(4-methylbenzene sulfenyl) sulfo-acryloyl imido acid amyl group ester

¹H-NMR(CDCl ₃)δ(ppm)：0.89(3H，t J＝7.1Hz)，1.30-1.42(4H，m)，1.63-1.70(2H，m)，2.31(3H，s)，2.33(3H，s)，3.04(2H，t J＝7.4Hz)，6.03(1H，d，J＝15.7Hz)，6.61(2H，d，J＝8.2Hz)，7.04-7.37(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 425

Compound (487): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) sulfo-acryloyl imido acid amyl group ester

¹H-NMR(CDCl ₃)δ(ppm)：0.89(3H，t J＝7.1Hz)，1.29-1.42(4H，m)，1.63-1.70(2H，m)，2.31(3H，s)，3.04(2H，t J＝7.4Hz)，5.95(1H，d，J＝15.5Hz)，6.59(2H，d，J＝8.2Hz)，6.97-7.35(7H，m)。

The stereochemistry of-CH=CH-key is E.

Compound (488) is synthetic in the mode that is similar to embodiment 37.

Embodiment 426

Compound (488): 3-phenoxy group-N-(3,4,5-trimethylphenyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.10(3H，s)，2.22(6H，s)，5.84(1H，d，J＝12.0Hz)，6.47(2H，s)，7.03-7.38(10H，m)，7.77(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (489) is with synthetic with embodiment 176 similar modes.

Embodiment 427

Compound (489): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-methyl-4H-1,2,4-triazole-3-base ester

¹H-NMR(CDCl ₃)δ(ppm)：2.24(1.08H，s)，2.28(0.54H，s)，2.34(1.38H，s)，3.49(1.08H，s)，3.53(0.54H，s)，3.62(1.38H，s)，6.16(0.46H，d，J＝15.4Hz)，6.29(0.36H，d，J＝15.4Hz)，6.38(0.18H，d J＝10.2Hz)，6.72-7.14(5H，m)，7.30-7.55(5H，m)，7.67(0.18H，s)，7.69(0.36H，s)，7.88(0.46H，s)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (490) is synthetic in the mode that is similar to embodiment 37.

Embodiment 428

Compound (490): 3-phenoxy group-N-(3-thienyl) acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.95(1H，d，J＝11.8Hz)，6.52(1H，dd，J ₁＝3.1Hz，J ₂＝1.2Hz)，6.70(1H，dd，J ₁＝5.1Hz，J ₂＝1.2Hz)，7.07-7.40(11H，m)，7.83(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (491)-(494) are synthetic in the mode that is similar to embodiment 100.

Embodiment 429

Compound (491): 3-(1-methyl ethidine amino oxygen base)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.92(6H，s)，2.20(6H，s)，2.35(3H，s)，5.56(1H，d，J＝12.4Hz)，6.52-6.54(1H，m)，6.59(1H，brs.)，6.94-7.01(4H，m)，7.21-7.23(1H，m)，8.01(1H，d，J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 430

Compound (492): N-(3,4-3,5-dimethylphenyl)-3-(1-phenyl ethidine amino oxygen base) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.22(6H，s)，2.30(3H，s)，2.36(3H，s)，5.69(1H，d，J＝12.4Hz)，6.55-6.58(1H，m)，6.62(1H，brs.)，6.95-7.04(4H，m)，7.23-7.27(1H，m)，7.36-7.44(3H，m)，7.63-7.66(2H，m)，8.18(1H，d，J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 431

Compound (493): 3-cyclohexylidene amino oxygen base-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.55-1.70(6H，m)，2.19(6H，s)，2.19-2.23(2H，m)，2.35(3H，s)，2.45-2.49(2H，m)，5.54(1H，d，J＝12.4Hz)，6.53-6.55(1H，m)，6.59(1H，brs.)，6.93-7.01(4H，m)，7.23-7.24(1H，m)，8.02(1H，d，J＝12.4Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 432

Compound (494): 3-dimethylamino oxygen base-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(6H，s)，2.35(3H，s)，2.66(6H，s)，5.52(1H，d，J＝12.6Hz)，6.51-6.53(1H，m)，6.58(1H，brs.)，6.93-7.01(4H，m)，7.21-7.25(1H，m)，7.62(1H，d，J＝12.6Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (495)-(497) are synthetic in the mode that is similar to embodiment 176.

Embodiment 433

Compound (495): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 1-methyl isophthalic acid H-imidazoles-2-base ester

¹H-NMR (CDCl ₃) δ (ppm): 2.25 (0.9H, s), 2.29 (0.8H, s), (2.35 1.29H, s), 3.55 (0.8H, s), (3.58 0.77H, s), 3.61 (0.52H, s), (3.63 0.90H, s), 6.19 (0.30H, d J=15.4Hz), (6.25 d J=9.8Hz), the total 0.43H of 6.26 (d J=9.8Hz), 6.32 (0.27H, d J=15.4Hz), (6.49-7.13 7H, m), 7.29-7.54 (6H, m).

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 434

Compound (496): N-(4-aminomethyl phenyl)-3-thiophenyl sulfo-acryloyl imido acid benzothiazole-2-base ester

¹H-NMR(CDCl ₃)δ(ppm)：2.32(1.23H，s)，2.36(1.14H，s)，2.37(0.63H，s)，5.75(0.38H，d J＝14.6Hz)，6.11(0.21H，d J＝10.Hz)，6.23(0.41H，d J＝15.4Hz)，6.81-8.06(14H，m)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 435

Compound (497): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 2-methyl furan-3-base ester

¹H-NMR(CDCl ₃)δ(ppm)：2.12(0.3H，s)，2.16(1.4H，s)，2.18(0.6H，s)，2.22(0.7H，s)，2.29(0.47H，s)，2.33(2.53H，s)，5.41(0.1H，dJ＝14.1Hz)，5.53(0.2H，d J＝14.4Hz)，5.69(0.7H，d J＝14.9Hz)，6.18(1H，s)，6.83(2H，d J＝8.3Hz)，7.14-7.53(9.3H，m)，7.55(0.7H，d J＝14.9Hz)。

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (498)-(501) are synthetic in the mode that is similar to embodiment 100.

Embodiment 436

Compound (498): N-(3,4-3,5-dimethylphenyl)-3-(2-methyl furan-3-base sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.18(3H，s)，2.19(3H，s)，2.26(3H，s)，2.34(3H，s)，5.72(1H，d，J＝15.0Hz)，6.29(1H，brs.)，6.45-6.50(2H，m)，6.94-6.99(4H，m)，7.21-7.25(2H，m)，7.39(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 437

Compound (499): N-(3,4-3,5-dimethylphenyl)-3-(4,5-dimethylthiazole-2-base sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(6H，s)，2.29(3H，s)，2.32(3H，s)，2.36(3H，s)，6.14(1H，d，J＝15.5Hz)，6.49-6.55(2H，m)，6.97-7.01(4H，m)，7.23-7.27(1H，m)，7.78(1H，d，J＝15.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 438

Compound (500): N-(3,4-3,5-dimethylphenyl)-3-(thiophene-2-methylthiol) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(6H，s)，2.35(3H，s)，4.11(2H，s)，5.94(1H，d，J＝15.0Hz)，6.46-6.54(2H，m)，6.82-6.99(6H，m)，7.20-7.25(2H，m)，7.53(1H，d，J＝15.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 439

Compound (501): N-(3,4-3,5-dimethylphenyl)-3-(thiophene-2-base sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.18(6H，s)，2.34(3H，s)，5.82(1H，d，J＝15.2Hz)，6.45-6.50(2H，m)，6.93-6.99(5H，m)，7.17-7.23(2H，m)，7.41-7.42(1H，m)，7.48(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (502) is with synthetic with embodiment 176 similar modes.

Embodiment 440

(502): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-trifluoromethyl pyrimidine-2-base ester

¹H-NMR (CDCl ₃) δ (ppm): 2.26 (1.86H, s), 2.30 (0.27H, s), 2.32 (0.87H, s), (6.30 0.09H, d J=15.0Hz), 6.41 (d J=15.0Hz), 6.41 (dJ=10.1Hz) total 0.91H, 6.71-6.92 (2H, m), 7.02-7.14 (2H, m), 7.27-7.52 (6.38H, m), 7.69 (0.62H, d J=15.0Hz), 8.70 (0.62H, d J=5.1Hz), 8.77 (0.29H, d J=4.8Hz), 8.80 (0.09H, d J=4.8Hz).

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (503) is synthetic in the mode that is similar to embodiment 37.

Embodiment 441

Compound (503): N-[4-(1,1-dimethyl ethylmercapto group) phenyl]-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：1.24(9H，s)，5.69(1H，d，J＝11.8Hz)，6.74-7.42(14H，m)，7.82(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (504) and (505) are synthetic in the mode that is similar to embodiment 158.

Embodiment 442

Compound (504): N-[4-(4-aminomethyl phenyl) phenyl]-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：2.37(3H，s)，5.83(1H，d，J＝12.0Hz)，6.85-7.43(18H，m)，7.82(1H，d，J＝12.0Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 443

Compound (505): N-[4-(4-chlorophenyl) phenyl]-3-phenoxy group acryloyl imido acid phenylester

¹H-NMR(CDCl ₃)δ(ppm)：5.80(1H，d，J＝11.8Hz)，6.86-7.49(18H，m)，7.83(1H，d，J＝11.8Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (506) and (507) are synthetic in the mode that is similar to embodiment 176.

Embodiment 444

Compound (506): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid benzoxazole-2-base ester

¹H-NMR (CDCl ₃) δ (ppm): 2.16 (1.11H, s), 2.19 (0.63H, s), 2.38 (1.26H, s), (6.22 0.46H, d J=15.5Hz), 6.31 (d J=15.5Hz), (6.31 d J=10.4Hz) total 0.58H, 6.78-6.83 (1H, m), 7.06-7.23 (3H, m), 7.27-7.55 (8H, m).

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Embodiment 445

Compound (507): N-(4-aminomethyl phenyl)-3-(thiophenyl) sulfo-acryloyl imido acid 4-(4-chloro-1H-pyrazol-1-yl) pyrimidine-2-base ester

¹H-NMR (CDCl ₃) δ (ppm): 2.27 (1.79H, s), 2.33 (0.97H, s), 2.35 (0.24H, s), (6.31 0.08H, d J=15.0Hz), 6.41 (d J=14.7Hz), (6.44 d J=10.1Hz) total 0.92H, 6.74 (1H, d J=8.2Hz), (6.92-7.16 3H, m), 7.29-7.40 (4H, m), 7.52-7.58 (2H, m, Ar), 7.69-7.73 (2H, m), 8.42 (1H, s), 8.50-8.52 (0.68H, m), (8.57 0.32H, d J=5.3Hz).

The stereochemistry of-CH=CH-key is the mixture of E and Z.

Compound (508)-(512) are synthetic in the mode that is similar to embodiment 100.

