JP5131783B2 - Amine derivatives having NPYY5 receptor antagonistic activity and uses thereof - Google Patents

Description

  The compound used in the present invention has NPY Y5 receptor antagonistic activity, and the present invention is useful as an appetite suppressant or anti-obesity agent.

Obesity is classified according to its cause into primary obesity (simple obesity) and secondary obesity (symptomatic obesity). Possible causes of primary obesity include excessive intake of energy (for example, overeating), insufficient use of energy (for example, insufficient exercise), and reduced heat production. Currently, over 90% of obesity is primary obesity. If this primary obesity develops and persists, it causes various health problems. On the other hand, secondary obesity is obesity caused by some underlying disease. For example, endocrine obesity, hypothalamic obesity, hereditary obesity, or drug-based obesity. Obesity is an incentive for adult diseases, and it is easy to combine diabetes, hypertension, hyperlipidemia, coronary sclerosis (angina, myocardial infarction), ventilation, cholelithiasis, fatty liver, infertility and osteoarthritis Become.
The basis of obesity treatment is a combination of diet therapy and exercise therapy, but this has limitations, and drug therapy is expected to be effective particularly for severe obesity.
It is suggested that Y5 receptor, which is a subtype of neuropeptide Y (hereinafter referred to as NPY) receptor, is involved in at least the feeding function, and its antagonist becomes an anti-obesity drug (non-patent document). 1).

  An amine derivative having a sulfonyl group having an NPY Y5 receptor antagonistic activity having a structure similar to that of the compound according to the present invention is described in Patent Document 1, Patent Document 2, Patent Document 3, Patent Document 4, Non-Patent Document 1, and the like. Has been. In addition, Patent Literature 5, Patent Literature 8, Patent Literature 9, Patent Literature 10, and Patent Literature 11 describe that amide derivatives having a sulfonyl group have NPY Y5 antagonistic activity. Patent Document 12 also describes a derivative having a sulfonyl group having an NPY Y5 receptor antagonistic action. Patent Documents 15 and 16 also describe amine derivatives having a sulfonyl group having a similar structure to the compound according to the present invention and having an NPY Y5 receptor antagonistic action. These compounds differ in structure from the compounds used in the present invention.

  Moreover, although the compound which has a similar structure with the compound which concerns on this invention is described in patent document 6, patent document 7, patent document 13, patent document 14, etc., an effect | action differs completely, an antifeedant and There is no description useful as an anti-obesity drug, and it does not suggest the present invention.

International Publication No. 01/002379 Pamphlet International Publication No. 00/064880 Pamphlet WO99 / 055667 pamphlet International Publication No. 00/068197 Pamphlet International Publication No. 01/037826 Pamphlet International Publication No. 2006/014482 Pamphlet International Publication No. 2005/0973838 Pamphlet International Publication No. 97/20823 Pamphlet US Patent Application Publication No. 2006/293341 International Publication No. 2007/002126 Pamphlet International Publication No. 2006/001318 Pamphlet International Publication No. 2005/080348 Pamphlet US Patent Application Publication No. 2007/060598 Pamphlet International Publication No. 2005/121107 Pamphlet International Publication No. 2007/125595 International Publication No. 2008/134228 Pamphlet

Peptides, Vol. 18, 445 (1997) European Journal of Medicinal Chemistry, 2006, 42 (4), pp. 463-470

  An object of the present invention is to provide an excellent appetite suppressant or anti-obesity agent.

  As a result of intensive studies, the present inventors have succeeded in synthesizing a novel compound having the following excellent NPY Y5 receptor antagonistic activity. An amide derivative having a sulfonyl group is known in Patent Document 5 as a compound having an NPY Y5 receptor antagonistic action. However, the present inventors have found that a compound in which an amide derivative is an amine derivative is greatly improved in brain migration as compared with a compound before substitution. In addition, it was confirmed that the compound used in the present invention is a compound that hardly induces a drug metabolizing enzyme as compared with the compounds described in Patent Documents 1 and 2. About these novel compounds, the feeding suppression effect confirmation test, the body weight suppression effect confirmation test, etc. were performed, and it confirmed having having an eating suppression effect and a body weight suppression effect, and completed this invention. It has also been found that the compounds used in the present invention have good metabolic stability and water solubility. Further, the present inventors have found that the compound used in the present invention is a sufficiently safe compound for use as a medicine, which has low toxicity such as anemia-inducing action and does not cause reproductive toxicity and gastrointestinal tract disorders.

［式中、Ｒ^１は置換基を有していてもよい低級アルキルであり、
Ｙは−Ｓ(Ｏ)ｎ−（ｎは１または２である）または−ＣＯ−であり、
Ｒ^２は水素または置換基を有していてもよい低級アルキルであり、
Ｒ^１およびＲ^２は一緒になって低級アルキレンを形成してもよく、
Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、
Ｘは
置換基を有していてもよい低級アルキレン、
置換基を有していてもよい低級アルケニレン、
置換基を有していてもよい−ＣＯ−低級アルキレン、
置換基を有していてもよい−ＣＯ−低級アルケニレンまたは

（式中、Ｒ^３、Ｒ^４、Ｒ^５およびＲ^６は各々独立して水素または置換基を有していてもよい低級アルキルであり、

は置換基を有していてもよいシクロアルキレン、置換基を有していてもよいシクロアルケニレン、置換基を有していてもよいビシクロアルキレン、置換基を有していてもよいアリーレンまたは置換基を有していてもよいヘテロ環ジイルであり、ｐおよびｑは各々独立して０〜２の整数であり、ｐおよびｑのいずれか一方は０ではない）
であり、
−ＮＲ^２−Ｘ−は

（式中、

はピペリジンジイル、ピペラジンジイル、ピリジンジイル、ピラジンジイル、ピロリジンジイルまたはピロールジイルであり、Ｕは低級アルキレンまたは低級アルケニレンである）であってもよく、
Ｚは置換基を有していてもよい低級アルキル、置換基を有していてもよい低級アルケニル、置換基を有していてもよいアミノ、置換基を有していてもよい低級アルコキシ、置換基を有していてもよい炭化水素環式基、置換基を有していてもよいヘテロ環式基である、
（但し、Ｚは３環の縮合へテロ環式基、置換基を有していてもよいチアゾリルまたは置換基を有していてもよいキナゾリニルではない）］
である化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（２）Ｒ^１が低級アルキルである、（１）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（３）Ｙが−Ｓ(Ｏ)_２−である、（１）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（４）Ｚが置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である、（１）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（５）Ｘが

であり、Ｒ^１が置換基を有していてもよい炭素数２〜１０のアルキルである、（１）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（６）Ｚが置換基を有していてもよいヘテロ環式基である、（５）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（７）

が置換基を有していてもよいシクロアルキレン、置換基を有していてもよいシクロアルケニレン、置換基を有していてもよいビシクロアルキレンまたは置換基を有していてもよいピペリジニレンである、（５）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（８）

が置換基を有していてもよいシクロへキシレンまたは置換基を有していてもよいピペリジニレンであり、
ｐおよびｑは各々独立して０または1であり、ｐおよびｑのいずれか一方は０ではない、（５）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（９）Ｚが置換基を有していてもよい低級アルキル、置換基を有していてもよいフェニル、置換基を有していてもよいピリジル、置換基を有していてもよいピラゾリル、置換基を有していてもよいイソオキサゾリル、置換基を有していてもよいオキサジアゾリル、置換基を有していてもよいピリダジニル、置換基を有していてもよいピラジニル、置換基を有していてもよいピリミジニルまたは置換基を有していてもよい２環の縮合へテロ環である、（７）または（８）に記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１０）Ｘが

であり、ｐ＋ｑが１または２である、（１）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１１）ｐ＋ｑが１である、（１０）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１２）式（Ｉ）：

［式中、Ｒ^１は置換基を有していてもよい低級アルキルであり、
Ｙは−Ｓ(Ｏ)_２−であり、
Ｒ^２は水素または置換基を有していてもよい低級アルキルであり、
Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、
Ｘは

（式中、Ｒ^５およびＲ^６は各々独立して水素であり、

は置換基を有していてもよいシクロアルキレンであり、ｐは０であり、ｑは１または２である）であり、
Ｚは置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である］
である化合物（但し、Ｚが３環の縮合へテロ環式基である化合物を除く）、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１３）Ｚが置換基を有していてもよいフェニル、置換基を有していてもよいインダニル、置換基を有していてもよいピリジル、置換基を有していてもよいピリダジニル、置換基を有していてもよいピリミジニル、置換基を有していてもよいピラゾリル、置換基を有していてもよいイソオキサゾリル、置換基を有していてもよいオキサジアゾリルまたは置換基を有していてもよい２環の縮合へテロ環である、（１２）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１４）Ｚが置換基を有していてもよいイソキノリル、置換基を有していてもよいベンゾチアゾリル、置換基を有していてもよいベンゾオキサゾリル、置換基を有していてもよいベンゾピリジル、置換基を有していてもよいベンゾピリダジル、置換基を有していてもよいベンゾイミダゾリル、置換基を有していてもよいチアゾロピリジル、置換基を有していてもよいイソキサゾリノニル、置換基を有していてもよいオキサゾリノニル、置換基を有していてもよいベンズオキサジノニルまたは置換基を有していてもよいベンゾキシアゼピノニルである、（１２）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１５）式（Ｉ）：

［式中、Ｒ^１は置換基を有していてもよい低級アルキルであり、
Ｙは−Ｓ(Ｏ)_２−であり、
Ｒ^２は水素または置換基を有していてもよい低級アルキルであり、
Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、
Ｘは

（式中、Ｒ^３およびＲ^４は各々独立して水素であり、

は置換基を有していてもよいシクロアルキレンであり、ｐは１または２であり、ｑは０である）であり、
Ｚは置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である］
である化合物（但し、Ｚが３環の縮合へテロ環式基、置換基を有していてもよいチアゾリルまたは置換基を有していてもよいキナゾリニルである化合物を除く）、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１６）Ｚが置換基を有していてもよいフェニル、置換基を有していてもよいピリジル、置換基を有していてもよいピリダジニル、置換基を有していてもよいピラジニル、置換基を有していてもよいピリミジニル、置換基を有していてもよいキノリル、置換基を有していてもよいイソキノリル、置換基を有していてもよいベンゾチアゾリル、置換基を有していてもよいベンズイミダゾリル、置換基を有していてもよいベンズオキサゾリル、置換基を有していてもよいチアゾロピリジルまたは置換基を有していてもよいオキサゾロピリジルである、（１５）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１７）式（Ｉ）：

［式中、Ｒ^１は置換基を有していてもよい低級アルキルであり、
Ｙは−Ｓ(Ｏ)_２−であり、
Ｒ^２は水素または置換基を有していてもよい低級アルキルであり、
Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、
Ｘは

（式中、Ｒ^３およびＲ^４は各々独立して水素であり、

は置換基を有していてもよいシクロアルキレンであり、ｐは１または２であり、ｑは０である）であり、
Ｚは置換基を有していてもよいフェニル、置換基を有していてもよいピリジル、置換基を有していてもよいピリダジニル、置換基を有していてもよいピラジニル、置換基を有していてもよいピリミジニル、置換基を有していてもよいキノリル、置換基を有していてもよいイソキノリル、置換基を有していてもよいベンゾチアゾリル、置換基を有していてもよいベンズイミダゾリル、置換基を有していてもよいベンズオキサゾリル、置換基を有していてもよいチアゾロピリジルまたは置換基を有していてもよいオキサゾロピリジルである］である化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（１８）式：

で示される化合物、その製薬上許容される塩またはそれらの溶媒和物。
（１９）上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する医薬組成物。
（２０）上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有するＮＰＹ Ｙ５受容体拮抗作用を有する医薬組成物。
（２１）上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。
（２２）上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を投与する食欲の抑制方法。
（２３）上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を投与する肥満の予防または治療方法。
（２４）食欲抑制剤または抗肥満薬を製造するための 上記（１８）記載の化合物、その製薬上許容される塩またはそれらの溶媒和物の使用。 That is, the present invention relates to the following.
(1) Formula (I):

[Wherein, R ¹ is optionally substituted lower alkyl,
Y is -S (O) n- (n is 1 or 2) or -CO-
R ² is hydrogen or optionally substituted lower alkyl,
R ¹ and R ² together may form a lower alkylene,
R ⁷ is hydrogen or optionally substituted lower alkyl,
X is a lower alkylene which may have a substituent,
Lower alkenylene which may have a substituent,
-CO-lower alkylene which may have a substituent,
Optionally substituted -CO-lower alkenylene or

(Wherein R ³ , R ⁴ , R ⁵ and R ⁶ are each independently hydrogen or lower alkyl optionally having substituent (s);

Is an optionally substituted cycloalkylene, an optionally substituted cycloalkenylene, an optionally substituted bicycloalkylene, an optionally substituted arylene or a substituent And p and q are each independently an integer of 0 to 2, and one of p and q is not 0)
And
—NR ² —X— is

(Where

May be piperidinediyl, piperazinediyl, pyridinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl and U is lower alkylene or lower alkenylene)
Z is optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted amino, optionally substituted lower alkoxy, substituted A hydrocarbon cyclic group which may have a group, a heterocyclic group which may have a substituent,
(However, Z is not a tricyclic condensed heterocyclic group, an optionally substituted thiazolyl or an optionally substituted quinazolinyl)]
An appetite suppressant or anti-obesity drug comprising a compound, a pharmaceutically acceptable salt thereof or a solvate thereof.
(2) An appetite suppressant or anti-obesity drug containing the compound according to (1), pharmaceutically acceptable salt or solvate thereof, wherein R ¹ is lower alkyl.
(3) An appetite suppressant or anti-obesity drug containing the compound according to (1), pharmaceutically acceptable salt or solvate thereof, wherein Y is —S (O) ₂ —.
(4) The compound according to (1), a pharmaceutically acceptable salt thereof, wherein Z is a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent. Or an appetite suppressant or anti-obesity drug containing a solvate thereof.
(5) X is

And R ¹ is an optionally substituted alkyl having 2 to 10 carbon atoms, the compound according to (1), a pharmaceutically acceptable salt thereof or a solvate thereof containing an appetite suppressant Agent or anti-obesity agent.
(6) An appetite suppressant or anti-obesity containing the compound according to (5), a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Z is a heterocyclic group which may have a substituent. medicine.
(7)

Is an optionally substituted cycloalkylene, an optionally substituted cycloalkenylene, an optionally substituted bicycloalkylene, or an optionally substituted piperidinylene. (5) An appetite suppressant or anti-obesity drug containing the compound, pharmaceutically acceptable salt or solvate thereof according to (5).
(8)

Is optionally substituted cyclohexylene or optionally substituted piperidinylene,
p and q are each independently 0 or 1, and any one of p and q is not 0. An appetite containing the compound according to (5), a pharmaceutically acceptable salt thereof, or a solvate thereof. Inhibitors or anti-obesity drugs.
(9) Z may have a lower alkyl optionally having a substituent, phenyl optionally having a substituent, pyridyl optionally having a substituent, pyrazolyl optionally having a substituent, Isoxazolyl which may have a substituent, oxadiazolyl which may have a substituent, pyridazinyl which may have a substituent, pyrazinyl which may have a substituent, having a substituent The compound according to (7) or (8), a pharmaceutically acceptable salt thereof, or a solvate thereof, which is an optionally pyrimidinyl group or an optionally substituted bicyclic condensed heterocyclic ring. Contains an appetite suppressant or anti-obesity agent.
(10) X is