Embodiment 446

Compound (508): 3-(benzothiazole-2-base sulfenyl)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.23(3H，s)，2.24(3H，s)，2.40(3H，s)，6.61-6.68(2H，m)，6.73(1H，d，J＝14.5Hz)，7.02-7.15(5H，m)，7.22-7.38(4H，m)，8.29(1H，d，J＝14.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 447

Compound (509): 3-(benzoxazole-2-base sulfenyl)-N-(3,4-3,5-dimethylphenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.19(3H，s)，2.23(3H，s)，2.40(3H，s)，6.60-6.69(3H，m)，7.02-7.14(4H，m)，7.28-7.34(4H，m)，7.45-7.47(4H，m)，8.14(1H，d，J＝14.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 448

Compound (510): N-(3,4-3,5-dimethylphenyl)-3-(5-methyl isophthalic acid, 3,5-thiadiazoles-2-base sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.22(3H，s)，2.23(3H，s)，2.37(3H，s)，2.46(3H，s)，6.54-6.52(3H，m)，6.99-7.06(4H，m)，7.24-7.28(1H，m)，8.54(1H，d，J＝13.5Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 449

Compound (511): N-(3,4-3,5-dimethylphenyl)-3-(furans-2-methylthiol) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.20(6H，s)，2.35(3H，s)，3.92(2H，s)，5.96(1H，d，J＝15.2Hz)，6.06(1H，d，J＝3.1Hz)，6.28(1H，dd，J ₁＝3.1Hz，J ₂＝1.9Hz)，6.49(1H，dd，J ₁＝7.8Hz，J ₂＝2.1Hz)，6.55(1H，brs)，6.91-7.01(4H，m)，7.22-7.26(1H，m)，7.33(1H，brs)，7.55(1H，d，J＝15.2Hz)。

The stereochemistry of-CH=CH-key is E.

Embodiment 450

Compound (512): N-(3,4-3,5-dimethylphenyl)-3-(1-methyl isophthalic acid H-tetrazolium-5-base sulfenyl) acryloyl imido acid 3-aminomethyl phenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.21(6H，s)，2.38(3H，s)，3.89(3H，s)，6.53-6.60(2H，m)，6.97(1H，d，J＝14.2Hz)，7.01-7.06(4H，m)，7.25-7.30(1H，m)，8.18(1H，d，J＝14.2Hz)。

The stereochemistry of-CH=CH-key is E.

Compound (513), (598) and (599) are synthetic in the mode that is similar to embodiment 161.

Embodiment 451

Compound (513): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) acryloyl imido acid 1-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.00(3H，t，J＝7.4Hz)，1.36(3H，d，J＝7.0Hz)，1.60-1.76(2H，m)，2.32(3H，s)，3.78(1H，sext.，J＝6.8Hz)，5.95(1H，d，J＝15.5Hz)，6.59(2H，d，J＝8.2Hz)，6.97-7.35(7H，m)。

The stereochemistry of-CH=CH-key is E.

Embodiment 452

Compound (598): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) acryloyl imido acid decyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.87(3H，t J＝6.8Hz)，1.25-1.40(14H，m)，1.62-1.70(2H，m)，2.32(3H，s)，3.04(2H，t J＝7.2Hz)，5.96(1H，dJ＝15.5Hz)，6.59(2H，d J＝8.2Hz)，6.99(2H，m)，7.04(2H，d J＝8.2Hz)，7.25(1H，d J＝15.2Hz)，7.32-7.35(2H，m)

The stereochemistry of-CH=CH-key is E.

Embodiment 453

Compound (599): 3-(4-fluorobenzene sulfenyl)-N-(4-aminomethyl phenyl) acryloyl imido acid geranyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.59(3H，s)，1.67(3H，s)，1.70(3H，s)，1.94-2.13(4H，m)，2.32(3H，s)，3.71(2H，d，J＝7.8Hz)，5.08(1H，t，J＝6.3Hz)，5.33(1H，t，J＝7.8Hz)，5.96(1H，d，J＝15.4Hz)，6.60(2H，d，J＝7.9Hz)，6.99(2H，t，J＝8.7Hz)，7.05(2H，d，J＝7.9Hz)，7.24(1H，d，J＝15.4Hz)，7.33(2H，dd，J＝8.7，5.1Hz)

The stereochemistry of-CH=CH-key is E.

Can will show with compound number with other embodiment of the compound (I) of preparation as described above.

Wherein X, Y and Z are any of the substituting group combination shown in the table 1.

Table 1

Continued 1

Continued 1

Continued 1

Continued 1

Continued 1

Continued 1

Continued 1

Continued 1

Continued 1

And then will show with reference to Preparation Example.

With reference to Preparation Example 1

N-benzyloxy-3-(thiophenyl) acryloyl imido acid bromide (acrylimidoyl bromide)

Ice-cooled lower, pyridine (2.7ml) is joined in hydrochloride (2.6g) THF (80ml) solution of 3-(thiophenyl) acrylate chloride (3.0g) and O-benzyl hydroxyl 1 amine and under identical temperature and stirred 1 hour, then under room temperature, stir 3 and stir hour.The concentrating under reduced pressure reaction mixture.Chloroform (150ml) is joined in the residue, sequentially wash with 1N hydrochloric acid, pure water and saturated sodium-chloride water solution, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.Residue is through silica gel column chromatography (hexane: ethyl acetate 2: 1) obtain N-benzyloxy-3-(thiophenyl) acrylamide (3.5g), be colorless oil.

Make N-benzyloxy-3-(thiophenyl) acrylamide (1.0g) be dissolved in acetonitrile (70ml), ice-cooled lower, to wherein adding carbon tetrabromide (2.3g) and triphenyl phosphine (1.8g), then reflux is 4 hours.The concentrating under reduced pressure reaction mixture.Residue is through silica gel column chromatography (hexane: ethyl acetate 20: 1), obtain N-benzyloxy-3-(thiophenyl) acryloyl imido acid bromide (1.1g), be faint yellow oily thing.

¹H-NMR(CDCl ₃)δ(ppm)：5.21(1.7H，s)，5.35(0.3H，s)，6.05(0.17H，d，J＝10.4Hz)，6.14(0.83H，d，J＝14.7Hz)，6.70(0.17H，d，J＝10.4Hz)，7.21-7.48(10.83H，m)

With reference to Preparation Example 2

N-phenyl-3-(thiophenyl) acrylamide

3-thiophenyl vinylformic acid (6.74g) is suspended in the toluene (50ml), then to wherein adding thionyl chloride (5.00ml) and 1 DMF.This mixture was stirred 30 minutes in 60 ℃ of oil baths.The concentrating under reduced pressure reaction mixture.Ice-cooled lower, residue is added dropwise in acetonitrile (60ml) solution of aniline (8.5ml), and and under identical temperature, stirred 3 hours.In the reaction mixture impouring 250ml ice-water, and be adjusted to pH3 with concentrated hydrochloric acid.Filter the crystallization of collecting precipitation, wash with water and drying, obtain N-phenyl-3-(thiophenyl) acrylamide (9.09g), be the light brown crystallization.

¹H-NMR(CDCl ₃)δ(ppm)：5.78(0.84H，d J＝14.6Hz)，5.98(0.16H，dJ＝9.8Hz)，7.00-7.59(11.16H，m)，7.84(0.84H，d J＝14.6Hz)

Following compound is synthetic to be similar to aforesaid mode.

N-(4-chlorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.74(0.92H，d J＝15.0Hz)，5.96(0.08H，dJ＝9.9Hz)，7.03-7.59(9.08H，m)，7.84(0.92H，d J＝14.9Hz)

N-(3-chlorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.74(0.94H，d J＝14.9Hz)，5.97(0.06H，dJ＝9.7Hz)，7.03-7.67(9.06H，m)，7.85(1H，d J＝14.9Hz)

N-(2-chlorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.88(1H，d J＝15.1Hz)，6.98-7.08(1H，m)，7.22-7.58(8H，m)，7.88(1H，d J＝15.1Hz)

N-phenyl-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.70(1H，d，J＝12.0Hz)，7.07-7.20(5H，m)，7.30-7.39(4H，m)，7.52-7.54(2H，m)，7.89(1H，d，J＝12.0Hz)

N-(4-p-methoxy-phenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.78(3H，s)，5.77(1H，d J＝14.7Hz)，6.81-6.88(1H，m)，6.97-7.04(2H，m)，7.24-7.55(5H，m)，7.81(1H，d J＝14.7Hz)

N-(2-difluorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.82(1H，d J＝14.7Hz)，6.98-7.57(9H，m)，7.86(1H，d J＝14.7Hz)

N-(3-pyridyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.87(0.81H，d J＝14.7Hz)，6.11(0.19H，dJ＝9.9Hz)，7.18-7.58(5.19H，m，Ar-H)，7.85(0.81H，d J＝14.7Hz)，8.17-8.30(2H，m)，8.49-8.65(2H，m)

With reference to Preparation Example 3

N-phenyl-3-(cyclohexyl sulfenyl) acrylamide

Under room temperature, thionyl chloride (0.58ml) and 1 DMF are joined 3-(cyclohexyl sulfenyl) sulfo-vinylformic acid (1.0g) in the suspension of toluene (15ml), and it was stirred 1.5 minutes in 80 ℃ of oil baths.The concentrating under reduced pressure reaction mixture.Acetonitrile (20ml) is joined in the residue, then lower aniline (0.50g) and triethylamine (0.73ml) are joined in this mixture ice-cooled.And under identical temperature, stirred this mixture 3 hours, concentrating under reduced pressure then. 1N hydrochloric acid (50ml) is joined in the residue, and extract with ethyl acetate (100ml).Organic layer water and saturated sodium-chloride water solution sequentially wash, through anhydrous magnesium sulfate drying and concentrating under reduced pressure.Separating residue and through purification by silica gel column chromatography (hexane: ethyl acetate=5: 1) obtain E form (0.60g) and the Z-shaped formula (0.38g) of N-phenyl-3-(cyclohexyl sulfenyl) acrylamide.

The E form

¹H-NMR(CDCl ₃)δ(ppm)：1.26-1.49(5H，m)，1.60-1.65(1H，m)，1.77-1.80(2H，m)，2.01-2.04(2H，m)，3.01-3.07(1H，m)，5.95(1H，d，J＝14.8Hz)，7.08-7.11(1H，m)，7.08-7.11(1H，m)，7.24(1H，brs)，7.29-7.33(2H，m)，7.53-7.55(2H，m)，7.77(1H，d，J＝14.8Hz)

Z-shaped formula

¹H-NMR(CDCl ₃)δ(ppm)：1.25-1.48(5H，m)，1.59-1.64(1H，m)，1.79-1.83(2H，m)，2.01-2.04(2H，m)，2.79-2.84(1H，m)，5.90(1H，d，J＝10.4Hz)，7.05-7.10(2H，m)，7.23(1H，brs)，7.26-7.31(2H，m)，7.54-7.62(2H，m)

With reference to Preparation Example 4

N-(4-aminomethyl phenyl)-3-(thiophenyl) acrylamide

Make p-toluidine (2.46g) be dissolved in acetonitrile (20ml), then ice-cooled lower, to acetonitrile (3ml) solution that wherein is added dropwise to 3-(thiophenyl) acrylate chloride (2.0g).This mixture was stirred under room temperature 1.5 hours.In reaction mixture impouring 50ml ice-water, and be adjusted to pH 4 with concentrated hydrochloric acid.Filter the crystallization of collecting precipitation, wash with water and drying, obtain N-(4-aminomethyl phenyl)-3-(thiophenyl) acrylamide (2.62g), be the light brown crystallization.

¹H-NMR(CDCl ₃)δ(ppm)：2.28(3H，s)，5.86(0.8H，d J＝14.3Hz)，5.99(0.2H，d J＝9.9Hz)，7.02-7.15(2H，m)，7.28-7.63(7.2H，m)，7.84(0.67H，d J＝14.4Hz)，7.95(0.13H，d J＝14.5Hz)

Following compound is synthetic to be similar to aforesaid mode.

N-(4-difluorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.76(0.77H，d J＝14.7Hz)，5.96(0.23H，dJ＝9.4Hz)，6.93-7.60(9.23H，m)，7.83(0.77H，d J＝14.7Hz)

N-(3-difluorophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.77(0.77H，d J＝14.5Hz)，5.99(0.23H，dJ＝9.97Hz)，6.73-6.84(1H，m)，7.10-7.63(8.23H，m)，7.84(1H，dJ＝14.5Hz)

N-(4-trifluoromethyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.74(0.83H，d J＝14.4Hz)，5.99(0.17H，dJ＝9.7Hz)，7.23-7.77(9.17H，m)，7.90(0.83H，d J＝14.4Hz)

N-(4-aminomethyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.31(3H，s)，5.70(1H，d，J＝11.6Hz)，7.05-7.19(5H，m)，7.23(1H，brs)，7.34-7.40(4H，m)，7.87(1H，d，J＝11.6Hz)

N-(4-p-methoxy-phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.78(3H，s)，5.69(1H，d，J＝11.6Hz)，6.84-6.86(2H，m)，7.06-7.08(2H，m)，7.15-7.19(2H，m)，7.34-7.43(3H，m)，7.87(1H，d，J＝11.6Hz)

N-(2-chlorophenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.75(1H，d，J＝11.7Hz)，7.01-7.05(1H，m)，7.09-7.12(2H，m)，7.18-7.30(2H，m)，7.35-7.41(3H，m)，7.48(1H，brs)，7.92(1H，d，J＝11.7Hz)，8.43(1H，d，J＝8.3Hz)

N-(3,5-dichlorophenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.66(1H，d，J＝11.6Hz)，7.06-7.08(3H，m)，7.18-7.21(1H，m)，7.26(1H，s)，7.36-7.51(2H，m)，7.51(2H，s)，7.90(1H，d，J＝11.6Hz)

N-(3,4,5-trichloro-benzene base)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.63(1H，d，J＝11.6Hz)，7.07-7.09(3H，m)，7.19-7.23(1H，m)，7.37-7.41(2H，m)，7.67(2H，s)，7.91(1H，d，J＝11.6Hz)

N-(3-aminomethyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，5.70(1H，d，J＝11.6Hz)，6.92(1H，d，J＝7.5Hz)，7.06-7.09(2H，m)，7.15(1H，brs)，7.16-7.21(2H，m)，7.29-7.39(4H，m)，7.88(1H，d，J＝11.6Hz)

N-(3,4-3,5-dimethylphenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.21(3H，s)，2.23(3H，s)，5.69(1H，d，J＝11.6Hz)，7.05-7.10(4H，m)，7.15-7.19(1H，m)，7.23(1H，br.)，7.32-7.38(3H，m)，7.87(1H，d，J＝11.6Hz)

N-[3-(1-methylethyl) phenyl]-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.24(6H，d，J＝7.5Hz)，2.89(1H，sept，J＝7.5Hz)，5.70(1H，d，J＝11.6Hz)，6.98(1H，d，J＝7.5Hz)，7.07-7.09(2H，m)，7.16-7.24(3H，m)，7.35-7.43(4H，m)，7.90(1H，d，J＝11.6Hz)

N-[4-(1-methylethyl) phenyl]-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.23(6H，d，J＝7.5Hz)，2.88(1H，sept，J＝7.5Hz)，5.70(1H，d，J＝11.6Hz)，6.98(1H，d，J＝7.5Hz)，7.07-7.09(3H，m)，7.16-7.19(3H，m)，7.35-7.39(3H，m)，7.43(1H，brs)，7.88(1H，d，J＝11.6Hz)

N-(4-difluorophenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.67(1H，d，J＝11.6Hz)，7.00-7.10(5H，m)，7.17-7.21(1H，m)，7.36-7.40(2H，m)，7.48(2H，br.)，7.90(1H，d，J＝11.6Hz)

N-(4-bromo phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.67(1H，d，J＝11.6Hz)，7.06-7.09(2H，m)，7.17-7.21(2H，m)，7.35-7.45(6H，m)，7.89(1H，d，J＝11.6Hz)

N-(3-p-methoxy-phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.80(3H，s)，5.69(1H，d，J＝11.7Hz)，6.66(1H，dd，J ₁＝8.3Hz，J ₂＝1.7Hz，)，6.98(1H，d，J＝7.8Hz)，7.06-7.09(2H，m)，7.16-7.23(3H，m)，7.35-7.39(3H，m)，7.89(1H，d，J＝11.7Hz)

N-(4-iodine substituted phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.67(1H，d，J＝11.6Hz)，7.06-7.08(2H，m)，7.15-7.21(2H，m)，7.31-7.39(4H，m)，7.60-7.62(2H，m)，7.88，(1H，d，J＝11.6Hz)

N-(5-indanyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.00-2.10(2H，m)，2.84-2.90(4H，m)，5.70(1H，d，J＝11.6Hz)，7.07-7.19(6H，m)，7.35-7.39(2H，m)，7.48(1H，brs)，7.87(1H，d，J＝11.6Hz)

N-[4-(methylthio group) phenyl]-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.46(3H，s)，5.68(1H，d，J＝11.7Hz)，7.07-7.09(3H，m)，7.17-7.25(3H，m)，7.35-7.40(2H，m)，7.46(2H，br.)，7.89(1H，d，J＝11.7Hz)

N-(phendioxin-6-yl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：4.23(4H，s)，5.67(1H，d，J＝11.6Hz)，6.80(1H，d，J＝8.7Hz)，6.90(1H，brs)，7.01(1H，brs)，7.06-7.09(2H，m)，7.15-7.19(2H，m)，7.35-7.39(2H，m)，7.87(1H，d，J＝11.6Hz)

N-(4-benzyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.95(2H，s)，5.67(1H，d，J＝11.6Hz)，6.98(1H，brs)，7.08-7.10(2H，m)，7.13-7.21(6H，m)，7.28-7.30(2H，m)，7.35-7.43(4H，m)，7.89(1H，d，J＝11.6Hz)

N-(4-Trifluoromethoxyphen-l)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.68(1H，d，J＝11.6Hz)，7.07-7.10(2H，m)，7.14-7.21(4H，m)，7.36-7.40(2H，m)，7.55-7.58(2H，m)，7.91(1H，d，J＝11.6Hz)

N-(3-xenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.74(1H，d，J＝11.8Hz)，7.06-7.59(14H，m)，7.80(1H，brs)，7.91(1H，d，J＝11.8Hz)

N-(4-benzoylphenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.78(1H，d，J＝11.8Hz)，7.11-7.84(14H，m)，7.33(1H，brs)，7.94(1H，d，J＝11.8Hz)

N-(4-acetylphenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.58(3H，s)，5.69(1H，d，J＝11.8Hz)，7.09-7.96(9H，m)，7.25(1H，brs)，7.94(1H，d，J＝11.8Hz)

N-(4-methoxycarbonyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.90(3H，s)，5.68(1H，d，J＝11.6Hz)，7.09-7.64(7H，m)，7.58(1H，brs)，7.93(1H，d，J＝11.6Hz)，8.00-8.02(2H，m)

3-(phenoxy group)-N-(quinoline-6-yl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.70(1H，brs)，6.00(1H，d，J＝12.0Hz)，7.24-9.08(11H，m)，7.87(1H，d，J＝12.0Hz)

3-(phenoxy group)-N-(3,4,5-trimethylphenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.13(3H，s)，2.26(6H，s)，5.68(1H，d，J＝11.6Hz)，6.98(1H，brs)，7.07-7.39(7H，m)，7.87(1H，d，J＝11.6Hz)

N-[4-(1,1-dimethyl ethylmercapto group) phenyl]-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.27(9H，s)，1.68(1H，brs)，5.70(1H，d，J＝11.6Hz)，7.08-7.53(9H，m)，7.90(1H，d，J＝11.6Hz)

3-(phenoxy group)-N-(3-thienyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.67(1H，d，J＝11.8Hz)，7.01(1H，dd，J ₁＝5.2Hz，J ₂＝1.3Hz)，7.06-7.09(2H，m)，7.16-7.24(2H，m)，7.35-7.39(2H，m)，7.46(1H，brs)，7.59(1H，brs)，7.89(1H，d，J＝11.8Hz)

With reference to Preparation Example 5

N-(3-aminomethyl phenyl)-3-(thiophenyl) acrylamide

Ice-cooled lower, THF (45ml) solution of 3-(thiophenyl) acrylate chloride (3.03g) is joined triethylamine (2.09ml) THF (45ml) solution.Ice-cooled lower, join 3-monomethylaniline (1.62g) in this mixture and under room temperature, stirred 10 hours.The concentrating under reduced pressure reaction soln.Join in residue with ethyl acetate (200ml) ice-cooled 1N hydrochloric acid (40ml) and separate each layer.Organic layer is with saturated sodium-chloride water solution washing (40ml) twice, and through anhydrous magnesium sulfate drying, filtering inorganic salt and concentrating under reduced pressure obtain N-(3-aminomethyl phenyl)-3-(thiophenyl) acrylamide (3.46g).

¹H-NMR(CDCl ₃)δ(ppm)：2.33(3H，s)，5.77(0.83H，d J＝14.6Hz)，5.97(0.17H，d J＝9.9Hz)，6.86-6.96(2H，m)，7.12-7.58(7.17H，m)，7.84(0.83H，d J＝14.6Hz)

Following compound is synthetic to be similar to aforesaid mode.