And an appetite suppressant or anti-obesity drug containing the compound according to (1), a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein p + q is 1 or 2.
(11) An appetite suppressant or anti-obesity drug containing the compound according to (10), a pharmaceutically acceptable salt thereof, or a solvate thereof, wherein p + q is 1.
(12) Formula (I):

[Wherein, R ¹ is optionally substituted lower alkyl,
Y is —S (O) ₂ —;
R ² is hydrogen or optionally substituted lower alkyl,
R ⁷ is hydrogen or optionally substituted lower alkyl,
X is

Wherein R ⁵ and R ⁶ are each independently hydrogen,

Is an optionally substituted cycloalkylene, p is 0, and q is 1 or 2.
Z is a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent]
An appetite suppressant or anti-obesity drug containing a compound wherein Z is a compound in which Z is a three-ring fused heterocyclic group, a pharmaceutically acceptable salt thereof, or a solvate thereof.
(13) Z may be optionally substituted phenyl, optionally substituted indanyl, optionally substituted pyridyl, optionally substituted pyridazinyl, substituted Pyrimidinyl which may have a group, pyrazolyl which may have a substituent, isoxazolyl which may have a substituent, oxadiazolyl which may have a substituent or a substituent An appetite suppressant or anti-obesity drug containing the compound according to (12), a pharmaceutically acceptable salt thereof, or a solvate thereof, which is a fused bicyclic heterocyclic ring.
(14) Z may have an isoquinolyl which may have a substituent, benzothiazolyl which may have a substituent, benzoxazolyl which may have a substituent, or may have a substituent Benzopyridyl, optionally substituted benzopyridyl, optionally substituted benzimidazolyl, optionally substituted thiazolopyridyl, optionally substituted isoxazolyl The compound according to (12), which is nonyl, optionally substituted oxazolinonyl, optionally substituted benzoxazinonyl or optionally substituted benzoxyazepinonyl. , An appetite suppressant or anti-obesity drug containing a pharmaceutically acceptable salt or solvate thereof.
(15) Formula (I):

[Wherein, R ¹ is optionally substituted lower alkyl,
Y is —S (O) ₂ —;
R ² is hydrogen or optionally substituted lower alkyl,
R ⁷ is hydrogen or optionally substituted lower alkyl,
X is

Wherein R ³ and R ⁴ are each independently hydrogen,

Is an optionally substituted cycloalkylene, p is 1 or 2, and q is 0),
Z is a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent]
A compound wherein Z is a condensed heterocyclic group having 3 rings, thiazolyl optionally having substituent (s) or quinazolinyl optionally having substituent (s), and pharmaceutically acceptable thereof Appetite suppressant or anti-obesity drug containing the salt or solvate thereof.
(16) Z is optionally substituted phenyl, optionally substituted pyridyl, optionally substituted pyridazinyl, optionally substituted pyrazinyl, substituted Pyrimidinyl which may have a group, quinolyl which may have a substituent, isoquinolyl which may have a substituent, benzothiazolyl which may have a substituent, Benzimidazolyl which may be substituted, benzoxazolyl which may have a substituent, thiazolopyridyl which may have a substituent or oxazolopyridyl which may have a substituent, (15) Appetite suppressant or anti-obesity agent comprising the described compound, a pharmaceutically acceptable salt thereof or a solvate thereof.
(17) Formula (I):

[Wherein, R ¹ is optionally substituted lower alkyl,
Y is —S (O) ₂ —;
R ² is hydrogen or optionally substituted lower alkyl,
R ⁷ is hydrogen or optionally substituted lower alkyl,
X is

Wherein R ³ and R ⁴ are each independently hydrogen,

Is an optionally substituted cycloalkylene, p is 1 or 2, and q is 0),
Z is an optionally substituted phenyl, an optionally substituted pyridyl, an optionally substituted pyridazinyl, an optionally substituted pyrazinyl, and an optionally substituted substituent. Pyrimidinyl which may have a substituent, Quinolyl which may have a substituent, Isoquinolyl which may have a substituent, Benzothiazolyl which may have a substituent, Benz which may have a substituent Imidazolyl, optionally substituted benzoxazolyl, optionally substituted thiazolopyridyl or optionally substituted oxazolopyridyl], and its pharmaceutical An appetite suppressant or anti-obesity drug containing a top acceptable salt or a solvate thereof.
(18) Formula:

Or a pharmaceutically acceptable salt or solvate thereof.
(19) A pharmaceutical composition comprising the compound according to (18) above, a pharmaceutically acceptable salt thereof or a solvate thereof.
(20) A pharmaceutical composition having an NPY Y5 receptor antagonistic action, comprising the compound according to (18) above, a pharmaceutically acceptable salt thereof, or a solvate thereof.
(21) An appetite suppressant or anti-obesity drug containing the compound according to (18) above, a pharmaceutically acceptable salt thereof or a solvate thereof.
(22) A method for suppressing appetite, comprising administering the compound according to (18), a pharmaceutically acceptable salt thereof, or a solvate thereof.
(23) A method for preventing or treating obesity, comprising administering the compound according to (18) above, a pharmaceutically acceptable salt thereof, or a solvate thereof.
(24) Use of the compound of the above (18), a pharmaceutically acceptable salt thereof or a solvate thereof for producing an appetite suppressant or anti-obesity agent.

で示される化合物、その製薬上許容される塩またはそれらの溶媒和物。
（１−２）式：

で示される化合物、その製薬上許容される塩またはそれらの溶媒和物。
（１−３）式：

で示される化合物、その製薬上許容される塩またはそれらの溶媒和物。
（１−４）（１−１）〜（１−３）のいずれかに記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する医薬組成物。
（１−５）ＮＰＹ Ｙ５受容体拮抗作用を有する（１−４）記載の医薬組成物。
（１−６）（１−１）〜（１−３）のいずれかに記載の化合物、その製薬上許容される塩またはそれらの溶媒和物を含有する食欲抑制剤または抗肥満薬。 Specifically, the present invention relates to the following.
(1-1) Formula:

Or a pharmaceutically acceptable salt or solvate thereof.
(1-2) Formula:

Or a pharmaceutically acceptable salt or solvate thereof.
(1-3) Formula:

Or a pharmaceutically acceptable salt or solvate thereof.
(1-4) A pharmaceutical composition comprising the compound according to any one of (1-1) to (1-3), a pharmaceutically acceptable salt thereof, or a solvate thereof.
(1-5) The pharmaceutical composition according to (1-4), which has an NPY Y5 receptor antagonistic action.
(1-6) An appetite suppressant or anti-obesity drug containing the compound according to any one of (1-1) to (1-3), a pharmaceutically acceptable salt thereof, or a solvate thereof.

  The compounds used in the present invention exhibit NPY Y5 receptor antagonism, and the present invention relates to pharmaceuticals, in particular, appetite suppressants or anti-obesity for the treatment and / or prevention of eating disorders, obesity, anorexia nervosa Very useful as a medicine.

  The terms used in this specification will be described below. In the present specification, each term has the same meaning whether used alone or in combination with other terms.

  “Halogen” includes fluorine, chlorine, bromine and iodine. In particular, fluorine and chlorine are preferable.

  Protecting groups for “optionally protected hydroxy” and “optionally protected hydroxy lower alkyl” include all commonly used hydroxy protecting groups. For example, acyl (acetyl, trichloroacetyl, benzoyl etc.), lower alkoxycarbonyl (t-butoxycarbonyl etc.), lower alkylsulfonyl (methanesulfonyl etc.), lower alkoxy lower alkyl (methoxymethyl etc.), trialkylsilyl (t-butyldimethyl) Silyl etc.).

“Lower alkyl” includes linear or branched alkyl having 1 to 10 carbon atoms, such as methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, Examples include n-pentyl, isopentyl, neopentyl, hexyl, isohexyl, n-heptyl, isoheptyl, n-octyl, isooctyl, n-nonyl and n-decyl.
“Lower alkyl” in R ¹ is preferably 2 to 10 carbon atoms, more preferably 2 to 6 carbon atoms, and most preferably ethyl, isopropyl or t-butyl.

  “Lower alkyl” in other cases preferably has 1 to 6 carbon atoms, more preferably 1 to 4 carbon atoms.

（式中、Ｒ^１０およびＲ^１１は各々独立して水素または低級アルキルであり、２以上のＲ^１０および／またはＲ^１１が存在するとき、各々のＲ^１０およびＲ^１１は異なっていてもよく、
Ｗは単結合、Ｏ、ＳまたはＮＲ^１２であり、
Ｒ^１２は水素、低級アルキルまたはフェニルであり、

はそれぞれ下記に定義する置換基群αから選択される１以上の置換可能な基で置換されていてもよいシクロアルキル、ビシクロアルキル、シクロアルケニル、アリールまたはヘテロ環式基であり、
ｓは０〜４の整数）
で示される基等が挙げられる。 Examples of the substituent of “lower alkyl optionally having substituent (s)” for Z include (1) halogen; (2) cyano;
(3) (i) hydroxy, (ii) lower alkoxy, (iii) mercapto, (iv) lower, each optionally substituted with one or more substitutable groups selected from the substituent group β defined below Alkylthio, (v) acyl, (vi) acyloxy, (vii) carboxy, (viii) lower alkoxycarbonyl, (ix) imino, (x) carbamoyl, (xi) thiocarbamoyl, (xii) lower alkylcarbamoyl, (xiii) Lower alkylthiocarbamoyl, (xiv) amino, (xv) lower alkylamino or (xvi) heterocyclic carbonyl; or
Equation (4):

Wherein R ¹⁰ and R ¹¹ are each independently hydrogen or lower alkyl, and when two or more R ¹⁰ and / or R ¹¹ are present, each R ¹⁰ and R ¹¹ may be different,
W is a single bond, O, S or NR ¹² ,
R ¹² is hydrogen, lower alkyl or phenyl;

Are each a cycloalkyl, bicycloalkyl, cycloalkenyl, aryl or heterocyclic group optionally substituted with one or more substitutable groups selected from the substituent group α defined below,
s is an integer of 0 to 4)
Group etc. which are shown by these are mentioned.

Here, the substituent group α is (1) halogen; (2) oxo; (3) cyano; (4) nitro; (5) imino optionally substituted with lower alkyl or hydroxy;
(6) (i) hydroxy, (ii) lower alkyl, (iii) lower alkenyl, (iv) lower alkoxy, each optionally substituted with one or more substitutable groups selected from substituent group β v) carboxy, (vi) lower alkoxycarbonyl, (vii) acyl, (viii) acyloxy, (ix) imino, (x) mercapto, (xi) lower alkylthio, (xii) carbamoyl, (xiii) lower alkylcarbamoyl, xiv) cycloalkylcarbamoyl, (xv) thiocarbamoyl, (xvi) lower alkylthiocarbamoyl, (xvii) lower alkylsulfinyl, (xviii) lower alkylsulfonyl, (xix) sulfamoyl, (xx) lower alkylsulfamoyl and (xxi) Cycloalkylsulfamoyl;
(7) Substituent group β, lower alkyl, lower alkoxy lower alkyl, optionally protected hydroxy lower alkyl, halogeno lower alkyl, lower alkylsulfonyl and / or arylsulfonyl, respectively, (i) Cycloalkyl, (ii) cycloalkenyl, (iii) cycloalkyloxy, (iv) amino and (v) alkylenedioxy; and
(8) (i) phenyl, (ii) naphthyl, (iii) phenoxy, (iv) phenyl lower alkoxy, (v) each optionally substituted with substituent group β, lower alkyl, halogeno lower alkyl and / or oxo. ) Phenylthio, (vi) phenyl lower alkylthio, (vii) phenylazo, (viii) heterocyclic group, (ix) heterocyclic oxy, (x) heterocyclic thio, (xi) heterocyclic carbonyl and (xii) heterocyclic sulfonyl A group consisting of

Preferred examples of the substituent group α as a substituent in the ring B are halogen; nitro; hydroxy;
Lower alkyl optionally having substituent (wherein the substituent is halogen, cyano, phenyl, carboxy and / or lower alkoxycarbonyl);
Lower alkenyl; lower alkoxycarbonyl lower alkenyl;
Lower alkoxy which may have a substituent (wherein the substituent is halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino and / or cyano);
Hydroxyimino; lower alkylthio; lower alkylsulfinyl; sulfamoyl;
Optionally substituted amino (wherein the substituent is lower alkyl, optionally protected hydroxy lower alkyl, phenyl and / or acyl);
Cyanophenyl; heterocycle-substituted phenyl; biphenylyl; phenoxy; phenylazo optionally substituted with lower alkyl;
Optionally substituted heterocyclic group (wherein the substituent may be protected hydroxy; mercapto; halogen; lower alkyl; cycloalkyl; lower alkoxycarbonyl; amino; lower alkoxycarbonylamino; carbamoyl) Oxo; phenyl; lower alkoxyphenyl; or a heterocyclic group), more preferably halogen; lower alkyl optionally substituted with halogen; lower alkoxy optionally substituted with halogen.

  Substituent group β is halogen, optionally protected hydroxy, mercapto, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl, cyano, A group consisting of cycloalkyl, phenyl, phenoxy, lower alkylphenyl, lower alkoxyphenyl, halogenophenyl, naphthyl and heterocyclic groups.

Examples of the substituent of “lower alkyl optionally having a substituent” other than Z (for example, in the case of R ¹ ) include one or more groups selected from the substituent group β, and an arbitrary position is It may be substituted with these substituents.

  “Lower alkoxy”, “lower alkoxycarbonyl”, “lower alkoxycarbonyl lower alkyl”, “lower alkylphenyl”, “lower alkoxyphenyl”, “lower alkylcarbamoyl”, “lower alkylthiocarbamoyl”, “lower alkylamino”, “ “Halogeno lower alkyl”, “hydroxy lower alkyl”, “phenyl lower alkoxy”, “lower alkylthio”, “phenyl lower alkylthio”, “lower alkoxycarbonylamino”, “lower alkoxycarbonyl lower alkenyl”, “lower alkylsulfinyl”, “ The lower alkyl part of “lower alkylsulfonyl”, “aryl lower alkoxycarbonyl”, “lower alkylbenzoyl” and “lower alkoxybenzoyl” is the same as the above “lower alkyl”.

  Examples of the substituent of “lower alkoxy optionally having substituent (s)” include one or more groups selected from substituent group β, preferably phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl or heterocyclic ring Formula group.

  “Cycloalkyl” includes cyclic alkyl having 3 to 8 carbon atoms, preferably 5 or 6 carbon atoms. Specific examples include cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl.

  Examples of the substituent of “optionally substituted cycloalkyl” include one or more groups selected from the substituent group α, and any position may be substituted.

  “Bicycloalkyl” includes a group formed by removing one hydrogen from an aliphatic ring having 5 to 8 carbon atoms in which two rings share two or more atoms. Specific examples include bicyclo [2.1.0] pentyl, bicyclo [2.2.1] heptyl, bicyclo [2.2.2] octyl and bicyclo [3.2.1] octyl.

  “Lower alkenyl” is a straight or branched alkenyl having 2 to 10 carbon atoms, preferably 2 to 8 carbon atoms, more preferably 3 to 6 carbon atoms, having one or more double bonds at any position. Is included. Specific examples include vinyl, propenyl, isopropenyl, butenyl, isobutenyl, prenyl, butadienyl, pentenyl, isopentenyl, pentadienyl, hexenyl, isohexenyl, hexadienyl, heptenyl, octenyl, nonenyl and decenyl.

  The “lower alkenyl” moiety in the “lower alkoxycarbonyl-lower alkenyl” is the same as the above “lower alkenyl”.

  The substituent of “optionally substituted lower alkenyl” includes halogen, lower alkoxy, lower alkenyl, amino, lower alkylamino, lower alkoxycarbonylamino, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, carbamoyl. , Cyano, cycloalkyl, phenyl, lower alkylphenyl, lower alkoxyphenyl, naphthyl and / or heterocyclic group.

  “Acyl” means (1) straight or branched alkylcarbonyl or alkenylcarbonyl having 1 to 10 carbon atoms, more preferably 1 to 6 carbon atoms, most preferably 1 to 4 carbon atoms, and (2) carbon number. It includes 4 to 9, preferably 4 to 7 carbon cycloalkylcarbonyl and (3) aryl carbonyl having 7 to 11 carbon atoms. Specific examples include formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, pivaloyl, hexanoyl, acryloyl, propioyl, methacryloyl, crotonoyl, cyclopropylcarbonyl, cyclohexylcarbonyl, cyclooctylcarbonyl and benzoyl.

  The acyl part of “acyloxy” is the same as above.

  “Cycloalkenyl” includes those having one or more double bonds at any position in the ring of the cycloalkyl, specifically, cyclopropenyl, cyclobutenyl, cyclopentenyl, cyclohexenyl and cyclohexenyl. Sadienyl and the like can be mentioned.

  Examples of the substituent of “optionally substituted cycloalkenyl” include one or more groups selected from substituent group β.

  Examples of the substituent of the “optionally substituted amino” include the substituent group β, the optionally substituted benzoyl and / or the optionally substituted heterocyclic carbonyl (here And the substituent includes hydroxy, lower alkyl, lower alkoxy and / or lower alkylthio).

  “Aryl” is a monocyclic or polycyclic aromatic carbocyclic group, and includes phenyl, naphthyl, anthryl, phenanthryl and the like. Also included are aryls fused with other non-aromatic hydrocarbon cyclic groups, and specific examples include indanyl, indenyl, biphenylyl, acenaphthyl, tetrahydronaphthyl and fluorenyl. Particularly preferred is phenyl.

The same applies to the aryl moiety of “aryl lower alkoxycarbonyl”.
The “optionally substituted aryl” and the “optionally substituted phenyl” in Z are one or more substitutable groups selected from the substituent group α and the substituent group α. It includes “aryl” and “phenyl” which may be substituted with lower alkyl which may be substituted.

  Examples of the substituent of “optionally substituted aryl” and “optionally substituted phenyl” other than Z include one or more groups selected from the substituent group β.

  The “hydrocarbon cyclic group” includes the above “cycloalkyl”, “cycloalkenyl”, “bicycloalkyl” and “aryl”.

  The “non-aromatic hydrocarbon cyclic group” includes the above “cycloalkyl”, “cycloalkenyl” and “bicycloalkyl”.

  The “hydrocarbon cyclic group which may have a substituent” means the above “cycloalkyl which may have a substituent”, “cycloalkenyl which may have a substituent”, “substitution” It includes “bicycloalkyl which may have a group” and “aryl which may have a substituent”.

  "Heterocyclic group" includes a heterocycle having one or more heteroatoms arbitrarily selected from O, S and N, specifically pyrrolyl, imidazolyl, pyrazolyl, pyridyl, pyridazinyl, pyrimidinyl 5- to 6-membered heteroaryl such as pyrazinyl, triazolyl, triazinyl, tetrazolyl, isoxazolyl, oxazolyl, oxadiazolyl, isothiazolyl, thiazolyl, thiadiazolyl, furyl and thienyl; indolyl, isoindolyl, indazolyl, indolizinyl, indolinyl, isoindolinyl, quinolyl, isoquinolyl, Cinnolinyl, phthalazinyl, quinazolinyl, naphthyridinyl, quinoxalinyl, purinyl, pteridinyl, benzopyranyl, benzimidazolyl, benzisoxazolyl, benzo Sazolyl, benzoxiadiazolyl, benzoisothiazolyl, benzothiazolyl, benzothiadiazolyl, benzofuryl, isobenzofuryl, benzothienyl, benzotriazolyl, imidazopyridyl, triazolopyridyl, imidazothiazolyl, pyrazinopyridazini , Tetrahydroquinolyl, tetrahydrobenzothienyl, oxazolopyridyl, thiazolopyridyl (eg, thiazolo [5,4-b] pyridin-2-yl, thiazolo [5,4-c] pyridin-2-yl, thiazolo [ 4,5-b] pyridin-2-yl, thiazolo [4,5-c] pyridin-2-yl, etc.), benzoxazolinonyl, benzisoxazolinonyl, benzoxazinonyl, benzoxyazepinonyl, Bicyclic fused heterocyclic groups such as oxazolopyridinonyl, benzodioxolyl; carbazolyl, acridinyl, xanthenyl Tricyclic fused heterocyclic groups such as phenothiazinyl, phenoxathinyl, phenoxazinyl, dibenzofuryl; dioxanyl, thiylyl, oxiranyl, oxathiolanyl, azetidinyl, thianyl, pyrrolidinyl, pyrrolinyl, imidazolidinyl, imidazolinyl, pyrazolidinyl, pyrazolinyl, piperidyl , Non-aromatic heterocyclic groups such as morpholinyl, morpholino, thiomorpholinyl, thiomorpholino, dihydropyridyl, tetrahydrofuryl, tetrahydropyranyl, tetrahydrothiazolyl, tetrahydroisothiazolyl and the like.

  A condensed heterocyclic group condensed with a ring other than a heterocyclic ring (for example, benzothiazolyl) may have a bond on any ring.

  The substituents of “heterocyclic group which may have a substituent” and “bicyclic fused heterocyclic group which may have a substituent” may be the above-mentioned “having a substituent. Same as “good aryl”.

  The heterocyclic group moiety of “heterocyclic carbonyl”, “heterocyclic oxy”, “heterocyclic thio” and “heterocyclic substituted phenyl” is the same as the above “heterocyclic group”.

  “Lower alkylene” includes a divalent group in which 1 to 6, preferably 2 to 6, and more preferably 3 to 6 methylenes are continuous. Specifically, methylene, ethylene, trimethylene, tetra Examples include methylene, pentamethylene and hexamethylene. Particularly preferred is tetramethylene.

を形成する場合を包含する。好ましくは

である。 When R ¹ and R ² together form a lower alkylene,

The case of forming is included. Preferably

It is.

  The lower alkylene part of “lower alkylenedioxy” is the same as the above “lower alkylene”, preferably methylenedioxy or ethylenedioxy.

  “Lower alkenylene” is a divalent group in which 2 to 6, preferably 3 to 6, more preferably 4 to 5 methylenes are continuous, and at least one of the carbon-carbon bonds is a double bond. Is included.

  “Cycloalkylene” is a divalent group formed by removing one hydrogen atom from the above “cycloalkyl”. The “cycloalkylene” in X is preferably 1,4-cyclohexanediyl.

  The “cycloalkenylene” includes a group having at least one double bond in the ring of the cycloalkylene.

  “Bicycloalkylene” includes a group formed by removing one hydrogen from the above “bicycloalkyl”. Specific examples include bicyclo [2.1.0] pentylene, bicyclo [2.2.1] heptylene, bicyclo [2.2.2] octylene, bicyclo [3.2.1] octylene.

  The “heterocyclic diyl” includes a divalent group formed by removing one hydrogen atom from the above “heterocyclic group”. Preferred are piperidine diyl, piperazine diyl, pyridine diyl, pyrimidine diyl, pyrazine diyl, pyrrolidine diyl or pyrrole diyl, and more preferred is piperidine diyl.

  “Arylene” includes a divalent group formed by removing one hydrogen atom from the above “aryl”. Preferable is phenylene.

  The “heteroarylene” includes those having the aromatic attribute among the above “heterocyclic diyl”. Specifically, pyrrole diyl, imidazole diyl, pyrazole diyl, pyridine diyl, pyridazine diyl, pyrimidine diyl, pyrazine diyl, triazole diyl, triazine diyl, isoxazole diyl, oxazole diyl, oxadiazole diyl, isothiazole diyl, thiazole diyl, thiadiazole diyl , Flangedyl and thiophenediyl.

である場合、好ましくはＵがメチレン、エチレンであり、さらに好ましくは

である。 “Lower alkylene optionally having substituent”, “lower alkenylene optionally having substituent”, “cycloalkylene optionally having substituent”, “having substituent” May be substituted cyclohexylene ”,“ bicycloalkylene optionally having substituent ”,“ cycloalkenylene optionally having substituent ”,“ phenylene optionally having substituent ”,“ substituent ” Examples of the substituent of “optionally substituted heterocyclic diyl” and “optionally substituted piperidinylene” include one or more substitutable groups selected from the substituent group β, Is halogen, hydroxy, lower alkyl, halogeno lower alkyl, lower alkoxy, amino, lower alkylamino, acyl, carboxy, lower alkoxycarbonyl or the like. Any position may be substituted with these groups.
—NR ² —X— is

And preferably U is methylene or ethylene, more preferably

It is.

［式中、Ｒ^１は低級アルキルであり、
Ｙは−Ｓ(Ｏ)_２−であり、
Ｒ^２は水素であり、
Ｒ^７は水素であり、
Ｘは

（式中、Ｒ^３およびＲ^４は各々独立して水素であり、

はシクロアルキレンであり、ｐは１であり、ｑは０である）であり、
Ｚは置換基を有していてもよいピラゾリル、置換基を有していてもよいベンゾチアゾリルまたは置換基を有していてもよいベンズオキサゾリルである］である化合物。
さらには、以下に記載の化合物が好ましい。

As the compound according to the present invention, the following compounds are preferable.
Formula (I):

[Wherein R ¹ is lower alkyl,
Y is —S (O) ₂ —;
R ² is hydrogen;
R ⁷ is hydrogen;
X is

Wherein R ³ and R ⁴ are each independently hydrogen,

Is cycloalkylene, p is 1 and q is 0),
Z is an optionally substituted pyrazolyl, an optionally substituted benzothiazolyl, or an optionally substituted benzoxazolyl].
Furthermore, the compounds described below are preferred.

  The above-mentioned compound has an excellent feature that it exhibits a body weight-suppressing action at a low dose.

  The compound according to the present invention includes a pharmaceutically acceptable salt capable of producing each compound. “Pharmaceutically acceptable salts” include, for example, salts of inorganic acids such as hydrochloric acid, sulfuric acid, nitric acid or phosphoric acid; salts of organic acids such as paratoluenesulfonic acid, methanesulfonic acid, oxalic acid or citric acid; ammonium, Examples include salts of organic bases such as trimethylammonium or triethylammonium; salts of alkali metals such as sodium or potassium; and salts of alkaline earth metals such as calcium or magnesium.

  The compound according to the present invention includes its solvate and is directed to compound (I). Preferably, it is a hydrate, and one molecule of the compound according to the present invention may be coordinated with an arbitrary number of water molecules.

  When the compound (I) according to the present invention has an asymmetric carbon atom, it includes racemates, both enantiomers and all stereoisomers (geometric isomers, epimers, enantiomers, etc.). In addition, when the compound (I) according to the present invention has a double bond, both of the E-form and the Z-form can be present. In addition, when X is cycloalkylene, both cis and trans forms are included.

Compound (I) according to the present invention can be synthesized, for example, by the following method. Hereinafter, the X _-CH 2 -G-, or -G-CH ₂ - is described as.

（式中、Ｈａｌはハロゲンであり、−Ｇ−ＣＨ_２−は式（Ｉ）の−Ｘ−と同義であり、Ｒ^１３は低級アルキルであり、その他の記号は前記と同義である）
工程Ａ
化合物１と目的化合物に対応する置換基Ｒ^１を有するスルホニルハライド２と適当な溶媒中、０℃〜５０℃で数分〜数時間反応させればｎが２である化合物３が得られる。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジエチルエーテル、ジクロロメタン、トルエン、ベンゼン、キシレン、シクロヘキサン、へキサン、クロロホルム、酢酸エチル、酢酸ブチル、ペンタン、ヘプタン、ジオキサン、アセトン、アセトニトリルおよびそれらの混合溶媒等が使用可能である。

工程Ｂ
化合物１と置換基Ｒ^１を有するスルフィニルハライド４を反応させてｎ＝１である化合物５を得ることもできる。反応条件は上記工程Ａと同様である。

工程Ｃ
工程Ｂで得られた化合物５を常法により酸化反応に付せば、ｎ＝２である化合物３が得られる。酸化剤としてはｍ−クロロ過安息香酸、過酢酸、過酸化水素、過トリフルオロ酢酸、過よう素酸ナトリウム、次亜塩素酸ナトリウム、過マンガン酸カリウム等を使用することができ、反応は０℃〜５０℃で行えばよい。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジエチルエーテル、ジクロロメタン、トルエン、ベンゼン、キシレン、シクロヘキサン、へキサン、クロロホルム、酢酸エチル、酢酸ブチル、ペンタン、ヘプタン、ジオキサン、アセトン、アセトニトリル、水、メタノール、エタノール、イソプロパノールおよびそれらの混合溶媒等を用いることができる。

工程Ｄ
工程ＡあるいはＣで得た化合物３を適当な溶媒中、塩基で処理し、化合物６を得る。塩基としては水酸化バリウム、水酸化ナトリウム、水酸化カリウム、ヒドラジン、プロパンチオールリチウム塩等を用いることができ、溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジオキサン、アセトン、アセトニトリル、メタノール、エタノール、プロパノール、水およびそれらの混合溶媒等が使用可能である。０℃〜１００℃で数分〜数十時間反応させればよい。

工程Ｅ
工程Ｄで得られた化合物６と目的化合物に対応する置換基ＺおよびＲ^７を有するアミノ化合物７を適当な溶媒中、０℃〜５０℃で数分〜数時間反応させて化合物８を得る。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジエチルエーテル、ジクロロメタン、トルエン、ベンゼン、キシレン、シクロヘキサン、へキサン、クロロホルム、酢酸エチル、酢酸ブチル、ペンタン、ヘプタン、ジオキサン、アセトン、アセトニトリルおよびそれらの混合溶媒等が使用可能であり、必要であれば塩化チオニル、酸ハロゲン化物、酸無水物、活性化エステル等の活性化剤を用いてもよい。

工程Ｆ
得られた化合物８を適当な溶媒中、適当な還元剤で処理し、化合物(I−Ａ)を得る。還元剤としては水素化ホウ素ナトリウム、水素化ホウ素リチウム、水素化リチウムアルミニウム等を用いることができ、溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジオキサン、アセトニトリル、メタノール、エタノール、プロパノール、酢酸およびそれらの混合溶媒等が使用可能である。０℃〜１００℃で数分〜数十時間反応させればよい。

工程Ｇ
工程Ｄで得られた化合物６を適当な溶媒中、還元剤で処理し、化合物９を得る。還元剤としては水素化ホウ素ナトリウム、水素化ホウ素リチウム、水素化リチウムアルミニウム、ジボラン等を用いることができ、溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジオキサン、アセトニトリル、メタノール、エタノール、プロパノールおよびそれらの混合溶媒等が使用可能である。０℃〜１００℃で数分〜数十時間反応させればよく、必要であれば酸ハロゲン化物、酸無水物、活性化エステル等の中間体を経由してもよい。

工程Ｈ
工程Ｇで得られた化合物９を常法により酸化反応に付せば、化合物１０が得られる。酸化剤としてはｍ−クロロ過安息香酸、過酢酸、過酸化水素、過トリフルオロ酢酸、過よう素酸ナトリウム、次亜塩素酸ナトリウム、過マンガン酸カリウム、デス‐マーチン過よう素酸、ジメチルスルホキシド/オキサリルクロライド（Swern酸化）、ルテニウム触媒等を使用することができ、反応は−８０℃〜５０℃で行えばよい。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジエチルエーテル、ジクロロメタン、トルエン、ベンゼン、キシレン、シクロヘキサン、へキサン、クロロホルム、酢酸エチル、酢酸ブチル、ペンタン、ヘプタン、ジオキサン、アセトン、アセトニトリル、水、メタノール、エタノール、イソプロパノールおよびそれらの混合溶媒等を用いることができる。

工程J
得られた化合物１０と目的化合物に対応する置換基ＺおよびＲ^７を有するアミノ化合物７を常法により還元的アミノ化反応に付せば、化合物(Ｉ−Ａ)が得られる。還元剤としては水素化ホウ素ナトリウム、トリアセトキシ水素化ホウ素ナトリウム、シアノ水素化ホウ素ナトリウム等を使用することができ、反応は０℃〜５０℃で行えばよい。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジオキサン、アセトニトリル、メタノール、エタノール、プロパノール、酢酸、塩酸およびそれらの混合溶媒等を用いることができる。 [When Y = S (O) n]

(In the formula, Hal is halogen, -G-CH ₂ -has the same meaning as -X- in formula (I), R ¹³ is lower alkyl, and the other symbols are as defined above).
Process A
When compound 1 and sulfonyl halide 2 having substituent R ¹ corresponding to the target compound are reacted in an appropriate solvent at 0 ° C. to 50 ° C. for several minutes to several hours, compound 3 in which n is 2 is obtained. As the solvent, tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, and mixed solvents thereof can be used. It is.