N-(4-bromo phenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.60(0.13H，d，J＝14.5Hz)，5.76(0.67H，d，J＝14.7Hz)，5.96(0.18H，d，J＝9.9Hz)，7.13-7.59(9.18H，m)，7.84(0.67H，d，J＝14.4Hz)，7.95(0.13H，d，J＝14.5Hz)

N-(4-nitrophenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.73(0.71H，d，J＝14.3Hz)，6.01(0.29H，d，J＝9.6Hz)，7.34-7.59(6H，m)，7.70(1H，d，＝9.2Hz)，7.81(0.29H，d，J＝9.6Hz)，7.95(0.71H，d，J＝14.3Hz)，8.17-8.25(2H，m)

N-(3,4-dichlorophenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.65(1H，d，J＝11.6Hz)，7.07-7.09(2H，m)，7.13(1H，brs)，7.18-7.22(1H，m)，7.35-7.40(4H，m)，7.78(1H，s)，7.90(1H，d，J＝11.6Hz)

N-(4-cyano-phenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.75(0.71H，d，J＝15.0Hz)，6.00(0.23H，d，J＝9.9Hz)，7.29-7.79(9.23H，m)，7.91(0.77H，d，J＝15.0Hz)

N-(4-ethylphenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.20(2H，t，J＝7.6Hz)，2.60(3H，q，J＝7.6Hz)，5.79(0.83H，d，J＝14.8Hz)，5.98(0.17H，d，J＝9.9Hz)，7.06-7.22(3.17H，m)，7.30-7.56(6H，m)，7.82(0.83H，d，J＝14.8Hz)

N-[4-(1-methylethyl) phenyl]-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.22(6H，d，J＝7.0Hz)，2.87(1H，sept，J＝7.0Hz)，5.78(0.83H，d，J＝14.6Hz)，5.97(0.17H，d，J＝10.1Hz)，6.97-7.57(9.17H，m)，7.82(0.83H，d，J＝14.6Hz)

N-(4-propyl group phenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：0.93(2H，t，J＝7.5Hz)，1.61(3H，sext，J＝7.5Hz)，2.54(2H，t，J＝7.5Hz)，5.79(0.83H，d，J＝14.5Hz)，5.97(0.17H，d，J＝9.9Hz)，6.98-7.59(9.17H，m)，7.82(0.83H，d，J＝14.5Hz)

N-[4-(1,1-dimethyl ethyl) phenyl]-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.30(9H，s)，5.64(0.08H，d，J＝15.2Hz)，5.78(0.75H，d，J＝14.5Hz)，5.97(0.17H，d，J＝10.1Hz)，7.07-7.18(2H，m)，7.24-7.68(7.27H，m)，7.79(0.64H，d，J＝14.6Hz)，7.86(0.09H，d，J＝15.3Hz)

N-(4-thiophenyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.68(1H，d，J＝11.6Hz)，7.08-7.10(3H，m)，7.18-7.27(6H，m)，7.35-7.40(4H，m)，7.50-7.52(2H，m)，7.90(1H，d，J＝11.6Hz)

N-(4-propyl group phenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.06-1.47(6H，m)，1.58-1.93(4H，m)，2.35-2.51(1H，m)，5.64(0.09H，d，J＝15.3Hz)，5.86(0.64H，d，J＝14.6Hz)，6.00(0.27H，d，J＝10.1Hz)，7.16-7.58(9.17H，m)，7.83(0.75H，d，J＝14.5Hz)，7.88(0.08H，d，J＝15.2Hz)

N-(4-cyclohexyl sulfenyl phenyl)-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.19-1.35(6H，m)，1.57-1.62(1H，m)，1.75-1.77(2H，m)，1.94-1.96(2H，m)，2.96-3.05(1H，m)，5.68(1H，d，J＝11.6Hz)，7.00-7.48(10H，m)，7.90(1H，d，J＝11.6Hz)

N-(4-Phenoxyphenyl)-3-(thiophenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：5.64(0.09H，d，J＝15.1Hz)，6.03(0.64H，d，J＝14.8Hz)，6.11(0.27H，d，J＝9.9Hz)，6.83-6.95(4H，m)，6.98-7.07(1H，m)，7.16-7.58(9.27H，m)，7.83(0.75H，d，J＝14.5Hz)，7.88(0.08H，d，J＝15.2Hz)

N-[4-(1,1-dimethyl ethyl oxygen base) phenyl]-3-(phenoxy group) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.32(9H，s)，5.69(1H，d，J＝11.6Hz)，6.94-6.96(2H，m)，7.02(1H，brs)，7.08-7.10(2H，m)，7.16-7.20(1H，m)，7.36-7.40(1H，m)，7.89(1H，d，J＝11.6Hz)

3-(phenoxy group)-N-(4-piperidino-(1-position only) phenyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：1.56-1.61(2H，m)，1.67-1.73(4H，m)，3.09-3.12(4H，m)，5.68(1H，d，J＝11.6Hz)，6.89(2H，d，J＝8.9Hz)，7.00(1H，brs)，7.07(2H，d，J＝8.0Hz)，7.15-7.19(1H，m)，7.34-7.38(4H，m)，7.86(1H，d，J＝11.6Hz)

3-(thiophenyl)-N-(2,2,2-trifluoroethyl) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：3.90-4.02(2H，m)，5.65(0.77H，d，J＝14.5Hz)，5.66(0.77H，br.)，5.88(0.23H，d，J＝9.9Hz)，5.90(0.23H，br.)，7.20(0.23H，d，J＝9.9Hz)，7.33-7.49(5H，m)，7.80(0.77H，d，J＝14.5Hz)

3-(thiophenyl)-N-(1-phenyl ethidine is amino) acrylamide

¹H-NMR(CDCl ₃)δ(ppm)：2.20(2.4H，s)，2.29(0.6H，s)，6.89(0.8H，d，J＝15.1Hz)，7.04(0.2H，d，J＝10.2Hz)，7.36-7.60(10.2H，m)，7.95(0.8H，d，J＝15.1Hz)，8.69(0.8H，brs)，8.90(0.2H，brs)

With reference to Preparation Example 6

N-benzenesulfonyl-3-(thiophenyl) acrylamide

Ice-cooled lower, (55% in oil with sodium hydride, 0.48g) join in THF (30ml) solution of 3-(thiophenyl) acrylate chloride (1.0g) and benzsulfamide (0.87g), and under identical temperature, stirred 2 hours, then under room temperature, stirred 2 hours.The concentrating under reduced pressure reaction mixture.1N hydrochloric acid (50ml) is joined in the residue, and extract twice with chloroform (50ml).Organic layer washs with saturated sodium-chloride water solution, through anhydrous magnesium sulfate drying, and concentrating under reduced pressure.The crystallization that obtains is washed with t-butyl methyl ether, filters and collects, and drying under reduced pressure obtains N-benzenesulfonyl-3-(thiophenyl) acrylamide (1.4g).

¹H-NMR(CDCl ₃)δ(ppm)：5.62(0.8H，d，J＝14.7Hz)，5.99(0.2H，d，J＝10.1Hz)，7.34-7.66(8.2H，m)，7.86(0.8H，d，J＝14.7Hz)，7.99-8.01(1.6H，m)，8.10-8.12(0.4H，m)，8.48(0.8H，brs)，8.72(0.2H，brs)

With reference to Preparation Example 7

N-phenyl-3-(trimethyl silyl) sulfo-propyl group imido acid isopropyl esters

Make ethynyl trimethyl silane (0.93g) be dissolved in anhydrous THF (30ml), in-78 ℃ to wherein being added dropwise to n-Butyl Lithium/hexane solution (1.6mol/l; 5.6ml), then make it be warmed to 0 ℃.Reaction mixture is cooled to-78 ℃, THF (5ml) solution of isothiocyanic acid phenylester (1.24g) is added dropwise in the reaction mixture.Then make it be warmed to gradually 0 ℃.After this, ice-cooled lower, to THF (5ml) solution that wherein is added dropwise to 2-iodo propane (1.52g), then under room temperature, stirred 14 hours.Concentrated reaction solution.Residue obtains N-phenyl-3-(trimethyl silyl) sulfo-propyl group imido acid isopropyl esters (1.7g) through silica gel column chromatography (hexane/ethyl acetate=15/1).

¹H-NMR(CDCl ₃)δ(ppm)：0.09(6H，s)，0.28(3H，s)，1.37(0.33H，d，J＝6.7Hz)，1.40(0.66H，d，J＝6.7Hz)，3.82-3.98(1H，m)，6.85-7.36(5H，m)

Following compound is synthetic to be similar to aforesaid mode.

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.10(6H，s)，0.30(3H，s)，2.34(3H，s)，2.51(0.67H，s)，2.54(0.33H，s)，6.83-7.40(5H.m)

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.10(6H，s)，0.28(3H，s)，4.37(1.5H，s)，4.60(0.5H，s)，6.85-7.43(10H.m)

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid 2-propenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.10(6H，s)，0.28(3H，s)，3.72-3.82(2H，m)，5.10-5.35(2H，m)，5.80-6.02(1H，m)，6.83-7.39(5H，m)

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid 2-propynyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.11(6H，s)，0.31(3H，s)，2.21(0.66H，t，J＝2.6Hz)，2.26(0.33H，t，J＝2.6Hz)，3.82(1.3H，d，J＝2.6Hz)，3.90(0.7H.d，J＝2.6Hz)，6.88-7.38(5H，m)

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.09(6H，s)，0.31(3H，s)，1.77(2H，d，J＝7.2Hz)，2.05(1H，d，J＝7.2Hz)，5.07(0.66H，q，J＝7.2Hz)，5.12(0.33H，q，J＝7.2Hz)，7.02-7.47(10H，m)