Process B
Compound 5 in which n = 1 can also be obtained by reacting compound 1 with sulfinyl halide 4 having substituent R ¹ . The reaction conditions are the same as in step A above.

Process C
If compound 5 obtained in step B is subjected to an oxidation reaction by a conventional method, compound 3 where n = 2 is obtained. As the oxidizing agent, m-chloroperbenzoic acid, peracetic acid, hydrogen peroxide, pertrifluoroacetic acid, sodium periodate, sodium hypochlorite, potassium permanganate and the like can be used, and the reaction is 0 What is necessary is just to perform at 50 degreeC. Solvents include tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, methanol, ethanol, isopropanol and A mixed solvent thereof or the like can be used.

Process D
Compound 6 obtained in Step A or C is treated with a base in an appropriate solvent to give Compound 6. As the base, barium hydroxide, sodium hydroxide, potassium hydroxide, hydrazine, propanethiol lithium salt and the like can be used, and as the solvent, tetrahydrofuran, dimethylformamide, dioxane, acetone, acetonitrile, methanol, ethanol, propanol, water and A mixed solvent thereof or the like can be used. What is necessary is just to make it react for several minutes-dozens of hours at 0 to 100 degreeC.

Process E
Compound 8 obtained by reacting compound 6 obtained in step D with amino compound 7 having substituents Z and R ⁷ corresponding to the target compound at 0 ° C. to 50 ° C. for several minutes to several hours in an appropriate solvent is obtained. As the solvent, tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, and mixed solvents thereof can be used. If necessary, an activating agent such as thionyl chloride, acid halide, acid anhydride, or activated ester may be used.

Process F
The obtained compound 8 is treated with a suitable reducing agent in a suitable solvent to obtain a compound (IA). As the reducing agent, sodium borohydride, lithium borohydride, lithium aluminum hydride and the like can be used, and as the solvent, tetrahydrofuran, dimethylformamide, dioxane, acetonitrile, methanol, ethanol, propanol, acetic acid, and mixed solvents thereof, etc. Can be used. What is necessary is just to make it react for several minutes-dozens of hours at 0 to 100 degreeC.

Process G
Compound 9 obtained in Step D is treated with a reducing agent in a suitable solvent to obtain Compound 9. As the reducing agent, sodium borohydride, lithium borohydride, lithium aluminum hydride, diborane, etc. can be used, and as the solvent, tetrahydrofuran, dimethylformamide, dioxane, acetonitrile, methanol, ethanol, propanol, and mixed solvents thereof, etc. Can be used. The reaction may be carried out at 0 ° C. to 100 ° C. for several minutes to several tens of hours. If necessary, intermediates such as acid halides, acid anhydrides and activated esters may be used.

Process H
Compound 10 is obtained by subjecting compound 9 obtained in step G to an oxidation reaction by a conventional method. As oxidizing agents, m-chloroperbenzoic acid, peracetic acid, hydrogen peroxide, pertrifluoroacetic acid, sodium periodate, sodium hypochlorite, potassium permanganate, Dess-Martin periodate, dimethyl sulfoxide / Oxalyl chloride (Swern oxidation), a ruthenium catalyst, and the like can be used, and the reaction may be performed at -80 ° C to 50 ° C. Solvents include tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, water, methanol, ethanol, isopropanol and A mixed solvent thereof or the like can be used.

Process J
Compound (IA) is obtained by subjecting the resulting compound 10 and amino compound 7 having substituents Z and R ⁷ corresponding to the target compound to a reductive amination reaction by a conventional method. As the reducing agent, sodium borohydride, sodium triacetoxyborohydride, sodium cyanoborohydride and the like can be used, and the reaction may be performed at 0 ° C to 50 ° C. As the solvent, tetrahydrofuran, dimethylformamide, dioxane, acetonitrile, methanol, ethanol, propanol, acetic acid, hydrochloric acid, a mixed solvent thereof or the like can be used.

（式中、各記号は前記と同義であり、−Ｇ−ＣＨ_２− は式（Ｉ）の −Ｘ− と同義である）

工程Ｋ
化合物１と目的化合物に対応する置換基Ｒ^１を有するアシルハライド１１と適当な溶媒中、−２０℃〜５０℃で数分〜数時間反応させれば化合物１２が得られる。溶媒としてはテトラヒドロフラン、ジメチルホルムアミド、ジエチルエーテル、ジクロロメタン、トルエン、ベンゼン、キシレン、シクロヘキサン、へキサン、クロロホルム、酢酸エチル、酢酸ブチル、ペンタン、ヘプタン、ジオキサン、アセトン、アセトニトリルおよびそれらの混合溶媒等が使用可能である。

工程Ｄ、工程Ｇ、工程Ｈおよび工程Ｊ
こうして得られた化合物１２を上記工程Ｄ、工程Ｇ、工程Ｈおよび工程Ｊと同様の方法に付せば本発明に係る化合物（Ｉ-Ｂ）を得ることができる。 [When Y = CO]

(In the formula, each symbol has the same meaning as described above, and -G-CH ₂ -has the same meaning as -X- in formula (I)).

Process K
Compound 12 can be obtained by reacting compound ¹ with acyl halide 11 having substituent R ¹ corresponding to the target compound in an appropriate solvent at −20 ° C. to 50 ° C. for several minutes to several hours. As the solvent, tetrahydrofuran, dimethylformamide, diethyl ether, dichloromethane, toluene, benzene, xylene, cyclohexane, hexane, chloroform, ethyl acetate, butyl acetate, pentane, heptane, dioxane, acetone, acetonitrile, and mixed solvents thereof can be used. It is.

Process D, Process G, Process H and Process J
The compound (IB) according to the present invention can be obtained by subjecting the compound 12 thus obtained to the method similar to the above Step D, Step G, Step H and Step J.

（式中、各記号は前記と同意義であり、−ＣＨ_２−Ｇ−は式（Ｉ）の−Ｘ−と同義であり、Ｒはアルキル）
工程Ｌ
化合物１６に、置換基Ｒ^７を導入する工程である。例えば、Ｒ^７Ｘ^１(Ｘ^１はハロゲン)を塩基存在下で反応させることにより、化合物１７を得ることができる。溶媒としては、テトラヒドロフラン、ジメチルホルムアミドを使用することができる。反応は、室温で行うことができる。塩基としては、トリエチルアミン、ピリジン、ジメチルアミノピリジン等を用いることができる。なお、式（Ｉ-Ｃ）において、Ｒ^７が水素である化合物は、本工程を行わない。

工程Ｍ
化合物１７に置換基Ｚを導入する工程である。例えば、ＺＸ^１(Ｘ^１はハロゲン)を塩基存在下で反応させることにより、化合物１８を得ることができる。溶媒としては、メタノール、エタノール、イソプロパノール、ジメチルホルムアミド等を用いることができる。反応は、室温下または加温下で行うことができる。例えば、封管し、マイクロウェ−ブ反応装置を用いて行うこともできる。塩基としては、Ｎ,Ｎ-ジイソプロピルエチルアミン等を用いることができる。

工程Ｎ
化合物１８を還元し、化合物１９を得る工程である。還元剤として、水素化リチウムアルミニウムを用いることができる。溶媒としては、テトラヒロドフラン等を用いることができる。反応は、室温で行うことができる。

工程Ｏ
化合物１９をアジド化して、化合物２０に誘導する工程である。例えば、化合物１９に、塩基としてトリエチルアミンを用い、メタンスルホニルクロライドを反応させて、化合物１９をメシレートに誘導する。メシル化する際の溶媒としては、クロロホルムを用いることができる。得られた化合物に、アジ化ナトリウムを反応させ、ジメチルホルムアミド中等で、室温下または加温下で、アジド化を行い、化合物２０を得ることができる。

工程Ｐ
化合物２０を還元し、化合物２１を得る工程である。接触還元で行うことができる。触媒としては、１０％パラジウム炭素等を用いることができる。溶媒としては、エタノール等を用いることができる。

工程Ｑ
化合物２１に、式：Ｒ^１−Ｙ−Ｘ^１（Ｘ^１はハロゲン等、ＹはＳ、ＳＯ、ＳＯ_２またはＣＯである）で示される化合物を反応させ、化合物２２を得る工程である。式：Ｒ^１−Ｙ−Ｘ^１で示される化合物として、各種のスルホニルクロライド、スルフィニルクロライド、アシルクロライド等を用いることができる。溶媒としては、テトラヒドロフラン、ジメチルホルムアミド等を用いることができる。反応は、室温下または加温下で行うことができる。塩基の存在下で行うのが好ましく、塩基としては、ピリジン、トリエチルアミン等を用いることができる。なお、式（Ｉ−Ｃ）において、Ｒ^２が水素である化合物は、以降の工程Ｒを行わず、化合物２２が最終目的化合物となる。また、Ｙ＝ＳまたはＳＯである式：Ｒ^１−Ｙ−Ｘ^１で示される化合物を用いて反応させ、化合物２２を得て、その後に酸化して、ＹがＳＯ_２である化合物に変換し、次の工程に用いても良い。

工程Ｒ
化合物２２に、置換基Ｒ^２を導入する工程である。Ｒ^２Ｘ^１（Ｘ^１はハロゲン等）を塩基存在下で化合物２２に反応させることにより、化合物（Ｉ−Ｃ）を得ることができる。塩基としては、水素化ナトリウム等を用いることができる。溶媒としては、ジメチルホルムアミド等を用いることができる。

(In the formula, each symbol is as defined above, —CH ₂ —G— is synonymous with —X— in formula (I), and R is alkyl)
Process L
In this step, substituent R ⁷ is introduced into compound 16. For example, compound 17 can be obtained by reacting R ⁷ X ¹ (X ¹ is halogen) in the presence of a base. Tetrahydrofuran and dimethylformamide can be used as the solvent. The reaction can be carried out at room temperature. As the base, triethylamine, pyridine, dimethylaminopyridine and the like can be used. Note that in the formula (IC), this step is not performed for compounds in which R ⁷ is hydrogen.

Process M
In this step, the substituent Z is introduced into the compound 17. For example, compound 18 can be obtained by reacting ZX ¹ (X ¹ is halogen) in the presence of a base. As the solvent, methanol, ethanol, isopropanol, dimethylformamide, or the like can be used. The reaction can be carried out at room temperature or under warming. For example, it can be sealed and sealed using a microwave reactor. As the base, N, N-diisopropylethylamine or the like can be used.

Process N
In this step, compound 18 is reduced to obtain compound 19. As a reducing agent, lithium aluminum hydride can be used. Tetrahydrofuran or the like can be used as the solvent. The reaction can be carried out at room temperature.

Process O
In this step, compound 19 is azidated to give compound 20. For example, compound 19 is reacted with methanesulfonyl chloride using triethylamine as a base to induce compound 19 to mesylate. As a solvent for the mesylation, chloroform can be used. The obtained compound is reacted with sodium azide and azidated in dimethylformamide or the like at room temperature or under heating to obtain compound 20.

Process P
In this step, compound 20 is reduced to obtain compound 21. It can be carried out by catalytic reduction. As the catalyst, 10% palladium carbon or the like can be used. As the solvent, ethanol or the like can be used.

Process Q
In this step, compound 21 is reacted with a compound represented by the formula: R ¹ —Y—X ¹ (X ¹ is halogen or the like, Y is S, SO, SO ₂ or CO) to obtain compound 22. As the compound represented by the formula: R ¹ —Y—X ¹ , various sulfonyl chlorides, sulfinyl chlorides, acyl chlorides, and the like can be used. As the solvent, tetrahydrofuran, dimethylformamide, or the like can be used. The reaction can be carried out at room temperature or under warming. The reaction is preferably performed in the presence of a base, and pyridine, triethylamine, or the like can be used as the base. In the formula (IC), the compound in which R ² is hydrogen does not perform the subsequent step R, and the compound 22 is the final target compound. Alternatively, the compound represented by the formula: R ¹ —Y—X ^{1 in} which Y═S or SO is reacted to obtain a compound 22, which is then oxidized to be converted into a compound in which Y is SO _2. You may use for the following process.

Process R
In this step, substituent R ² is introduced into compound 22. Compound (IC) can be obtained by reacting R ² X ¹ (X ¹ is halogen or the like) with compound 22 in the presence of a base. As the base, sodium hydride or the like can be used. As the solvent, dimethylformamide or the like can be used.

（式中、Ｒは置換基を有していてもよい低級アルキルであり、Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、Ｇは1,4-シクロアルキレンであり、Ｚは置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である）
Ｒとしては、特に、低級アルキル、さらには、メチル、エチルが好ましい。特にエチルが好ましい。
Ｒ^７としては、水素が好ましい。
Ｚとしては、置換基を有していてもよいヘテロ環式基が好ましい。
特に、以下の化合物が好ましい。
式：

（式中、Ｒ^１５はＮＨ_２またはＯＨであり、
Ｚは置換基を有していてもよいピリジル、置換基を有していてもよいピリダジニル、置換基を有していてもよいピラジニル、置換基を有していてもよいピリミジニル、置換基を有していてもよいキノリル、置換基を有していてもよいイソキノリル、置換基を有していてもよいベンゾチアゾリル、置換基を有していてもよいベンゾオキサゾリル、置換基を有していてもよいベンゾピリジル、置換基を有していてもよいベンゾピリダジル、置換基を有していてもよいベンズイミダゾリル、置換基を有していてもよいベンズオキサゾリル、置換基を有していてもよいチアゾロピリジル置換基を有していてもよいイソキサゾリノニル、置換基を有していてもよいオキサゾリノニル、置換基を有していてもよいベンズオキサジノニルまたは置換基を有していてもよいベンゾキシアゼピノニルである）で示される化合物。 In the above steps, the following intermediates are useful.

Wherein R is optionally substituted lower alkyl, R ⁷ is hydrogen or optionally substituted lower alkyl, G is 1,4-cycloalkylene, Z is a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent.
R is particularly preferably lower alkyl, more preferably methyl or ethyl. Ethyl is particularly preferable.
R ⁷ is preferably hydrogen.
Z is preferably a heterocyclic group which may have a substituent.
In particular, the following compounds are preferable.
formula:

Wherein R ¹⁵ is NH ₂ or OH;
Z is pyridyl which may have a substituent, pyridazinyl which may have a substituent, pyrazinyl which may have a substituent, pyrimidinyl which may have a substituent, and a substituent. Quinolyl which may have a substituent, isoquinolyl which may have a substituent, benzothiazolyl which may have a substituent, benzoxazolyl which may have a substituent, Benzopyridyl which may have a substituent, benzopyridazyl which may have a substituent, benzimidazolyl which may have a substituent, benzoxazolyl which may have a substituent, which may have a substituent Good thiazolopyridyl substituent optionally having isoxazolinonyl, optionally having oxazolinonyl, optionally having benzoxazinonyl or having a substituent Compounds represented by have a good benzoxycarbonyl azelate Pinot sulfonyl be).

（式中、各記号は前記と同意義であり、−ＣＨ_２−Ｇ−は式（Ｉ）の−Ｘ−と同義であり、Ｒはアルキル、Ｐｒｏはアミノ保護基である）

工程Ｓ
化合物１７に、保護基を導入する工程である。保護基としては、広く、Protective Groups in Organic Synthesis(Theodra W. Greene著)等に記載の保護基を用いることができる。酸性条件下で除去することができるアミノ保護基が好ましい。ベンジルオキシカルボニル基、tert-ブチルオキシカルボニル基等があげられる。例えば、ＰｒｏＸ^１（Ｘ^１はハロゲン等、Ｐｒｏはベンジルオキシカルボニル基、tert-ブチルオキシカルボニル等）、Ｐｒｏ−Ｏ−Ｐｒｏ（Ｐｒｏはベンジルオキシカルボニル基、tert-ブチルオキシカルボニル等）を塩基存在下で反応させることにより、化合物２３を得ることができる。溶媒としては、テトラヒドロフラン、ジメチルホルムアミドを使用することができる。反応は、室温で行うことができる。塩基としては、トリエチルアミン、ピリジン、ジメチルアミノピリジン等を用いることができる。なお、Ｒ^７が水素の化合物でも、同様に反応を行うことができる。

工程Ｔ
化合物２３を還元し、化合物２４を得る工程である。還元剤として、水素化リチウムアルミニウムを用いることができる。溶媒としては、テトラヒロドフラン等を用いることができる。反応は、室温で行うことができる。

工程Ｕ
化合物２４をアジド化して、化合物２５に誘導する工程である。例えば、化合物２４に、塩基としてトリエチルアミンを用い、メタンスルホニルクロライドを反応させて、化合物２４をメシレートに誘導する。メシル化する際の溶媒としては、クロロホルムを用いることができる。得られた化合物に、アジ化ナトリウムを反応させ、ジメチルホルムアミド中等で、室温下または加温下で、アジド化を行い、化合物２５を得ることができる。

工程Ｖ
化合物２５を還元し、化合物２６を得る工程である。化合物２５を、トリフェニルホスフィン及び水を用いて、還元することにより、化合物２６を得る。反応は、加温下で行うことができる。溶媒としては、テトラヒドロフランを用いることができる。トリフェニルホスフィンを用いた還元法以外にも、接触還元で行うことができる。接触還元の場合は、触媒としては、１０％パラジウム炭素などを用いることができる。溶媒としては、エタノールなどを用いることができる。いずれの還元法を用いるかは、使用する保護基により、適宜選択することができる。

工程Ｗ
化合物２６に、式：Ｒ^１−Ｙ−Ｘ^１（Ｘ^１はハロゲン等、ＹはＳ、ＳＯ、ＳＯ_２またはＣＯである）で示される化合物を反応させ、化合物２７を得る工程である。式：Ｒ^１−Ｙ−Ｘ^１（Ｘ^１はハロゲン等）で示される化合物として、各種のスルホニルクロライド、スルフィニルクロライド、アシルクロライド等を用いることができる。溶媒としては、テトラヒドロフラン、ジメチルアミド等を用いることができる。反応は、室温下または加温下で行うことができる。塩基の存在下で行うのが好ましく、塩基としては、ピリジン、トリエチルアミン等を用いることができる。また、Ｙ＝ＳまたはＳＯである式：Ｒ^１−Ｙ−Ｘ^１で示される化合物を用いて反応させ、化合物２７を得て、その後に酸化して、ＹがＳＯ_２である化合物に変換し、次の工程に用いても良い。

工程Ｘ
化合物２７の保護基を除去する工程である。保護基の除去は、保護基によって各種の条件を選択して用いることができる。例えば、tert-ブチルオキシカルボニル基は酸ではずすことができる。ベンジルオキシカルボニル基は、接触還元等ではずすことができる。

工程Ｙ
化合物２８に置換基Zを導入する工程である。例えば、ＺＸ^１（Ｘ^１はハロゲン）を塩基存在下で反応させることにより、化合物（Ｉ−Ｄ）を得ることができる。溶媒としては、メタノール、エタノール、イソプロパノール、ジメチルホルムアミド等を用いることができる。反応は、室温下または加温下で行うことができる。例えば、封管し、マイクロウェ−ブ反応装置を用いて行うこともできる。塩基としては、Ｎ,Ｎ-ジイソプロピルエチルアミン等を用いることができる。

上記の工程において、以下の中間体は有用である。

（式中、Ｒは置換基を有していてもよい低級アルキルであり、Ｐｒｏは保護基であり、Ｒ^７は水素または置換基を有していてもよい低級アルキルであり、Ｇは1,4-シクロアルキレンであり、ＹはＳＯ_２またはＳＯであり、Ｒ^１は置換基を有していてもよい低級アルキルであり、Ｒ^２は水素または置換基を有していてもよい低級アルキルである）
Ｒとしては、特に、低級アルキル、さらには、メチル、エチルが好ましい。特にエチルが好ましい。
Ｐｒｏとしては、酸性条件下で除去することができるアミノ保護基が好ましい。例えば、Ｐｒｏとしては、式：−（Ｃ＝Ｏ）-Ｏ-Ｒ（Ｒは置換基を有していてもよい低級アルキル、置換基を有していてもよい低級アルケニル）で示される基が好ましい。特に、tert-ブチルオキシカルボニル基が好ましい。
Ｒ^７としては、水素が好ましい。
Ｙとしては、ＳＯ_２が好ましい。
Ｒ^１としては、特に、低級アルキル、さらには、イソプロピル、エチル、tert-ブチルが好ましい。特にtert-ブチルが好ましい。
Ｒ^２としては、水素が好ましい。
特に、以下の化合物が好ましい。
式：

（式中、Ｒ^１はエチルまたはtert-ブチルである）で示される化合物。
式：

（式中、Ｒ^１はエチル、イソプロピルまたはtert-ブチルである）で示される化合物。
式：

（式中、Ｚは置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である）で示される化合物。

(Wherein each symbol is as defined above, _-CH 2 -G- are as defined for formula of (I) -X-, R is alkyl, Pro is an amino protecting group)

Process S
In this step, a protecting group is introduced into compound 17. As the protecting group, a protecting group described in Protective Groups in Organic Synthesis (Theodra W. Greene) and the like can be widely used. Amino protecting groups that can be removed under acidic conditions are preferred. Examples thereof include benzyloxycarbonyl group and tert-butyloxycarbonyl group. For example, ProX ¹ (X ¹ is halogen, Pro is benzyloxycarbonyl group, tert-butyloxycarbonyl, etc.), Pro-O-Pro (Pro is benzyloxycarbonyl group, tert-butyloxycarbonyl, etc.) in the presence of a base. To give compound 23. Tetrahydrofuran and dimethylformamide can be used as the solvent. The reaction can be carried out at room temperature. As the base, triethylamine, pyridine, dimethylaminopyridine and the like can be used. It is to be noted that the reaction can be similarly performed even when R ⁷ is a hydrogen compound.

Process T
In this step, compound 23 is reduced to obtain compound 24. As a reducing agent, lithium aluminum hydride can be used. Tetrahydrofuran or the like can be used as the solvent. The reaction can be carried out at room temperature.

Process U
In this step, compound 24 is azidated to give compound 25. For example, compound 24 is reacted with methanesulfonyl chloride using triethylamine as a base to induce compound 24 to mesylate. As a solvent for the mesylation, chloroform can be used. The obtained compound is reacted with sodium azide and azidated in dimethylformamide or the like at room temperature or under heating to obtain compound 25.

Process V
In this step, compound 25 is reduced to obtain compound 26. Compound 26 is obtained by reducing compound 25 with triphenylphosphine and water. The reaction can be carried out under warming. Tetrahydrofuran can be used as the solvent. In addition to the reduction method using triphenylphosphine, it can be carried out by catalytic reduction. In the case of catalytic reduction, 10% palladium carbon or the like can be used as a catalyst. As the solvent, ethanol or the like can be used. Which reduction method is used can be appropriately selected depending on the protecting group to be used.

Process W
In this step, compound 26 is reacted with a compound represented by the formula: R ¹ —Y—X ¹ (X ¹ is halogen or the like, Y is S, SO, SO ₂ or CO) to obtain compound 27. As the compound represented by the formula: R ¹ —Y—X ¹ (X ¹ is halogen or the like), various sulfonyl chlorides, sulfinyl chlorides, acyl chlorides and the like can be used. As the solvent, tetrahydrofuran, dimethylamide, or the like can be used. The reaction can be carried out at room temperature or under warming. The reaction is preferably performed in the presence of a base, and pyridine, triethylamine, or the like can be used as the base. Alternatively, the compound represented by the formula: R ¹ —Y—X ^{1 in} which Y═S or SO is reacted to obtain a compound 27, which is then oxidized to be converted into a compound in which Y is SO _2. You may use for the following process.

Process X
In this step, the protecting group of compound 27 is removed. The removal of the protecting group can be used by selecting various conditions depending on the protecting group. For example, the tert-butyloxycarbonyl group can be removed with an acid. The benzyloxycarbonyl group can be removed by catalytic reduction or the like.

Process Y
In this step, the substituent Z is introduced into the compound 28. For example, compound (ID) can be obtained by reacting ZX ¹ (X ¹ is halogen) in the presence of a base. As the solvent, methanol, ethanol, isopropanol, dimethylformamide, or the like can be used. The reaction can be carried out at room temperature or under warming. For example, it can be sealed and sealed using a microwave reactor. As the base, N, N-diisopropylethylamine or the like can be used.

In the above steps, the following intermediates are useful.

(In the formula, R is an optionally substituted lower alkyl, Pro is a protecting group, R ⁷ is hydrogen or an optionally substituted lower alkyl, and G is 1, 4-cycloalkylene, Y is SO ₂ or SO, R ¹ is optionally substituted lower alkyl, R ² is hydrogen or optionally substituted lower alkyl is there)
R is particularly preferably lower alkyl, more preferably methyl or ethyl. Ethyl is particularly preferable.
Pro is preferably an amino protecting group that can be removed under acidic conditions. For example, as Pro, a group represented by the formula: — (C═O) —O—R (R represents a lower alkyl which may have a substituent, a lower alkenyl which may have a substituent) preferable. In particular, a tert-butyloxycarbonyl group is preferable.
R ⁷ is preferably hydrogen.
Y is preferably SO ₂ .
R ¹ is particularly preferably lower alkyl, more preferably isopropyl, ethyl or tert-butyl. In particular, tert-butyl is preferred.
R ² is preferably hydrogen.
In particular, the following compounds are preferable.
formula:

(Wherein R ¹ is ethyl or tert-butyl).
formula:

Wherein R ¹ is ethyl, isopropyl or tert-butyl.
formula:

(Wherein Z is a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent).

  Although all the compounds according to the present invention have NPY Y5 receptor antagonistic action, particularly preferred compounds include the following compounds.

であり、

が置換基を有していてもよいシクロアルキレン、置換基を有していてもよいシクロアルケニレン、置換基を有していてもよいビシクロアルキレン、置換基を有していてもよいフェニレンまたは置換基を有していてもよいヘテロ環ジイルである（以下、ＸがＸ−１であるとする）化合物、
Ｘが炭素数２〜６のアルキレン、炭素数３〜６のアルケニレンまたは

であり、

が置換基を有していてもよいシクロアルキレン、置換基を有していてもよいシクロアルケニレン、置換基を有していてもよいビシクロアルキレン、置換基を有していてもよいフェニレン、置換基を有していてもよいピペリジニレン、置換基を有していてもよいチオフェンジイルまたは置換基を有していてもよいフランジイルである（以下、ＸがＸ−２であるとする）化合物、
Ｘが炭素数２〜６のアルキレンまたは

であり、

が置換基を有していてもよいシクロアルキレン、置換基を有していてもよいフェニレン、置換基を有していてもよいピペリジニレン、置換基を有していてもよいチオフェンジイルまたは置換基を有していてもよいフランジイルである（以下、ＸがＸ−３であるとする）化合物、
Ｘが炭素数２〜６のアルキレンまたはそれぞれハロゲン、ヒドロキシ、低級アルキルもしくはハロゲノ低級アルキルで置換されていてもよいシクロアルキレンもしくはフェニレンである（以下、ＸがＸ−４であるとする）化合物、
Ｘが炭素数２〜６のアルキレンまたは炭素数５〜６のシクロアルキレンである（以下、ＸがＸ−５であるとする）化合物、
Ｘが炭素数３〜６のアルキレンまたは１，４−シクロヘキシレンである（以下、ＸがＸ−６であるとする）化合物、

Ｙが−ＳＯ−である（以下、ＹがＹ−１であるとする）化合物、
Ｙが−ＳＯ_２−である（以下、ＹがＹ−２であるとする）化合物、
Ｙが−ＣＯ−である（以下、ＹがＹ−３であるとする）化合物、