3-(trimethyl silyl)-N-phenyl-sulfo-propyl group imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.09(6H，s)，0.30(3H，s)，1.13-1.80(8H，m)，2.04-2.18(2H，m)，3.52-3.64(0.33H.m)，3.75-3.87(0.66H，m)，6.87-7.36(5H，m)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid ethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，1.23-1.38(3H，m)，2.33(3H，s)，3.07-3.13(2H，m)，6.82(1H，d J＝8.3Hz)，6.99(1H，d J＝8.3Hz)，7.09-7.15(2H，m)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid propyl diester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.93-1.05(3H，m)，1.66-1.78(2H，m)，2.33(3H，s)，3.04-3.10(2H，m)，6.83(1H，d，J＝8.2Hz)，6.99(1H，d，J＝8.4Hz)，7.10(1H，d，J＝8.0Hz)，7.15(1H，d J＝7.7Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.88-1.00(3H，m)，1.37-1.50(2H，m)，1.62-1.77(2H，m)，2.33(3H，s)，3.06-3.13(2H，m)，6.83(1H，d，J＝8.2Hz)，6.99(1H，d，J＝8.2Hz)，7.10(1H，d，J＝8.0Hz)，7.15(1H，d J＝8.0Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid 2-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.98(2H，d J＝6.8Hz)，1.03(4H，d，J＝6.3Hz)，1.88-2.00(1H，m)，2.32(1.8H，s)，2.33(1.2H，s)，2.99(0.8H，d，J＝7.0Hz)，3.03(1.2H，d，J＝6.5Hz)，6.83(1H，d，J＝8.2Hz)，6.87(1H，d，J＝8.2Hz)，7.10(1H，d，J＝8.2Hz)，7.15(1H，d，J＝8.0Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid 1-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.98(1.3H，t，J＝8.5Hz)，1.03(1.7H，t，J＝8.5Hz)，1.36(1.3H，d，J＝7.0Hz)，1.39(1.7H，d，J＝6.7Hz)，1.60-1.78(2H，m)，2.33(3H，s)，3.64(0.4H，q，J＝6.3Hz)，3.83(0.6H，q，J＝6.8Hz)，6.83(1H，d，J＝8.5Hz)，7.00(1H，d，J＝8.2Hz)，7.10(1H，d，J＝8.0Hz)，7.15(1H，d，J＝7.7Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid cyclopentyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.11(6H，s)，0.28(3H，s)，1.61-1.75(6H，m)，2.15-2.18(2H，m)，2.32(3H，s)，3.88-3.91(0.4H，m)，3.98-4.02(0.6H，m)，6.83(1H，d，J＝8.2Hz)，7.00(1H，d，J＝8.2Hz)，7.10(1H，d，J＝8.2Hz)，7.15(1H，d，J＝8.2Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid 3,3-dimethyl-2-propenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，1.66-1.74(6H，m)，2.32(0.8H，s)，2.33(2.2H，s)，3.64(2H，d J＝7.3Hz)，5.15-5.23(1H，m)，6.83(1H，d，J＝8.3Hz)，7.01(1H，d，J＝8.0Hz)，7.00-7.15(2H，m)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(4.5H，s)，0.30(4.5H，s)，1.26-1.52(6H，m)，1.77(2H，brs)，2.10(2H，brs)，2.33(3H，s)，3.56-3.84(1H，m)，6.82(1H，d，J＝8.2Hz)，6.99(1H，d，J＝8.2Hz)，7.10(1H，d，J＝8.5Hz)，7.15(1H，d，J＝8.5Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid amyl group ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.87-0.92(3H，m)，1.32-1.43(4H，m)，1.63-1.74(2H，m)，2.33(3H，s)，3.05-3.12(2H，m)，6.83(1H，d，J＝8.2Hz)，6.99(1H，d，J＝8.5Hz)，7.10(1H，d，J＝8.0Hz)，7.15(1H，d，J＝8.0Hz)

N-(4-aminomethyl phenyl)-3-trimethyl silyl-sulfo-propyl group imido acid decyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.12(6H，s)，0.29(3H，s)，0.88(3H，t，J＝6.9Hz)，1.26-1.71(16H，m)，2.33(3H，s)，3.05-3.11(2H，m)，6.82(1H，d，J＝8.3Hz)，6.99(1H，d，J＝8.3Hz)，7.10(1H，d，J＝8.0Hz)，7.14(1H，d，J＝8.0Hz)

With reference to Preparation Example 8

N-phenyl-sulfo-propyl group imido acid isopropyl esters

Make N-phenyl-3-(trimethyl silyl) sulfo-propyl group imido acid isopropyl esters (1.6g) be dissolved in methyl alcohol (50ml), ice-cooled lower, to wherein adding a small amount of salt of wormwood, then stirred 30 minutes, in reaction soln impouring sodium chloride aqueous solution, and use ethyl acetate extraction.Organic layer washes with water, and dry and distillation desolventizing obtains N-phenyl-sulfo-propyl group imido acid isopropyl esters (1.1g).

¹H-NMR(CDCl ₃)δ(ppm)：1.38(1.5H，d，J＝6.8Hz)，1.41(4.5H，d，J＝7.0Hz)，3.20(0.8H，s)，3.40(0.2H，s)，3.80-4.20(1H，m)，6.88-7.38(5H，m)

Following compound is synthetic to be similar to aforesaid mode.

N-phenyl-sulfo-propyl group imido acid methyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.35(2H，s)，2.37(1H，s)，3.25(0.66H.s)，2.49(0.33H，s)，6.98-7.37(5H，m)

N-phenyl-sulfo-propyl group imido acid benzyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.25(0.75H，s)，3.51(0.25H，s)，4.38(1.3H，s)，4.60(0.7H，s)，6.88-7.42(10H.m)

N-phenyl-sulfo-propyl group imido acid 2-propenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：3.25(0.8H，s)，3.46(0.2H.s)，3.77-3.82(2H，m)，5.13-5.35(2H，m)，5.82-6.03(1H，m)，6.88-7.38(5H，m)

N-phenyl-sulfo-propyl group imido acid 2-propynyl ester

¹H-NMR(CDCl ₃)δ(ppm)：2.22(0.8H，t，J＝2.6Hz)，2.26(0.2H，t，J＝2.6Hz)，3.29(0.8H，s)，3.52(0.2H，s)，3.86(0.4H，d，J＝2.6Hz)，3.92(1.6H，d，J＝2.6Hz)，6.88-7.38(5H，m)

N-phenyl-sulfo-propyl group imido acid 1-styroyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.76(1.5H，d，J＝6.8Hz)，2.05(0.5H，d，J＝6.8Hz)，3.21(0.75H，s)，3.44(0.25H，s)，5.08(0.75H，q，J＝7.0Hz)，5.22(0.25H，q，7.0Hz)，6.98-7.55(10H，m).88-7.38(5H，m)

N-phenyl-sulfo-propyl group imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.27-1.80(8H，m)，2.05-2.14(2H，m)，3.20(0.66H，s)，3.38(0.33H，s)，3.55-3.66(0.33H，s)，3.80-3.90(0.66H，s)，6.88-7.48(5H.m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid ethyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.25(3H，m)，2.33(3H，s)，2.89(0.2H，q，J＝7.3Hz)，3.12(1.8H，q，J＝7.3Hz)，3.24(0.75H，s)，3.40(0.25H，s)，6.75-7.17(4H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid propyl diester

¹H-NMR(CDCl ₃)δ(ppm)：0.95-1.08(3H，m)，1.67-1.79(2H，m)，2.33(3H，s)，3.07-3.13(2H，m)，3.24(0.75H，s)，3.40(0.25H，s)，6.84(0.5H，d，J＝8.3Hz)，6.93(1.5H，d，J＝8.3Hz)，7.10-7.17(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid butyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.88-1.00(3H，m)，1.34-1.50(2H，m)，1.63-1.77(2H，m)，2.31(0.4H，s)，2.33(2.6H，s)，3.09-3.15(2H，m)，3.25(0.75H，s)，3.40(0.25H，s)，6.84(0.5H，d，J＝8.2Hz)，6.94(1.5H，d，J＝8.2Hz)，7.08-7.17(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid 2-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.98(1.5H，d J＝6.5Hz)，1.04(4.5H，d，J＝6.8Hz)，1.87-2.04(1H，m)，2.33(2.25H，s)，2.34(0.75H，s)，3.01(0.5H，d，J＝6.8Hz)，3.05(1.5H，d，J＝6.5Hz)，3.25(0.75H，s)，3.40(0.25H，s)，6.84(0.5H，d，J＝8.2Hz)，6.93(1.5H，d，J＝8.5Hz)，7.12(1.5H，d，J＝8.0Hz)，7.16(0.5H，d，J＝8.0Hz)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid 1-methyl-propyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.98(1H，t，J＝7.3Hz)，1.03(2H，t，J＝7.3Hz)，1.36(1H，d，J＝6.8Hz)，1.40(2H，d，J＝7.1Hz)，1.59-1.78(2H，m)，2.33(3H，s)，3.22(0.75H，s)，3.37(0.25H，s)，3.68(0.25H，q，J＝6.8Hz)，3.86(0.75H，q，J＝6.8Hz)，6.83(0.5H，d，J＝8.3Hz)，6.94(1.5H，d，J＝8.0Hz)，7.14(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid cyclopentyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.59-1.76(6H，m)，2.16-2.23(2H，m)，2.33(3H，s)，3.23(0.7H，s)，3.39(0.3H，s)，3.92-4.05(1H，m)，6.83(0.5H，d J＝8.5Hz)，6.93(1.5H，d J＝8.2Hz)，7.11-7.16(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid 3,3-dimethyl-2-propenyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.62-1.77(6H，m)，2.32(1H，s)，2.33(2H，s)，3.24(0.75H，s)，3.44(0.25H，s)，3.78(2H，d，J＝7.8Hz)，6.84(0.5H，d，J＝8.3Hz)，6.95(1.5H，d，J＝8.3Hz)，7.12-7.15(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid cyclohexyl ester

¹H-NMR(CDCl ₃)δ(ppm)：1.24-1.53(6H，m)，1.73-1.75(2H，m)，2.08-2.10(2H，m)，2.33(3H，s)，3.22(0.7H，s)，3.37(0.3H，s)，3.58-3.86(1H，m)，6.83(0.5H，d，J＝8.2Hz)，6.93(1.5H，d，J＝8.2Hz)，7.11-7.16(2H，m)

N-(4-aminomethyl phenyl)-sulfo-propyl group imido acid amyl group ester

¹H-NMR(CDCl ₃)δ(ppm)：0.91(3H，t，J＝7.2Hz)，1.31-1.45(4H，m)，1.63-1.75(2H，m)，2.33(3H，s)，3.07-3.13(2H，m)，3.24(0.7H，s)，3.40(0.3H，s)，6.84(0.5H，d，J＝8.5Hz)，6.93(1.5H，d，J＝8.2Hz)，7.12-7.17(2H，m)

N-(4-methyl-phenyl)-sulfo-propyl group imido acid decyl ester

¹H-NMR(CDCl ₃)δ(ppm)：0.88(3H，t，J＝6.8Hz)，1.26-1.74(16H，m)，2.33(3H，s)，3.08-3.13(2H，m)，3.24(0.75H，s)，3.40(0.25H，s)，6.83(0.5H，d，J＝8.3Hz)，6.94(1.5H，d，J＝8.3Hz)，7.12(1.5H，d，J＝8.0Hz)，7.15(0.5H，d，J＝8.0Hz)

Then, will show example of formulations.All umbers are weight part.

Example of formulations 1

Any in 10 parts of the compounds of this invention (1)-(599) is dissolved in the mixture of 35 parts of dimethylbenzene and 35 parts of DMFs, then adds 14 parts of polyoxyethylene styryl phenyl ethers and 6 parts of calcium dodecylbenzene sulphonates.Fully stir this mixture, obtain 10% emulsion.

Example of formulations 2

To 4 parts of sodium lauryl sulphate, 2 parts of calcium lignin sulphonates, in 20 parts of synthetic hydrated SiO 2 fine powders and the 54 parts of diatomaceous mixtures, add any in 20 parts of the compounds of this invention (1)-(599).Fully stir this mixture, obtain 20% wetting properties agricultural chemicals.

Example of formulations 3

In any, 1 part of synthetic hydrated SiO 2 fine powder in 2 parts of the compounds of this invention (1)-(599), the mixture of 2 parts of calcium lignin sulphonates, add 30 parts of wilkinites and 65 parts of kaolin, then fully stir.Then, the water of sufficient quantity joins in this mixture.Further stir this mixture, granulate with nodulizer, and dry through pressurized air flow, obtain 2% granule.