Ｚが置換基を有していてもよい低級アルキル、置換基を有していてもよい炭化水素環式基または置換基を有していてもよいヘテロ環式基である（以下、ＺがＺ−１であるとする）化合物、
Ｚが−（ＣＲ^８Ｒ^９）ｒ−Ｗ−（ＣＲ^１０Ｒ^１１）ｓ−Ｖ
［式中、Ｒ^８、Ｒ^９、Ｒ^１０およびＲ^１１は各々独立して水素または低級アルキルであり、２以上のＲ^８、Ｒ^９、Ｒ^１０および／またはＲ^１１が存在するとき、各々のＲ^８、Ｒ^９、Ｒ^１０およびＲ^１１は異なっていてもよく、Ｗは単結合、Ｏ、ＳまたはＮＲ^１２であり、Ｒ^１２は水素、低級アルキルまたはフェニルであり、Ｖは水素、置換基を有していてもよいシクロアルキル、置換基を有していてもよいビシクロアルキル、置換基を有していてもよいアリールまたは置換基を有していてもよいヘテロ環式基であり、ｒは１〜４の整数であり、ｓは０〜４の整数である］
である（以下、ＺがＺ−２であるとする）化合物、
Ｚが−（ＣＨ_２）ｒ−Ｗ−（ＣＨ_２）ｓ−Ｖ
［式中、Ｗは単結合、Ｏ、ＳまたはＮＲ^１２であり、Ｒ^１２は水素または低級アルキルであり、Ｖはそれぞれ置換基を有していてもよいアリールまたはヘテロ環式基（ここで置換基とはハロゲン、ヒドロキシ、低級アルキル、ハロゲノ低級アルキル、低級アルコキシ、低級アルケニル、アミノ、低級アルキルアミノ、アシル、カルボキシ、低級アルコキシカルボニル、フェニルまたは単環のヘテロアリール）であり、ｒは１〜４の整数であり、ｓは０〜４の整数である］
である（以下、ＺがＺ−３であるとする）化合物、
Ｚが−（ＣＨ_２）ｒ−Ｗ−（ＣＨ_２）ｓ−Ｖ
［式中、Ｗは単結合、Ｏ、Ｓ、ＮＨまたはＮＭｅであり、Ｖはそれぞれ置換基を有していてもよいフェニルまたはヘテロアリール（ここで置換基とはハロゲン、低級アルキル、ハロゲノ低級アルキル、低級アルコキシ、アミノまたは低級アルキルアミノ）であり、ｒは１〜３の整数であり、ｓは０または１である］
である（以下、ＺがＺ−４であるとする）化合物、
Ｚが置換基を有していてもよい炭化水素環式基
［ここで置換基とはハロゲン；ヒドロキシ；
置換基を有していてもよい低級アルキル（ここで置換基とはハロゲン、ヒドロキシ、カルボキシ、低級アルコキシカルボニル、シアノおよび／またはフェニル）；
低級アルコキシカルボニルで置換されていてもよい低級アルケニル；
置換基を有していてもよい低級アルコキシ（ここで置換基とはハロゲン、ヒドロキシ、低級アルコキシ、カルボキシ、低級アルコキシカルボニル、低級アルキルアミノ、シクロアルキル、シアノおよび／またはヘテロ環式基）；
シクロアルキル；シクロアルキルオキシ；アシル；低級アルキルチオ；カルバモイル；低級アルキルカルバモイル；シクロアルキルカルバモイル；ヒドロキシイミノ；
置換基を有していてもよいアミノ（ここで置換基とは低級アルキル、保護されていてもよいヒドロキシ低級アルキル、低級アルコキシ低級アルキル、アシル、低級アルキルスルホニル、アリールスルホニルおよび／またはフェニル）；
ハロゲン、シアノ、フェニルおよび／またはヘテロ環式基で置換されていてもよいフェニル；
低級アルキルスルフィニル；低級アルキルスルファモイル；シクロアルキルスルファモイル；
ニトロ；シアノ；アルキレンジオキシ；低級アルキルで置換されていてもよいフェニルアゾ；フェノキシ；オキソ；
置換基を有していてもよいヘテロ環式基（ここで置換基とは保護されていてもよいヒドロキシ；メルカプト；ハロゲン；低級アルキル；シクロアルキル；低級アルコキシカルボニル；アシル；アミノ；低級アルコキシカルボニルアミノ；カルバモイル；オキソ；フェニル；低級アルコキシフェニル；ハロゲノフェニル；ヘテロ環式基および／またはオキソ）；
低級アルキルで置換されていてもよいヘテロ環スルホニル；ヘテロ環オキシ；低級アルキルで置換されていてもよいヘテロ環カルボニル］
である（以下、ＺがＺ−５であるとする）化合物、
Ｚが置換基を有していてもよいフェニル
（ここで置換基とはハロゲン；ヒドロキシ；ハロゲン、ヒドロキシ、低級アルコキシカルボニル、シアノおよび／またはフェニルで置換されていてもよい低級アルキル；低級アルコキシカルボニル低級アルケニル；ハロゲン、低級アルコキシ、低級アルコキシカルボニル、シクロアルキルおよび／またはヘテロ環式基で置換されていてもよい低級アルコキシ；シクロアルキル；シクロアルキルオキシ；アシル；低級アルキルチオ；カルバモイル；低級アルキルカルバモイル；低級アルキル、ヒドロキシ低級アルキル、アシル、低級アルキルスルホニルおよび／またはフェニルで置換されていてもよいアミノ；ハロゲン、シアノ、フェニルおよび／またはヘテロ環式基で置換されていてもよいフェニル；
低級アルキルスルファモイル；シクロアルキルスルファモイル；ニトロ；アルキレンジオキシ；低級アルキルで置換されていてもよいフェニルアゾ；フェノキシ；オキソ；ヒドロキシ、ハロゲン、低級アルキル、低級アルコキシカルボニル、アミノ、カルバモイル、フェニル、ハロゲノフェニル、ヘテロ環式基および／またはオキソで置換されていてもよいヘテロ環式基；ヘテロ環オキシ；並びに／または低級アルキルで置換されていてもよいヘテロ環スルホニル）である（以下、ＺがＺ−６であるとする）化合物、
Ｚが置換基を有していてもよいフェニル
（ここで置換基とはハロゲン；ハロゲン、ヒドロキシ、低級アルコキシカルボニルおよび／またはフェニルで置換されていてもよい低級アルキル；ハロゲンおよび／またはシクロアルキルで置換されていてもよい低級アルコキシ；シクロアルキル；シクロアルキルオキシ；アシル；低級アルキルチオ；低級アルキルカルバモイル；低級アルキル、ヒドロキシ低級アルキル、アシルおよび／またはフェニルで置換されていてもよいアミノ；ピペリジルで置換されていてもよいフェニル；シクロアルキルスルファモイル；アルキレンジオキシ；フェノキシ；
低級アルキルで置換されていてもよいモルホリニルもしくはモルホリノ；ヒドロキシ、低級アルキル、低級アルコキシカルボニル、フェニル、ハロゲノフェニルおよび／またはオキソで置換されていてもよいピペリジル；ヒドロキシ、カルバモイルおよび／またはオキソで置換されていてもよいピロリジニル；フェニルまたはピリミジルで置換されていてもよいピペラジニル；ジヒドロピリジル；ピロリル；ピロリニル；ハロゲンおよび／または低級アルキルで置換されていてもよいイミダゾリル；ピラゾリル；チエニル；チアジアゾリル；フリル；オキサゾリル；イソオキサゾリル；低級アルキルおよび／またはフェニルで置換されていてもよいテトラゾリル；インドリニル；インドリル；テトラヒドロキノリル；低級アルキルで置換されていてもよいベンゾチアゾリル；オキソで置換されていてもよいテトラヒドロイソチアゾリル；オキソで置換されていてもよいベンゾピラニル；テトラヒドロピラニルオキシ；テトラヒドロフリルオキシ；低級アルキルで置換されていてもよいモルホリノスルホニル；および／または低級アルキルで置換されていてもよいピペリジルスルホニル）である（以下、ＺがＺ−７であるとする）化合物、
Ｚが置換基を有していてもよいフェニル（ここで置換基とはハロゲン、低級アルキル、ハロゲノ低級アルキル、低級アルコキシ、シクロアルキルオキシ、低級アルキルカルバモイル、フェニル、低級アルキルモルホリノおよび／またはテトラヒドロピラニルオキシ）である（以下、ＺがＺ−８であるとする）化合物、
Ｚが置換基を有していてもよいヘテロ環式基（ここで置換基とはハロゲン、ヒドロキシ、低級アルキル、ハロゲノ低級アルキル、低級アルコキシ、メルカプト、低級アルキルチオ、アシル、カルボキシ、低級アルコキシカルボニル、アミノ、低級アルキルアミノ、フェニル、ナフチル、ハロゲンで置換されていてもよいフェニルチオ、ハロゲンで置換されていてもよいフェノキシ、オキソおよび／または低級アルキルで置換されていてもよいヘテロ環式基）である（以下、ＺがＺ−９であるとする）化合物、
Ｚがそれぞれ置換基を有していてもよいチエニル、ピラゾリル、チアゾリル、チアジアゾリル、ピリジル、ピリミジニル、ピラジニル、ピリダジニル、トリアジニル、インドリル、イソインドリル、インドリニル、イソインドリニル、インダゾリル、ベンゾピラニル、ベンズオキサゾリル、ベンゾチエニル、ベンゾチアゾリル、ベンゾチアゾリニル、ベンゾチアジアゾリル、ベンズイミダゾリル、キノリル、イソキノリル、ジヒドロベンゾフリル、カルバゾリル、アクリジニル、ジベンゾフリルまたはチアゾロピリジル（ここで置換基とは低級アルキル；ハロゲノ低級アルキル；低級アルコキシ；低級アルコキシカルボニル；アシル；低級アルコキシカルボニル低級アルキル；メルカプト；それぞれハロゲンで置換されていてもよいフェニル、ナフチル、フェニルチオもしくはフェノキシ；フリル；ニトロ；オキソ；および／または低級アルキルで置換されていてもよいモルホリノ）である（以下、ＺがＺ−１０であるとする）化合物、
Ｚがそれぞれ置換基を有していてもよいチエニル、チアゾリル、チアジアゾリル、ピリジル、ピラジニル、インドリル、イソインドリニル、ベンゾピラニル、キノリル、カルバゾリル、ジベンゾフリル、ベンゾピラニル、ベンゾチエニルまたはベンゾチアゾリル（ここで置換基とは低級アルキル、ハロゲノ低級アルキル、低級アルコキシ、低級アルコキシカルボニル、アシル、フェニル、ナフチル、フェニルチオ、低級アルキルモルホリノおよびオキソからなる群から選択される１以上の基）である（以下、ＺがＺ−１１であるとする）化合物、
Ｒ^１がＲ１−２であり、Ｒ^２がＲ２−２であり、ｎが２であり、Ｘ、ＹおよびＺの組み合わせ（Ｘ，Ｙ，Ｚ）が以下の組み合わせである化合物、
（Ｘ，Ｙ，Ｚ）＝（X-3，Y-2，Z-1），（X-3，Y-2，Z-2），（X-3，Y-2，Z-3），（X-3，Y-2，Z-4），（X-3，Y-2，Z-5），（X-3，Y-2，Z-6），（X-3，Y-2，Z-7），（X-3，Y-2，Z-8），（X-3，Y-2，Z-9），（X-3，Y-2，Z-10），（X-3，Y-2，Z-11），
（X-3，Y-3，Z-1），（X-3，Y-3，Z-2），（X-3，Y-3，Z-3），（X-3，Y-3，Z-4），（X-3，Y-3，Z-5），（X-3，Y-3，Z-6），（X-3，Y-3，Z-7），（X-3，Y-3，Z-8），（X-3，Y-3，Z-9），（X-3，Y-3，Z-10），（X-3，Y-3，Z-11），
（X-4，Y-2，Z-1），（X-4，Y-2，Z-2），（X-4，Y-2，Z-3），（X-4，Y-2，Z-4），（X-4，Y-2，Z-5），（X-4，Y-2，Z-6），（X-4，Y-2，Z-7），（X-4，Y-2，Z-8），（X-4，Y-2，Z-9），（X-4，Y-2，Z-10），（X-4，Y-2，Z-11），
（X-4，Y-3，Z-1），（X-4，Y-3，Z-2），（X-4，Y-3，Z-3），（X-4，Y-3，Z-4），（X-4，Y-3，Z-5），（X-4，Y-3，Z-6），（X-4，Y-3，Z-7），（X-4，Y-3，Z-8），（X-4，Y-3，Z-9），（X-4，Y-3，Z-10），（X-4，Y-3，Z-11），
（X-5，Y-2，Z-1），（X-5，Y-2，Z-2），（X-5，Y-2，Z-3），（X-5，Y-2，Z-4），（X-5，Y-2，Z-5），（X-5，Y-2，Z-6），（X-5，Y-2，Z-7），（X-5，Y-2，Z-8），（X-5，Y-2，Z-9），（X-5，Y-2，Z-10），（X-5，Y-2，Z-11），
（X-5，Y-3，Z-1），（X-5，Y-3，Z-2），（X-5，Y-3，Z-3），（X-5，Y-3，Z-4），（X-5，Y-3，Z-5），（X-5，Y-3，Z-6），（X-5，Y-3，Z-7），（X-5，Y-3，Z-8），（X-5，Y-3，Z-9），（X-5，Y-3，Z-10）または（X-5，Y-3，Z-11）
もしくはその製薬上許容される塩、またはそれらの溶媒和物が挙げられる。 A compound in which R ¹ in formula (I) is optionally substituted lower alkyl (hereinafter referred to as R ¹ is R1-1),
R ¹ is an alkyl having 1 to 10 carbon atoms which may be substituted with halogen (hereinafter, ^{R 1} is assumed to be R1-2) compound,
A compound in which R ¹ is isopropyl or t-butyl (hereinafter, R ¹ is R1-3),

A compound in which R ² is hydrogen or alkyl having 1 to 3 carbon atoms (hereinafter, R ² is R2-1),
A compound in which R ² is hydrogen (hereinafter, R ² is R2-2),

X is an optionally substituted lower alkylene, an optionally substituted lower alkenylene, or

And

Is optionally substituted cycloalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene, optionally substituted phenylene or substituent A compound that is a heterocyclic diyl (hereinafter, X is X-1),
X is alkylene having 2 to 6 carbons, alkenylene having 3 to 6 carbons, or

And

Is optionally substituted cycloalkylene, optionally substituted cycloalkenylene, optionally substituted bicycloalkylene, optionally substituted phenylene, substituent A piperidinylene optionally having a substituent, a thiophenediyl optionally having a substituent, or a furandyl optionally having a substituent (hereinafter, X is assumed to be X-2),
X is alkylene having 2 to 6 carbon atoms or

And

Is an optionally substituted cycloalkylene, an optionally substituted phenylene, an optionally substituted piperidinylene, an optionally substituted thiophenediyl or a substituent. A compound that is a flangile that may have (hereinafter, X is X-3),
A compound in which X is alkylene having 2 to 6 carbon atoms or cycloalkylene or phenylene each optionally substituted by halogen, hydroxy, lower alkyl or halogeno lower alkyl (hereinafter, X is X-4),
A compound in which X is alkylene having 2 to 6 carbons or cycloalkylene having 5 to 6 carbons (hereinafter, X is X-5),
A compound wherein X is alkylene having 3 to 6 carbon atoms or 1,4-cyclohexylene (hereinafter, X is X-6);

A compound in which Y is -SO- (hereinafter, Y is Y-1);
A compound in which Y is —SO ₂ — (hereinafter, Y is Y-2);
A compound in which Y is —CO— (hereinafter, Y is Y-3);