Example of formulations 4

Any in 1 part of the compounds of this invention (1)-(599) is dissolved in the acetone of sufficient quantity, then adds 5 parts of synthetic hydrated SiO 2 fine powders, 0.3 part of PAP and 93.7 parts of fubasami clays.Fully stir this mixture.Then, from this mixture, remove acetone by evaporation, obtain 1% pulvis.

Example of formulations 5

Any with in 10 parts of the compounds of this invention (1)-(599); 35 parts of white carbon(ink)s that contain 50 parts of Voranol EP 2001 ammonium sulfates; Pass through the wet method fine grinding with the mixture of 55 parts of water, but obtain 10% flowing agent (flowable agent).

Example of formulations 6

Any in 0.1 part of the compounds of this invention (1)-(599) is dissolved in 5 parts of dimethylbenzene and the 5 parts of trichloroethane.This solution is mixed with 89.9 parts of deodorized kerosines, obtain 0.1% oily matter.

Example of formulations 7

Make in any 0.5ml of the being dissolved in acetone in 10mg the compounds of this invention (1)-(599).The solid feed powder (the solid feed powder CE-2 that is used for nursing and feeding animals, by CLEA Japan, Inc. produces) of this solution and 5g animal is mixed closely, and then by evaporating acetone drying, obtain poison bait.

Then, show that by test example the compounds of this invention is being effective aspect the Control pests.

With 10 parts of compounds; 35 parts of white carbon(ink)s that contain 50 parts of Voranol EP 2001 ammonium sulfates; Pass through the wet method fine grinding with the mixture of 55 parts of water, obtain preparation.

With described preparation dilute with water, so that activity component concentration becomes 500ppm, be used for the test insecticide solution of test example 1-8 with system.

Test example 1 (prodenia litura (Spodoptela litura))

The filter paper that will have an identical diameter lies in (diameter: 5.5cm) at the bottom of the polyethylene cup.The thick Insecta LF (artificial diet of cutting double incision of 6mm will be sliced into; Nippon Nosankogyo Co.) is placed on it.Then with the above-mentioned test insecticide solution dipping of 2ml.After air-dry, 54 twill burglar moth larvaes in the length of time (prodenia litura) are placed cup and add a cover.After 6 days, check dead larva quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

Mortality ratio (%)={ (dead larva number)/(the larva number of detection) } * 100

Compound (1), (2), (3), (4), (6), (7), (9), (10), (11), (13), (14), (15), (16), (19), (20), (21), (22), (23), (24), (25), (26), (30), (31), (34), (35), (37), (38), (40), (41), (43), (44), (45), (46), (47), (50), (51), (53), (54), (55), (56), (57), (58), (59), (61), (63), (64), (65), (67), (69), (70), (71), (72), (73), (74), (75), (76), (77), (78), (80), (81), (83), (84), (86), (87), (88), (91), (97), (101), (102), (103), (104), (105), (106), (107), (108), (110), (111), (112), (113), (114), (115), (118), (119), (121), (123), (136), (142), (146), (149), (151), (152), (156), (157), (159), (166), (167), (168), (169), (174), (175), (177), (180), (184)-(187), (189), (193)-(195), (198), (200), (203)-(205), (211)-(237), (239)-(241), (247)-(252), (254)-(256), (258)-(260), (263)-(273), (277)-(307), (316), (317), (321), (322), (324), (325), (330), (332)-(339), (341)-(370), (373), (377), (385), (386), (388)-(401), (410)-(418), (427)-(453), (458), (459), (461)-(463), (469)-(490), (493), (495)-(502), (505), (507), (513), (598) and (599) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 2 (fruit leaf roller in summer (Adoxophyes orana))

The filter paper that will have an identical diameter lies in (diameter: 5.5cm) at the bottom of the polyethylene cup.Silkmate 2S (the artificial diet of 6mm thickness will be sliced into; Nippon Nosan kogyo Co.) is placed on it.Then with the above-mentioned test insecticide solution dipping of 1ml.After air-dry, the larva of the fruit roll leaf worm in summer (Adoxophyes orana) in 3 first length of times is placed cup and add a cover.After 7 days, check dead larva quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

Mortality ratio (%)={ (the larva number of the larva number of detection-survival)/(the larva number of detection) } X 100

Compound (1), (2), (3), (4), (6), (7), (9), (10), (11), (13), (14), (15), (16), (19), (20), (21), (22), (23), (24), (25), (26), (30), (31), (34), (35), (37), (38), (40), (41), (42), (43), (44), (45), (46), (47), (48), (50), (51), (52), (53), (54), (56), (57), (58), (59), (63), (64), (65), (69), (70), (71), (72), (73), (74), (75), (76), (77), (78), (80), (81), (83), (84), (86), (87), (88), (91), (92), (97), (100), (101), (102), (103), (104), (105), (106), (107), (108), (110), (111), (112), (113), (114), (115), (118), (119), (120), (121), (122), (123), (128), (136), (146), (149), (151), (152), (156), (157), (159), (162), (166), (167), (168), (169), (170), (174)-(180), (184)-(187), (189), (192)-(195), (198)-(200), (203)-(205), (211)-(237), (239)-(243), (247)-(261), (263)-(308), (311), (315)-(317), (321)-(325), (330)-(339), (341)-(379), (381), (383), (385), (386), (388)-(400), (410)-(415), (424), (428)-(453), (458), (459), (462), (463), (469)-(490), (492), (493), (495)-(502), (505), (507), (513), (598) and (599) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 3 (cotten aphid)

With cotten aphid (Aphis gossypii) larva in 30-first length of times be inoculated in 1 ounce of cup, grow first the leaf phase cucumber.After one day, spray the above-mentioned test insecticide solution of 20ml.After 6 days, check the larva quantity of survival.Calculate by following formula based on the untreated survival rate that checks, and result's exponential representation.4: survival rate 0%, 3: survival rate 1-10%, 2: survival rate 11-40%, 1: survival rate 41-70%, 0: survival rate is greater than the test larva number of 70% survival rate (%)=(the survival larva number on the cucumber of processing)/on untreated cucumber) X 100

Compound (1), (2), (3), (4), (8), (9), (10), (12), (14), (15), (16), (17), (18), (19), (20), (23), (24), (25), (26), (27), (29), (30), (31), (34), (35), (37), (38), (41), (45), (46), (47), (54), (63), (64), (69), (70), (73), (74), (81), (84), (85), (87), (88), (91), (103), (106), (111), (117), (118), (119), (130), (155), (157), (158), (159), (174), (177), (180), (187), (192), (198), (203), (259), (263)-(271), (278)-(281), (284), (288), (290)-(302), (307), (321), (322), (324), (330), (333)-(335), (341)-(345), (347)-(365), (367)-(371), (373), (386), (388), (393)-(397), (407), (409), (410), (415), (416), (428)-(431), (433)-(438), (440)-(449), (451), (458), (459), (463)-(465), (469)-(476), (480)-(484), (486)-(488), (497), (498), (501), (502), (505), (513), (598) and (599) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 4 (brown paddy plant hopper)

Make paddy growth, until in the 90ml plastic cup second or be cut into identical length 5cm tri-leaf period.Spray the above-mentioned test insecticide solution of 20ml.After air-dry, freely be positioned over brown planthopper (brown paddy plant hopper) larva in length of time in 3 first length of times to the second on the paddy rice and add a cover.After 6 days, check the larva quantity of survival.Calculate by following formula based on the untreated survival rate that checks, and result's exponential representation.4: survival rate 0%, 3: survival rate 1-10%, 2: survival rate 11-40%, 1: survival rate 41-70%, 0: survival rate is greater than 70%

The test larva number of survival rate (%)=(the survival larva number on the paddy rice of processing)/on untreated paddy rice) X 100

Compound (1), (2), (3), (16), (18), (20), (24), (25), (30), (31), (32), (33), (35), (37), (38), (43), (45), (47), (50), (54), (56), (57), (58), (59), (64), (69), (74), (75), (81), (84), (87), (103), (130), (151), (156), (157), (158), (159), (170), (174), (175), (177), (186), (187), (189)-(194), (198), (198), (203), (264)-(268), (280), (281), (284), (286), (288), (290), (292)-(297), (302), (321), (322), (324), (333), (334), (341), (344), (345), (347)-(354), (356)-(364), (367), (368), (370), (386), (388), (393)-(395), (407), (409), (428)-(432), (434)-(438), (441)-(449), (451), (463), (464), (469)-(476), (481), (482), (486)-(488), (490), (491), (497), (505), (513), (598) and (599) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 5 (housefly)

The filter paper that will have an identical diameter lies in (diameter: 5.5cm) at the bottom of the polyethylene cup.After above-mentioned test insecticide solution is added drop-wise on the filter paper with 0.7ml, will spread thereon equably as the 30mg sucrose of food.Be positioned over 10 female adult houseflies (Musca domestica) in the cup and add a cover.After 24 hours, check dead insect numbers.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 70-99%, 2: mortality ratio 40-69%, 1: mortality ratio 10-39%, 0: mortality ratio 0-9%

Mortality ratio (%)={ (dead insect number)/(the insect number of detection) } * 100

Compound (1), (2), (3), (4), (6), (9), (10), (13), (14), (16), (20), (23), (24), (25), (26), (30), (31), (34), (35), (37), (38), (40), (41), (43), (46), (47), (50), (54), (56), (57), (58), (59), (63), (64), (65), (66), (69), (70), (71), (72), (73), (74), (75), (81), (84), (86), (87), (91), (97), (98), (102), (103), (105), (106), (108), (111), (118), (119), (120), (121), (122), (136), (146), (149), (156), (157), (162), (163), (166), (174), (177), (185)-(187), (198), (203)-(205), (234), (259), (263)-(268), (278)-(281), (284), (286)-(302), (304), (305), (307), (321), (324), (332)-(334), (343), (354), (363), (368)-(370), (429)-(432), (434)-(437), (440), (443), (446), (447), (469)-(477), (480), (482), (486)-(488), (490), (497), (498) and (505) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 6 Groton bugs (Blattalla germanica)

The filter paper that will have an identical diameter is tiled in (diameter: 5.5cm) at the bottom of the polyethylene cup.After above-mentioned test insecticide solution is added drop-wise on the filter paper with 0.7ml, will spread thereon equably as the 30mg sucrose of food.Be positioned over 2 male adult Germany cockroach (Groton bug) in the cup and add a cover.After 6 days, check dead insect numbers.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 2: mortality ratio 50%, 0: mortality ratio 0%

Compound (1), (2), (3), (4), (9), (10), (13), (14), (16), (24), (25), (26), (30), (31), (34), (35), (37), (38), (40), (41), (43), (45), (46), (47), (50), (54), (58), (69), (72), (73), (74), (75), (87), (102), (103), (106), (107), (108), (111), (123), (146), (151), (156), (157), (166), (174), (175), (177), (180), (186), (187), (198), (200), (203), (204), (219), (228), (260), (263)-(268), (270)-(272), (274), (278)-(281), (284)-(286), (293), (295), (297), (321), (322), (324), (333), (334), (348), (388), (389), (394), (395), (398), (399), (428)-(449), (451), (452), (454), (456), (462), (463), (467), (469)-(476), (480)-(483), (485)-(487), (490), (495), (497), (501), (502), (505), (513) and (599) to demonstrate index be 4.