Z is a lower alkyl which may have a substituent, a hydrocarbon cyclic group which may have a substituent or a heterocyclic group which may have a substituent (hereinafter, Z is Z -1) compound,
Z is-(CR < ⁸ > R < ⁹ >) r-W- (CR < ¹⁰ > R < ¹¹ >) s-V.
[Wherein R ⁸ , R ⁹ , R ¹⁰ and R ¹¹ are each independently hydrogen or lower alkyl, and when two or more R ⁸ , R ⁹ , R ¹⁰ and / or R ¹¹ are present, R ⁸ , R ⁹ , R ¹⁰ and R ¹¹ may be different, W is a single bond, O, S or NR ¹² , R ¹² is hydrogen, lower alkyl or phenyl, V is hydrogen, substituent Cycloalkyl which may have a substituent, bicycloalkyl which may have a substituent, aryl which may have a substituent, or a heterocyclic group which may have a substituent, r Is an integer from 1 to 4, and s is an integer from 0 to 4.]
(Hereinafter, Z is Z-2),
Z is _{- (CH 2) r-W-} (CH 2) s-V
[Wherein W is a single bond, O, S or NR ¹² , R ¹² is hydrogen or lower alkyl, and V is an aryl or heterocyclic group optionally substituted (wherein substituted) Group is halogen, hydroxy, lower alkyl, halogeno lower alkyl, lower alkoxy, lower alkenyl, amino, lower alkylamino, acyl, carboxy, lower alkoxycarbonyl, phenyl or monocyclic heteroaryl), and r is 1-4. And s is an integer of 0 to 4.]
(Hereinafter, Z is Z-3),
Z is _{- (CH 2) r-W-} (CH 2) s-V
[Wherein W is a single bond, O, S, NH or NMe, and V is phenyl or heteroaryl each optionally having a substituent (wherein the substituents are halogen, lower alkyl, halogeno-lower alkyl) , Lower alkoxy, amino or lower alkylamino), r is an integer of 1 to 3, and s is 0 or 1.]
(Hereinafter, Z is Z-4),
Z is an optionally substituted hydrocarbon cyclic group [wherein the substituent is halogen; hydroxy;
Optionally substituted lower alkyl (wherein the substituent is halogen, hydroxy, carboxy, lower alkoxycarbonyl, cyano and / or phenyl);
Lower alkenyl optionally substituted by lower alkoxycarbonyl;
Lower alkoxy which may have a substituent (wherein the substituent is halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, lower alkylamino, cycloalkyl, cyano and / or heterocyclic group);
Cycloalkyl; Cycloalkyloxy; Acyl; Lower alkylthio; Carbamoyl; Lower alkylcarbamoyl; Cycloalkylcarbamoyl; Hydroxyimino;
Optionally substituted amino (wherein the substituent is lower alkyl, optionally protected hydroxy lower alkyl, lower alkoxy lower alkyl, acyl, lower alkylsulfonyl, arylsulfonyl and / or phenyl);
Phenyl optionally substituted by halogen, cyano, phenyl and / or heterocyclic groups;
Lower alkylsulfinyl; lower alkylsulfamoyl; cycloalkylsulfamoyl;
Nitro; cyano; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo;
Optionally substituted heterocyclic group (wherein the substituent may be protected hydroxy; mercapto; halogen; lower alkyl; cycloalkyl; lower alkoxycarbonyl; acyl; amino; lower alkoxycarbonylamino) Carbamoyl; oxo; phenyl; lower alkoxyphenyl; halogenophenyl; heterocyclic group and / or oxo);
Heterocyclic sulfonyl optionally substituted with lower alkyl; Heterocyclic oxy; Heterocyclic carbonyl optionally substituted with lower alkyl]
(Hereinafter, Z is Z-5),
Z is optionally substituted phenyl (wherein the substituent is halogen; hydroxy; halogen, hydroxy, lower alkoxycarbonyl, lower alkyl optionally substituted with cyano and / or phenyl; lower alkoxycarbonyl lower Alkenyl; lower alkoxy optionally substituted with halogen, lower alkoxy, lower alkoxycarbonyl, cycloalkyl and / or heterocyclic group; cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; carbamoyl; lower alkylcarbamoyl; Amino optionally substituted with hydroxy, lower alkyl, acyl, lower alkylsulfonyl and / or phenyl; phenyl optionally substituted with halogen, cyano, phenyl and / or heterocyclic group;
Lower alkyl sulfamoyl; cycloalkyl sulfamoyl; nitro; alkylenedioxy; phenylazo optionally substituted with lower alkyl; phenoxy; oxo; hydroxy, halogen, lower alkyl, lower alkoxycarbonyl, amino, carbamoyl, phenyl, Halogenophenyl, heterocyclic group and / or heterocyclic group optionally substituted with oxo; heterocyclic oxy; and / or heterocyclic sulfonyl optionally substituted with lower alkyl) (hereinafter Z is Z-6) compound,
Z is optionally substituted phenyl (wherein the substituent is halogen; halogen, hydroxy, lower alkoxycarbonyl and / or lower alkyl optionally substituted with phenyl; halogen and / or cycloalkyl substituted) Cycloalkyl; cycloalkyloxy; acyl; lower alkylthio; lower alkyl carbamoyl; amino optionally substituted with lower alkyl, hydroxy lower alkyl, acyl and / or phenyl; substituted with piperidyl Optionally phenyl; cycloalkylsulfamoyl; alkylenedioxy; phenoxy;
Morpholinyl or morpholino optionally substituted with lower alkyl; piperidyl optionally substituted with hydroxy, lower alkyl, lower alkoxycarbonyl, phenyl, halogenophenyl and / or oxo; substituted with hydroxy, carbamoyl and / or oxo Pyrrolidinyl optionally substituted with phenyl or pyrimidyl; dihydropyridyl; pyrrolyl; pyrrolyl; pyrrolinyl; imidazolyl optionally substituted with halogen and / or lower alkyl; pyrazolyl; thienyl; thiadiazolyl; furyl; oxazolyl; isoxazolyl Tetrazolyl optionally substituted with lower alkyl and / or phenyl; indolinyl; indolyl; tetrahydroquinolyl; substituted with lower alkyl Optionally benzothiazolyl; tetrahydroisothiazolyl optionally substituted with oxo; benzopyranyl optionally substituted with oxo; tetrahydropyranyloxy; tetrahydrofuryloxy; morpholinosulfonyl optionally substituted with lower alkyl; and (Or piperidylsulfonyl optionally substituted with lower alkyl) (hereinafter, Z is assumed to be Z-7),
Z may optionally have a substituent (wherein the substituent is halogen, lower alkyl, halogeno lower alkyl, lower alkoxy, cycloalkyloxy, lower alkylcarbamoyl, phenyl, lower alkylmorpholino and / or tetrahydropyranyl) Oxy) (hereinafter referred to as Z being Z-8),
Z is an optionally substituted heterocyclic group (wherein the substituents are halogen, hydroxy, lower alkyl, halogeno lower alkyl, lower alkoxy, mercapto, lower alkylthio, acyl, carboxy, lower alkoxycarbonyl, amino , Lower alkylamino, phenyl, naphthyl, phenylthio optionally substituted with halogen, phenoxy optionally substituted with halogen, oxo and / or heterocyclic group optionally substituted with lower alkyl) ( Hereinafter, a compound in which Z is Z-9),
Z may optionally have a substituent, thienyl, pyrazolyl, thiazolyl, thiadiazolyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, indolyl, isoindolyl, indolinyl, isoindolinyl, indazolyl, benzopyranyl, benzoxazolyl, benzothienyl, Benzothiazolyl, benzothiazolinyl, benzothiadiazolyl, benzimidazolyl, quinolyl, isoquinolyl, dihydrobenzofuryl, carbazolyl, acridinyl, dibenzofuryl or thiazolopyridyl (where the substituent is lower alkyl; halogeno lower alkyl; lower alkoxy; Lower alkoxycarbonyl; acyl; lower alkoxycarbonyl lower alkyl; mercapto; phenyl each optionally substituted by halogen Naphthyl, phenylthio or phenoxy; furyl; nitro; oxo; a and / or lower alkyl optionally substituted morpholino) (hereinafter, Z is assumed to be Z-10) compound,
Each Z may have a substituent such as thienyl, thiazolyl, thiadiazolyl, pyridyl, pyrazinyl, indolyl, isoindolinyl, benzopyranyl, quinolyl, carbazolyl, dibenzofuryl, benzopyranyl, benzothienyl or benzothiazolyl (where the substituent is lower alkyl) , Halogeno lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, phenyl, naphthyl, phenylthio, lower alkylmorpholino and oxo (hereinafter, Z is Z-11). Compound),
A compound in which R ¹ is R1-2, R ² is R2-2, n is 2, and the combination of X, Y and Z (X, Y, Z) is the following combination:
(X, Y, Z) = (X-3, Y-2, Z-1), (X-3, Y-2, Z-2), (X-3, Y-2, Z-3), (X-3, Y-2, Z-4), (X-3, Y-2, Z-5), (X-3, Y-2, Z-6), (X-3, Y-2 , Z-7), (X-3, Y-2, Z-8), (X-3, Y-2, Z-9), (X-3, Y-2, Z-10), (X -3, Y-2, Z-11),
(X-3, Y-3, Z-1), (X-3, Y-3, Z-2), (X-3, Y-3, Z-3), (X-3, Y-3 , Z-4), (X-3, Y-3, Z-5), (X-3, Y-3, Z-6), (X-3, Y-3, Z-7), (X -3, Y-3, Z-8), (X-3, Y-3, Z-9), (X-3, Y-3, Z-10), (X-3, Y-3, Z -11),
(X-4, Y-2, Z-1), (X-4, Y-2, Z-2), (X-4, Y-2, Z-3), (X-4, Y-2 , Z-4), (X-4, Y-2, Z-5), (X-4, Y-2, Z-6), (X-4, Y-2, Z-7), (X -4, Y-2, Z-8), (X-4, Y-2, Z-9), (X-4, Y-2, Z-10), (X-4, Y-2, Z -11),
(X-4, Y-3, Z-1), (X-4, Y-3, Z-2), (X-4, Y-3, Z-3), (X-4, Y-3 , Z-4), (X-4, Y-3, Z-5), (X-4, Y-3, Z-6), (X-4, Y-3, Z-7), (X -4, Y-3, Z-8), (X-4, Y-3, Z-9), (X-4, Y-3, Z-10), (X-4, Y-3, Z -11),
(X-5, Y-2, Z-1), (X-5, Y-2, Z-2), (X-5, Y-2, Z-3), (X-5, Y-2 , Z-4), (X-5, Y-2, Z-5), (X-5, Y-2, Z-6), (X-5, Y-2, Z-7), (X -5, Y-2, Z-8), (X-5, Y-2, Z-9), (X-5, Y-2, Z-10), (X-5, Y-2, Z -11),
(X-5, Y-3, Z-1), (X-5, Y-3, Z-2), (X-5, Y-3, Z-3), (X-5, Y-3 , Z-4), (X-5, Y-3, Z-5), (X-5, Y-3, Z-6), (X-5, Y-3, Z-7), (X -5, Y-3, Z-8), (X-5, Y-3, Z-9), (X-5, Y-3, Z-10) or (X-5, Y-3, Z -11)
Or its pharmaceutically acceptable salt, or those solvates are mentioned.

The appetite suppressant or anti-obesity agent of the present invention is useful for prevention and / or treatment of obesity and suppression of eating. It is also effective for the prevention and / or treatment of diseases in which obesity is a risk factor, such as diabetes, hypertension, hyperlipidemia, arteriosclerosis, and acute coronary syndrome.
Furthermore, the compound used in the present invention has not only NPY Y5 receptor antagonistic activity but also usefulness as a medicament, and has any or all of the following excellent characteristics.
a) Inhibition of CYP enzyme (eg, CYP1A2, CYP2C9, CYP3A4, etc.) is weak.
b) It is difficult to induce drug metabolizing enzymes.
c) Good pharmacokinetics such as high bioavailability.
d) Low toxicity such as anemia-inducing action.
e) High metabolic stability.
f) High Y5 receptor selectivity.
g) High water solubility.
h) High brain transferability.
i) Does not cause reproductive toxicity (eg teratogenicity).
j) Does not cause gastrointestinal disorders (eg, hemorrhagic enteritis, gastrointestinal ulcer, gastrointestinal bleeding, etc.).

  Furthermore, the compounds used in the present invention have low affinity for NPY Y1 and Y2 receptors and high Y5 receptor selectivity. NPY induces persistent defect contraction in the periphery, but this effect is mainly mediated by the Y1 receptor. Since the Y5 receptor is not involved in such an action at all, it is unlikely to induce side effects based on peripheral vasoconstriction, and can be suitably used as a safe pharmaceutical.

  The compound used in the present invention suppresses food intake and exhibits an anti-obesity effect. Therefore, side effects such as indigestion as seen in drugs that exhibit anti-obesity effects by inhibiting digestion and absorption, and central side effects such as antidepressant effects such as serotonin transporter inhibitors that exhibit anti-obesity effects Not to do is one of the features of this drug.

  When the appetite suppressant or anti-obesity agent of the present invention is administered, it can be administered either orally or parenterally. Oral administration may be prepared and administered in a commonly used dosage form such as tablets, granules, powders, capsules, pills, liquids, syrups, buccals or sublinguals according to conventional methods. For parenteral administration, any commonly used dosage forms such as injections such as intramuscular administration and intravenous administration, suppositories, percutaneous absorption agents, inhalants and the like can be suitably administered. Since the compound according to the present invention has high oral absorbability, it can be suitably used as an oral preparation.

  Various pharmaceutical additives such as excipients, binders, wetting agents, disintegrants, lubricants, diluents and the like suitable for the dosage form are mixed with an effective amount of the compound according to the present invention as necessary to produce a pharmaceutical preparation It can be. In the case of an injection, it may be sterilized with an appropriate carrier to form a preparation.

  Specifically, the excipients are lactose, sucrose, glucose, starch, calcium carbonate or crystalline cellulose, and the binders are methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, gelatin or polyvinyl. Examples of disintegrants include pyrrolidone, carboxymethyl cellulose, sodium carboxymethyl cellulose, starch, sodium alginate, agar powder or sodium lauryl sulfate, and lubricants include talc, magnesium stearate, or macrogol. It is done. As a suppository base, cacao butter, macrogol, methyl cellulose, or the like can be used. In addition, when preparing as liquid or emulsion or suspension injections, commonly used solubilizers, suspending agents, emulsifiers, stabilizers, preservatives, isotonic agents, etc. are added as appropriate. In the case of oral administration, a flavoring agent, a fragrance or the like may be added.

  The dose of the appetite suppressant or anti-obesity agent of the present invention is preferably set in consideration of the age, weight, type and degree of disease, route of administration, etc. of the patient. 0.05 to 100 mg / kg / day, preferably 0.1 to 10 mg / kg / day. In the case of parenteral administration, although it varies greatly depending on the administration route, it is usually 0.005 to 10 mg / kg / day, preferably 0.01 to 1 mg / kg / day. This may be administered once to several times a day.

The present invention will be described in more detail with reference to the following examples, but these are not intended to limit the present invention.
Moreover, the symbol used in this specification represents the following meaning.
Me: methyl Et: ethyl i-Pr: isopropyl DMSO: dimethyl sulfoxide Pd-C: palladium carbon THF: tetrahydrofuran DMF: N, N-dimethylformamide mCPBA: metachloroperbenzoic acid

３−フルオロニトロベンゼン(2.00 g, 14.2 mmol)をジメチルスルホキシド15 mlに溶解させ、3,5−ジメチルピペリジン(3.21 g, 28.4 mmol)と炭酸カリウム(3.92 g, 28.4 mmol)を加え３時間150℃で攪拌した。反応液を水へあけ酢酸エチルで抽出した。有機層を水洗し無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣に酢酸エチルおよびヘキサンを加え、析出した結晶を濾取することで目的物の置換ニトロベンゼンが2.05 g、収率62%で得られた。
¹H-NMR (CDCl3) δppm: 0.76 (q, 1H, J = 12.0 Hz), 0.96 (d, 6H, J = 6.3 Hz), 1.70-1.91 (m, 3H), 2.32 (t, 2H, J = 12.0 Hz), 3.62-3.72 (m, 2H), 7.17-7.25 (m, 1H), 7.34 (t, 1H, J = 8.1 Hz), 7.59 (d, 1H, J = 8.1 Hz), 7.71 (s, 1H).

第２工程

第１工程で得られた化合物(2.05 g, 8.75 mmol) をエタノール25 mlに溶解させ、10% Pd-C( 0.20g ) を加え水素添加反応を12時間行なった。Pd-Cをセライト濾過により除去し、濾液を減圧下濃縮した。残渣をシリカゲルクロマトグラフィにより精製すると目的物のアニリンが1.62 g、収率90%で得られた。
¹H-NMR (CDCl3) δppm: 0.69 (q, 1H, J = 12.0 Hz), 0.92 (d, 6H, J = 6.3 Hz), 1.75-1.98 (m, 3H), 2.22 (t, 2H, J = 12.0 Hz), 3.53-3.62 (m, 2H), 6.21 (d, 1H, J = 7.5 Hz), 6.38 (s, 1H), 6.42 (d, 1H, J = 8.1 Hz), 7.04 (t, 1H, J = 8.1 Hz).