Test example 7 culex pipiens pollens (Culex pipiens pallens)

The above-mentioned test insecticide solution of 0.7ml is joined 100ml ion exchanged water (activity component concentration: 3.5ppm).20 common culexs in the final length of time (culex pipiens pollens) are put into water.After 1 day, check dead larva quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 91-100%, 2: mortality ratio 10-90%, 0: mortality ratio 0-10%

Compound (1), (2), (3), (4), (6), (7), (9), (10), (13), (14), (16), (19), (20), (23), (24), (25), (26), (30), (31), (34), (35), (37), (38), (40), (41), (42), (43), (45), (46), (47), (50), (51), (53), (54), (56), (57), (58), (59), (63), (64), (65), (66), (69), (70), (71), (72), (73), (74), (75), (77), (78), (80), (81), (84), (86), (87), (88), (98), (100), (102), (103), (104), (105), (106), (107), (108), (111), (113), (114), (115), (118), (119), (121), (123), (128), (133), (136), (146), (150), (156), (157), (159), (162), (163), (166), (174), (175), (177), (180), (186), (187), (192)-(195), (198)-(201), (203)-(205), (213), (215)-(217), (223), (225)-(229), (234)-(238), (243), (256), (259)-(273), (278)-(281), (284)-(308), (316), (317), (321), (322), (324)-(328), (330)-(336), (338)-(355), (357)-(364), (368)-(370), (382), (385), (386), (388), (392)-(395), (401), (418), (419), (428)-(449), (452)-(455), (459), (465), (466), (469)-(483), (485)-(490), (492), (493), (495)-(497), (501), (502), (505), (507), (513), (598) and (599) to demonstrate index be 4.

Test example 8 Tetranychus urticaes (Tetranychus urticae)

In 3 ounces of cups, plant kidney bean, and grew for 1 week.The kidney bean leaf that many Tetranychus urticaes (Tetranychusurticae) are parasitic is cut and is positioned on the above-mentioned kidney bean leaf, places 1 day.After removing the parasitic kidney bean leaf of many Tetranychus urticaes (Tetranychus urticae), spray the above-mentioned test insecticide solution of 20ml.After 8 days, check the female insects quantity of survival.Result's exponential representation.4: the female insects 0-3 of survival only, 3: the female insects 4-10 of survival only, 2: the female insects 11-20 of survival only, 1: the female insects 21-30 of survival only, 0: the female insects 31 of survival or more than 31

Compound (17), (28), (29), (32), (33), (194), (272), (396), (409), (418), (436), (452), (480), (481), (486), (497), (499) and (501) demonstrate the index more than 3 or 3.

Test example 9 small cabbage moths (Plutella xylostella)

Dimethylbenzene and N with 0.075ml, (dimethylbenzene: (dimethylbenzene: Sorpol (Sorpol) 3005X=1: mixture 9) joins in each test compound of 30mg dinethylformamide for mixture DMF=1: 1) and 0.04ml dimethylbenzene and Sorpol (Sorpol) 3005X (TOHOChemical Industry Co.LTD).This mixture dilute with water is so that activity component concentration reaches 500ppm, with the preparation testing liquid.This testing liquid is applied on the wild cabbage (Brassicae oleracea) of the 4th leaf phase with the speed of every tank 20ml.After air-dry, the over-ground part of wild cabbage is cut, and the over-ground part of wild cabbage is positioned over the polyethylene cup (100ml volume) of the diamondback worm (small cabbage moth) of putting into 5 second length of times.In 25 ℃ of placements.

After 5 days, check dead worm quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

Compound (1), (2), (3), (4), (5), (6), (7), (8), (9), (10), (11), (13), (14), (15), (16), (17), (18), (19), (20), (21), (22), (23), (24), (25), (26), (27), (29), (30), (31), (34), (35), (37), (38), (40), (41), (42), (43), (44), (45), (46), (47), (50), (51), (52), (53), (54), (56), (57), (59), (63), (64), (65), (69), (70), (71), (72), (73), (74), (75), (76), (77), (78), (79), (80), (81), (83), (84), (86), (87), (88), (91), (95), (100), (101), (102), (103), (105), (106), (107), (108), (109), (110), (111), (112), (113), (114), (115), (116), (117), (118), (119), (120), (121), (122), (123), (133), (139), (145), (146), (149), (151), (156), (157), (158), (159), (163), (165), (166), (167), (168), (169), (174), (175), (177), (185), (186), (189), (191), (193), (194), (198)-(205), (211)-(221), (223)-(236), (239)-(242), (245), (247), (248), (252), (254), (256), (258)-(260), (263)-(273), (278)-(282), (284)-(302), (304), (307), (321), (322), (324), (325), (330)-(339), (341)-(371), (373), (375), (377), (379), (380), (386), (388)-(419), (422), (428)-(438), (441)-(449), (451), (452), (454), (457), (458), (462), (463), (465), (466), (469)-(475), (477)-(490), (493), (495)-(502), (505), (507), (513), (598) and (599) demonstrate index more than 3 or 3.Then observe effective insecticidal activity.

Test example 10 Bemisia argentifoliis (Bemisia argentifolii)

With 0.1ml dimethylbenzene and N, (dimethylbenzene: (dimethylbenzene: Sorpol (Sorpol) 3005X=1: mixture 9) joins in each test compound of 40mg dinethylformamide for mixture DMF=1: 1) and 0.04ml dimethylbenzene and Sorpol (Sorpol) 3005X (TOHOChemicalIndustry Co.LTD).This mixture dilute with water is so that activity component concentration reaches normality.In addition, add spreader-sticker (spreader) (Dain:Takeda Pharmaceutical Co.LTD) with 1/3000 amount based on this mixture, with the preparation testing liquid.

In 3 ounces of cups, plant wild cabbage, and grow about 3 weeks.Cut all leaves, but do not comprise the true leaf of two leaf stage.On the true leaf of two leaf stage, place the adult of Bemisia argentifolii (Bemisiaargentifolii) and make it to lay eggs 3 days, then remove adult.Wild cabbage is remained in the greenhouse 8 days.Then testing liquid is sprayed with the amount of every glass of 20ml.After 7 days, check dead worm quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 90-99%, 2: mortality ratio 60-89%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

When the concentration of activeconstituents is 200ppm, compound (1)-(4), (7)-(20), (23), (25), (26), (28)-(35), (37), (38), (40), (41), (43), (45), (46), (50), (51), (53), (54), (56), (58), (59), (63), (69)-(76), (80), (81), (87), (88), (91), (101), (103), (105), (106), (111), (113), (117), (123), (125), (130), (156)-(158), (174), (184)-(187), (189), (193), (194), (200), (202)-(210), (219), (225), (228), (230), (232), (234), (248), (250), (258), (260), (263)-(266), (268)-(271), (278)-(281), (284)-(294), (296), (298), (299), (301), (302), (305), (307), (321), (324), (325), (357), (388), (389), (459), (463), (469)-(476), (469)-(476), (481), (482) and (497) demonstrate index more than 3 or 3.

When the concentration of activeconstituents was 50ppm, compound (21), (24), (344), (348), (350), (352), (355), (358), (360), (364), (368), (394), (395), (398), (430), (436), (442) and (445) demonstrated the index more than 3 or 3.

When the concentration of activeconstituents was 12.5ppm, compound (333) and (431) demonstrated the index more than 3 or 3.

Test example 11 haemaphysalis longicornises (Haemaphysalis longicornis)

Make the 0.5mg test compound be dissolved in 1ml acetone.On the one side of the filter paper of 5cm * 10cm, use equably calcium solution, then air-dry.After this, with the filter paper doubling, fix with paper clip folder (paper clips) in the side, be similar to the shape of bag with formation.10 haemaphysalis longicornises are put into bag, then seal this bag with the paper clip folder.After 2 days, check dead insect numbers.

Compound (1), (2), (3), (4), (24), (26), (28), (29), (35), (37), (43), (45), (48), (50), (51), (52), (54), (59), (63), (69), (75), (77), (80), (88), (101), (102), (103), (104), (106), (107), (111), (113), (118), (119), (120), (121), (122), (123), (130), (146), (156), (186), (187), (188), (189), (195), (207), (208), (264), (265), (266), (267), (278), (280), (284), (321), (324), (333), (334), (341), (428), (429), (430), (431), (433), (434), (435), (441), (442), (443), (446), (447), (469), (470), (471), (472), (473), (474), (475), (469)-(475), (480) and (513) show that mortality ratio is 100%.

Test example 12 small cabbage moths (Plutella xylostella)

Dimethylbenzene and N with 0.1ml, (dimethylbenzene: (dimethylbenzene: Sorpol (Sorpol) 3005X=1: mixture 9) joins in each test compound of 16mg dinethylformamide for mixture DMF=1: 1) and the dimethylbenzene of 0.04ml and Sorpol (Sorpol) 3005X (TOHOChemical Industry Co.LTD).This mixture dilute with water is so that activity component concentration reaches 200ppm.In addition, add spreader-sticker (Dain:Takeda Pharmaceutical Co.LTD) with 1/3000 amount based on this mixture, with the preparation testing liquid.This testing liquid is applied to the wild cabbage (Brassicaeoleracea) of the 5th leaf phase with the speed of every tank 20ml.After air-dry, the diamondback worm (small cabbage moth) in 10 the 3rd length of times is positioned on the wild cabbage, and wild cabbage covers with porose cup.After 5 days, check dead worm quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

Compound (32), (33), (130) and (196) demonstrate the index more than 3 or 3.

Test example 13 (prodenia litura)

0 with .1ml dimethylbenzene and N, (dimethylbenzene: (dimethylbenzene: Sorpol (Sorpol) 3005X=1: mixture 9) joins in each test compound of 16mg dinethylformamide for mixture DMF=1: 1) and 0.04ml dimethylbenzene and Sorpol (Sorpol) 3005X (TOHOChemical Industry Co.LTD).This mixture dilute with water is so that activity component concentration reaches normality.In addition, add spreader-sticker (Dain:Takeda Pharmaceutical Co.LTD) with 1/3000 amount based on this mixture, with the preparation testing liquid.With this testing liquid with the speed of every tank 20ml be applied to the wild cabbage (Brassicae oleracea) of the 5th leaf phase air-dry after, the yellow cutworm (prodenia litura) in 10 the 4th length of times is positioned on the wild cabbage, and wild cabbage covers with porose cup.After 4 days, check dead worm quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

When the concentration of activeconstituents was 200ppm, compound (5), (8), (12), (17), (18), (27), (29), (32), (33), (117), (125), (126), (158) and (196) demonstrated the index more than 3 or 3.

When the concentration of activeconstituents was 50ppm, compound (130) demonstrated the index more than 3 or 3.

Test example fruit leaf roller in 14 summer (Adoxophyes orana)

With 0.1ml dimethylbenzene and N, (dimethylbenzene: (dimethylbenzene: Sorpol (Sorpol) 3005X=1: mixture 9) joins in each test compound of 16mg dinethylformamide for mixture DMF=1: 1) and 0.04ml dimethylbenzene and Sorpol (Sorpol) 3005X (TOHOChemical Industry Co.LTD).This mixture dilute with water is so that activity component concentration reaches normality.In addition, add spreader-sticker (Dain:Takeda Pharmaceutical Co.LTD) with 1/3000 amount based on this mixture, with the preparation testing liquid.The speed of this testing liquid with every tank 20ml is applied on the apple rice shoot with about 12-15cm height that is planted in 3 ounces of cups.After air-dry, the fruit leaf roller in summer (Adoxophyes orana) in about 60 first length of times is positioned on the apple, and this apple is covered with polyethylene cup.After 7 days, check dead larva quantity.Calculate mortality ratio by following formula, and result's exponential representation.4: mortality ratio 100%, 3: mortality ratio 80-99%, 2: mortality ratio 60-79%, 1: mortality ratio 30-59%, 0: mortality ratio 0-29%

Mortality ratio (%)={ (the larva number of test larva number-survival)/(test larva number) } * 100

When the concentration of activeconstituents was 200ppm, compound (5), (8), (12), (17), (18), (27), (117), (125), (126), (131) and (196) demonstrated the index more than 3 or 3.

When the concentration of activeconstituents was 50ppm, compound (29), (154) and (158) demonstrated the index more than 3 or 3.

When the concentration of activeconstituents was 12.5ppm, compound (32), (33) and (130) demonstrated the index more than 3 or 3.

Industrial usability

According to the present invention, compound (I) or its salt is because its control with good antagonism insect is active, thereby is the useful activity composition in the insect-killing composition.

Claims

1. the Iminopropene compound or its salt that are provided by formula (I):

Wherein,

X is OX ¹, NX ²X ³, SX ⁴Or S (O) ₂X ⁵

Wherein, X ¹Be the low alkyl groups that replaced by one or more at least one aryl that is selected from the optional replacement of following independent substituting group: (1) halogen, (2) low alkyl group and (3) lower alkoxy; Or by being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) by the optional low alkyl group that replaces of at least one halogen, (3) lower alkoxy, (4) lower alkoxycarbonyl, (5) lower alkylthio, (6) aryl, (7) cyano group, (8) nitro and (9) alkylenedioxy group

X ³Be low alkyl group or aryl,

X ⁴For by one or more optional low alkyl groups that replace of following substituting group that are selected from: the heterocyclic radical that (1) is replaced by at least one halogen by at least one halogen or the optional aryl that replaces of low alkyl group and (2); Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) nitro, (3) low alkyl group, (4) low-grade halogenated alkyl and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more low alkyl groups, and

X ⁵Be aryl,

Y is OY ¹, NY ²Y ³Or SY ⁴

Wherein, Y ¹Serve as reasons and be selected from the low alkyl group that at least one following substituting group is chosen replacement wantonly: (1) by the optional aryl that replaces of at least one low alkyl group, (2) are by the aryl and (3) heterocyclic radical by at least one halogen replacement of at least one halogen replacement; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) nitro, (4) low alkyl group, (5) amino, (6) lower alkylthio, (7) low alkyl group alkylsulfonyl, (8) low-grade cycloalkyl, (9) aryl, (10) lower alkoxycarbonyl, (11) lower alkoxy, (12) heterocyclic radical, (13) low-grade alkylidene and (14) low-grade alkylidene dioxy base; Heterocyclic radical; Or N=C (Y ¹¹) ₂, Y wherein ¹¹Be low alkyl group or aryl independently of one another;

Y ³Be low alkyl group or aryl,

Y ⁴For by one or more optional low alkyl groups that replace of following substituting group that are selected from: (1) is by the optional aryl that replaces of at least one halogen and (2) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Low-grade alkynyl; By one or more optional aryls that replace of following substituting group that are selected from: (1) halogen, (2) are by the optional low alkyl group that replaces of at least one halogen with by the optional lower alkoxy that replaces of at least one halogen; Or by one or more optional heterocyclic radicals that replace of following substituting group that are selected from: the heterocyclic radical that (1) is replaced by at least one halogen by the optional low alkyl group that replaces of at least one halogen and (2),

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) hydroxyl, (4) by at least one halogen or the optional low alkyl group that replaces of aryl, (5) low-grade alkenyl, (6) by the optional lower alkoxy that replaces of at least one halogen, (7) low-grade alkane acidyl oxygen base, (8) by at least one alkyl or the optional aryl that replaces of halogen, (9) heterocyclic radical, (10) lower alkylthio, (11) low alkyl group sulfinyl, (12) low alkyl group alkylsulfonyl, (13) arylthio, (14) elementary alkoxy carbonyl, (15) low-grade alkane acidyl, (16) aromatic hydrocarbons carbonyl, (17) low-grade alkynyl, (18) rudimentary cycloalkylthio, (19) low-grade alkylidene dioxy base, (20) low-grade alkylidene and (21) nitro; Heterocyclic radical; Lower alkoxycarbonyl; The aromatic hydrocarbons alkylsulfonyl; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; Lower alkoxy by at least one aryl replacement; Or amino by the rudimentary alkylidene of at least one aryl replacement;

Term " lower " means has 6 or the group of carbon atom still less;

Term " senior " means to have the group of 7-20 carbon atom;

Term " aryl " expression phenyl and naphthyl;

Term " heterocyclic radical " expression pyrryl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, dihydropyridine base, pyrimidyl, pyrazinyl, pyridazinyl, triazolyl, tetrazyl, pyrrolidyl, imidazolidyl, piperidyl, piperidino-(1-position only), piperazinyl, indyl, pseudoindoyl, indolinyl, indolyl, benzimidazolyl-, quinolyl, isoquinolyl, indazolyl, benzotriazole base, imidazopyridyl, Imidazothiazole base,

Azoles base, different

The azoles base,

Di azoly, morpholinyl, morpholino, benzo

Azoles base, benzo

Di azoly, thiazolyl, isothiazolyl, thiadiazolyl group, dihydro thiazinyl, thiazolidyl, thio-morpholinyl, thiomorpholine generation, thienyl, dihydro dithiene base, dihydro dithione base, tetrahydro-thienyl, dithiane base, benzothiazolyl, diazosulfide base, imidazo thiadiazolyl group, furyl, dihydro pyranyl, dioxine base, tetrahydrofuran base, THP trtrahydropyranyl, dioxane base, benzofuryl, benzo dioxolanyl, benzo dioxane base, dihydro

Thiophene thiazolinyl, benzothienyl, benzo dithiene base or benzo

The thiophene thiazolinyl.

2. according to the compound of claim 1, wherein

X is SX ⁴

Wherein, X ⁴Serve as reasons and be selected from the low alkyl group of the optional replacement of at least one following substituting group: (1) is by at least one halogen or the optional aryl that replaces of low alkyl group and (2) heterocyclic radical by the optional replacement of at least one halogen; Senior alkyl; Low-grade alkenyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen atom, (2) nitro, (3) low alkyl group, (4) low-grade halogenated alkyl and (5) lower alkoxy; Or by the optional heterocyclic radical that replaces of one or more low alkyl groups,

Y is OY ¹, NY ²Y ³Or SY ⁴

Wherein, Y ¹Serve as reasons and be selected from the low alkyl group that at least one following substituting group is chosen replacement wantonly: aryl and (3) heterocyclic radical by at least one halogen replacement that (1) is replaced by at least one halogen by the optional aryl that replaces of at least one low alkyl group, (2); By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) cyano group, (3) nitro, (4) low alkyl group, (5) amino, (6) lower alkylthio, (7) low alkyl group alkylsulfonyl, (8) low-grade cycloalkyl, (9) aryl, (10) lower alkoxycarbonyl, (11) lower alkoxy, (12) heterocyclic radical, (13) low-grade alkylidene and (14) low-grade alkylidene dioxy base; Heterocyclic radical;

Y ³Be low alkyl group,

Y ⁴Serve as reasons and be selected from the optional low alkyl group that replaces of at least one following substituting group: (1) is by the optional aryl that replaces of at least one halogen and (2) low-grade cycloalkyl; Senior alkyl; Low-grade cycloalkyl; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by optional low alkyl group, (3) lower alkoxy and (4) elementary halogenated alkoxy that replaces of at least one halogen; By being selected from the optional heterocyclic radical that replaces of following one or more independently substituting groups: (1) low alkyl group, (2) low-grade halogenated alkyl and (3) heterocyclic radical by at least one halogen replacement; By the optional low-grade alkenyl that replaces of at least one halogen; Senior thiazolinyl; Or low-grade alkynyl,

The Z low alkyl group that at least one halogen replaces of serving as reasons; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) nitro, (3) cyano group, (4) low alkyl group, (5) lower alkoxy and (6) low-grade halogenated alkyl; Heterocyclic radical; Lower alkoxycarbonyl; The aromatic hydrocarbons alkylsulfonyl; By the amino aryl replacement and chosen wantonly replacement by low alkyl group; The virtue-oxyl; By the lower alkoxy of at least one aryl replacement, or amino by the rudimentary alkylidene of at least one aryl replacement.

3. according to the compound of claim 1, wherein

X is OX ¹

Wherein, X ¹Be the low alkyl groups that replaced by one or more at least one aryl that is selected from the optional replacement of following independent substituting group: (1) halogen, (2) low alkyl group and (3) lower alkoxy; By being selected from the optional aryl that replaces of following one or more independently substituting groups: (1) halogen, (2) are by optional low alkyl group, (3) lower alkoxy, (4) lower alkoxycarbonyl, (5) lower alkylthio, (6) aryl, (7) cyano group, (8) nitro and (9) alkylenedioxy group that replaces of at least one halogen;

Y is OY ¹Or SY ⁴

Wherein, Y ¹The low alkyl group that at least one aryl replaces of serving as reasons, or by being selected from the optional aryl that replaces of following one or more independently substituting groups: halogen and low alkyl group,

Y ⁴The optional low alkyl group that replaces of at least one aryl of serving as reasons, or aryl,

4. insect-killing composition, it comprises the compound or its salt according to claim 1 as activeconstituents, and inert support.

5. the method for a Control pests, it comprises the step that the compound or its salt according to claim 1 of significant quantity is applied to insect or insect habitat.

6. according to the compound or its salt of claim 1 purposes in insect control.