第３工程

原料カルボン酸（合成法は国際公開第０１／０３７８２６号パンフレットに記載）(5.04 g, 19.1 mmol) をテトラヒドロフラン50 mlに懸濁させ、氷冷下水素化リチウムアルミニウム (0.726 g, 19.1 mmol)を加え、室温で１時間攪拌した。反応液を再び氷冷攪拌し、水( 1.5mL )を注意深く滴下した。滴下後、室温で5分間攪拌し、生じた沈殿物を濾過除去し、濾液を減圧下濃縮した。残渣に酢酸エチルおよびヘキサンを加え、析出した結晶を濾取することで目的物のアルコールが3.15 g、収率66%で得られた。
¹H-NMR (DMSO-d6) δppm: 0.88 (q, 2H, J = 11.6 Hz), 1.25 (s, 9H), 1.15-1.30 (m, 3H), 1.67-1.76 (m, 2H), 1.83-1.92 (m, 2H), 2.97 (m, 1H), 3.13-3.20 (m, 2H), 4.35 (t, 1H, J = 5.2 Hz), 6.71 (d, 1H, J = 8.8 Hz).

第４工程

第３工程で得た化合物(500 mg, 2.01 mmol) をクロロホルム5 mlに溶解させ、デス‐マーチン過よう素酸(893 mg, 2.11 mmol)を加え室温で1時間攪拌した。沈殿物を濾過除去し、濾液を減圧下濃縮した。残渣をシリカゲルクロマトグラフィにより精製すると目的物のアルデヒドが385 mg、収率77%で得られた。
¹H-NMR (DMSO-d6) δppm: 1.26 (s, 9H), 1.13-1.38 (m, 4H), 1.85-1.98 (m, 4H), 2.16 (m, 1H), 3.01 (m, 1H), 6.80 (d, 1H, J = 8.0 Hz), 9.54 (s, 1H).

第5工程

第２工程で得たアニリン(107 mg, 0.523 mmol) をテトラヒドロフラン3 mlに溶解させ、第４工程で得たアルデヒド(130 mg, 0.523 mmol)を加え室温で1時間攪拌した。反応液に水素化ホウ素ナトリウム(23.7mg, 0.628 mmol)を加え室温でさらに３時間攪拌した。反応液を水へあけ酢酸エチルで抽出した。有機層を水洗し無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣をシリカゲルクロマトグラフィにより精製すると目的物が99.3 mg、収率43%で得られた。
1H-NMR (DMSO-d6) δppm: 0.64 (q, 1H, J = 11.6 Hz), 0.87 (d, 6H, J = 6.0 Hz), 0.92-1.08 (m, 2H), 1.25 (s, 9H), 1.15-1.32 (m, 2H), 1.41 (m, 1H), 1.58-1.95 (m, 7H), 2.08 (t, 2H, J = 11.6 Hz), 2.75-2.82 (m, 2H), 3.00 (m, 1H), 3.48-3.55 (m, 2H), 5.31 (m, 1H), 5.94 (d, 1H, J = 8.5 Hz), 6.08-6.13 (m, 2H), 6.71 (d, 1H, J = 8.5 Hz), 6.85 (t, 1H, J = 8.5 Hz). 融点：161-162℃ Example 1 First Step of Synthesis of Compound (Ii-1)

3-Fluoronitrobenzene (2.00 g, 14.2 mmol) was dissolved in 15 ml of dimethyl sulfoxide, and 3,5-dimethylpiperidine (3.21 g, 28.4 mmol) and potassium carbonate (3.92 g, 28.4 mmol) were added for 3 hours at 150 ° C. Stir. The reaction mixture was poured into water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure, ethyl acetate and hexane were added to the residue, and the precipitated crystals were collected by filtration to obtain 2.05 g of the desired substituted nitrobenzene in a yield of 62%.
¹ H-NMR (CDCl3) δppm: 0.76 (q, 1H, J = 12.0 Hz), 0.96 (d, 6H, J = 6.3 Hz), 1.70-1.91 (m, 3H), 2.32 (t, 2H, J = 12.0 Hz), 3.62-3.72 (m, 2H), 7.17-7.25 (m, 1H), 7.34 (t, 1H, J = 8.1 Hz), 7.59 (d, 1H, J = 8.1 Hz), 7.71 (s, 1H).

Second step

The compound (2.05 g, 8.75 mmol) obtained in the first step was dissolved in 25 ml of ethanol, 10% Pd—C (0.20 g) was added, and hydrogenation reaction was performed for 12 hours. Pd-C was removed by Celite filtration, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel chromatography to obtain 1.62 g of the desired aniline in 90% yield.
¹ H-NMR (CDCl3) δppm: 0.69 (q, 1H, J = 12.0 Hz), 0.92 (d, 6H, J = 6.3 Hz), 1.75-1.98 (m, 3H), 2.22 (t, 2H, J = 12.0 Hz), 3.53-3.62 (m, 2H), 6.21 (d, 1H, J = 7.5 Hz), 6.38 (s, 1H), 6.42 (d, 1H, J = 8.1 Hz), 7.04 (t, 1H, J = 8.1 Hz).

Third step

Raw material carboxylic acid (the synthesis method is described in pamphlet of WO 01/037826) (5.04 g, 19.1 mmol) is suspended in 50 ml of tetrahydrofuran, and lithium aluminum hydride (0.726 g, 19.1 mmol) is added under ice cooling. And stirred at room temperature for 1 hour. The reaction mixture was stirred again on ice and water (1.5 mL) was carefully added dropwise. After dropping, the mixture was stirred at room temperature for 5 minutes, the resulting precipitate was removed by filtration, and the filtrate was concentrated under reduced pressure. Ethyl acetate and hexane were added to the residue, and the precipitated crystals were collected by filtration to obtain 3.15 g of the target alcohol in 66% yield.
¹ H-NMR (DMSO-d6) δppm: 0.88 (q, 2H, J = 11.6 Hz), 1.25 (s, 9H), 1.15-1.30 (m, 3H), 1.67-1.76 (m, 2H), 1.83- 1.92 (m, 2H), 2.97 (m, 1H), 3.13-3.20 (m, 2H), 4.35 (t, 1H, J = 5.2 Hz), 6.71 (d, 1H, J = 8.8 Hz).

4th process

The compound obtained in the third step (500 mg, 2.01 mmol) was dissolved in 5 ml of chloroform, des-Martin periodic acid (893 mg, 2.11 mmol) was added, and the mixture was stirred at room temperature for 1 hour. The precipitate was removed by filtration, and the filtrate was concentrated under reduced pressure. The residue was purified by silica gel chromatography to obtain the desired aldehyde (385 mg, yield 77%).
¹ H-NMR (DMSO-d6) δppm: 1.26 (s, 9H), 1.13-1.38 (m, 4H), 1.85-1.98 (m, 4H), 2.16 (m, 1H), 3.01 (m, 1H), 6.80 (d, 1H, J = 8.0 Hz), 9.54 (s, 1H).

5th process

The aniline (107 mg, 0.523 mmol) obtained in the second step was dissolved in 3 ml of tetrahydrofuran, the aldehyde (130 mg, 0.523 mmol) obtained in the fourth step was added, and the mixture was stirred at room temperature for 1 hour. Sodium borohydride (23.7 mg, 0.628 mmol) was added to the reaction solution, and the mixture was further stirred at room temperature for 3 hours. The reaction mixture was poured into water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to obtain 99.3 mg of the desired product in 43% yield.
1H-NMR (DMSO-d6) δppm: 0.64 (q, 1H, J = 11.6 Hz), 0.87 (d, 6H, J = 6.0 Hz), 0.92-1.08 (m, 2H), 1.25 (s, 9H), 1.15-1.32 (m, 2H), 1.41 (m, 1H), 1.58-1.95 (m, 7H), 2.08 (t, 2H, J = 11.6 Hz), 2.75-2.82 (m, 2H), 3.00 (m, 1H), 3.48-3.55 (m, 2H), 5.31 (m, 1H), 5.94 (d, 1H, J = 8.5 Hz), 6.08-6.13 (m, 2H), 6.71 (d, 1H, J = 8.5 Hz ), 6.85 (t, 1H, J = 8.5 Hz). Melting point: 161-162 ° C

原料アミン(1.20 g, 3.64 mmol)と２‐クロロ‐５‐トリフルオロメチルピリジン(727 mg, 4.01 mmol)をイソプロパノール4 mlに懸濁させ、N, N-ジイソプロピルエチルアミン(1.87 ml, 10.9 mmol)を加え封管後、マイクロウェーブ反応装置を用いて１時間160℃の条件で反応を行なった。反応液を水へあけ酢酸エチルで抽出した。有機層を水洗し無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣をシリカゲルクロマトグラフィにより精製すると目的物のエステルが222 mg、収率20%で得られた。

第２工程

第１工程で得たエステル(207 mg, 0.685 mmol) をテトラヒドロフラン3 mlに溶解させ、氷冷下水素化リチウムアルミニウム (31.1 mg, 0.822 mmol)を加え、室温で0.5時間攪拌した。反応液を氷水へあけ酢酸エチルで抽出した後、有機層を水洗し無水硫酸ナトリウムで乾燥し、溶媒を減圧下留去することでアルコールを得た。得られたアルコールをクロロホルム3mlに溶解し、トリエチルアミン（0.28 ml, 2.04 mmol）を加え、氷冷下メタンスルホニルクロライド (0.12 ml, 1.64 mmol)を滴下し、室温で１時間攪拌した。反応液を水へあけ酢酸エチルで抽出した後、有機層を水洗し無水硫酸ナトリウムで乾燥し、溶媒を減圧下留去することでメシレートを得た。得られたメシレートをジメチルホルムアミド3mlに溶解し、アジ化ナトリウム（221 mg, 3.40 mmol）を加え、３時間100℃で攪拌した。反応液を水へあけ酢酸エチルで抽出した。有機層を水洗し無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣をシリカゲルクロマトグラフィにより精製すると目的物のアジドが178 mg、収率87%で得られた。

第３工程

第２工程で得たアジド(178 mg, 0.595 mmol) をエタノール3 mlに溶解させ、10% Pd-C( 30 mg ) を加え水素添加反応を4時間行なった。Pd-Cをセライト濾過により除去し、濾液を減圧下濃縮することでアミンを得た。
得られたアミンをテトラヒドロフラン3mlに溶解し、トリエチルアミン（0.28 ml, 0.714 mmol）を加え、氷冷下イソプロピルスルホニルクロライド (0.10 ml, 1.64 mmol)を滴下し１時間攪拌した。反応液を水へあけ酢酸エチルで抽出した後、有機層を水洗し無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣をシリカゲルクロマトグラフィにより精製すると目的物が64.8 mg、収率29%で得られた。
¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2 H), 1.10-1.25 (m, 2H,), 1.22 (d, 6H, J = 6.4 Hz), 1.38 (m, 1H), 1.76-1.84 (m, 2H), 1.93-2.02 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.19 (m, 1H), 3.69 (m, 1H), 6.53 (d, 1H, J = 8.8 Hz), 6.95 (t, 1H, J = 5.6 Hz), 7.16 (d, 1H, J = 7.6 Hz), 7.58 (d, 1H, J = 8.8 Hz), 8.26 (s, 1H) 融点：155-156℃ Example 2 First Step of Synthesis of Compound (Ij-1)

The starting amine (1.20 g, 3.64 mmol) and 2-chloro-5-trifluoromethylpyridine (727 mg, 4.01 mmol) were suspended in 4 ml of isopropanol, and N, N-diisopropylethylamine (1.87 ml, 10.9 mmol) was suspended. In addition, after sealing the tube, the reaction was carried out at 160 ° C. for 1 hour using a microwave reactor. The reaction mixture was poured into water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to obtain 222 mg of the desired ester in a yield of 20%.

Second step

The ester (207 mg, 0.685 mmol) obtained in the first step was dissolved in 3 ml of tetrahydrofuran, lithium aluminum hydride (31.1 mg, 0.822 mmol) was added under ice cooling, and the mixture was stirred at room temperature for 0.5 hour. The reaction mixture was poured into ice water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain an alcohol. The obtained alcohol was dissolved in 3 ml of chloroform, triethylamine (0.28 ml, 2.04 mmol) was added, methanesulfonyl chloride (0.12 ml, 1.64 mmol) was added dropwise under ice cooling, and the mixture was stirred at room temperature for 1 hour. The reaction solution was poured into water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate, and the solvent was distilled off under reduced pressure to obtain mesylate. The obtained mesylate was dissolved in 3 ml of dimethylformamide, sodium azide (221 mg, 3.40 mmol) was added, and the mixture was stirred at 100 ° C. for 3 hours. The reaction mixture was poured into water and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to obtain 178 mg of the desired product, azide, in a yield of 87%.

Third step

The azide (178 mg, 0.595 mmol) obtained in the second step was dissolved in 3 ml of ethanol, 10% Pd-C (30 mg) was added, and hydrogenation reaction was performed for 4 hours. Pd—C was removed by Celite filtration, and the filtrate was concentrated under reduced pressure to obtain an amine.
The obtained amine was dissolved in 3 ml of tetrahydrofuran, triethylamine (0.28 ml, 0.714 mmol) was added, and isopropylsulfonyl chloride (0.10 ml, 1.64 mmol) was added dropwise under ice cooling, followed by stirring for 1 hour. The reaction solution was poured into water and extracted with ethyl acetate, and then the organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to obtain 64.8 mg of the desired product in 29% yield.
¹ H-NMR (DMSO-d ₆ ) δ: 0.92-1.06 (m, 2 H), 1.10-1.25 (m, 2H,), 1.22 (d, 6H, J = 6.4 Hz), 1.38 (m, 1H) , 1.76-1.84 (m, 2H), 1.93-2.02 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.19 (m, 1H), 3.69 (m, 1H), 6.53 (d , 1H, J = 8.8 Hz), 6.95 (t, 1H, J = 5.6 Hz), 7.16 (d, 1H, J = 7.6 Hz), 7.58 (d, 1H, J = 8.8 Hz), 8.26 (s, 1H ) Melting point: 155-156 ° C

原料アミン(132 g, 401 mmol)を氷冷下ジクロロメタン1000 mlに懸濁させ、トリエチルアミン(123 ml, 882 mmol)、(Boc)₂O(101 ml, 440 mmol)を順に加え10分間反応させた。その後さらに室温で2時間反応させ、溶媒を留去した。クエン酸水（クエン酸一水和物50g, 水400 ml）に残渣をあけ、pH4とし、酢酸エチルで抽出した。有機層を水洗し、無水硫酸マグネシウムで乾燥し、溶媒を減圧下留去することで目的物が定量的に得られた。
¹H-NMR (DMSO-d6) δppm: 1.06-1.25 (m, 2H), 1.25-1.43 (m, 2H), 1.37 (s, 9H), 1.75-1.94 (m, 4H), 2.19 (tt, 1H, J = 11.7, 3.9 Hz), 3.07-3.24 (m, 1H), 3.58 (s, 3H), 6.74 (d, 1H, J = 6.6 Hz).

第２工程

水素化リチウムアルミニウム (18.3 g, 483 mmol)をテトラヒドロフラン800 mlに懸濁させ、第１工程で得られたエステルのテトラヒドロフラン（300 ml）溶液を氷冷下攪拌しながら1時間かけてゆっくり加えた。氷冷下で10分間反応させた後、さらに室温で2.5時間反応させた。反応液を再び氷冷し、水とテトラヒドロフランの混合液（1:1, 36 ml）、2N水酸化ナトリウム水溶液(18 ml)、水（18 ml）を順に加え20分間攪拌した。その後さらに室温で1.5時間攪拌し、析出物を濾過除去し、濾液を減圧下濃縮した。残渣に酢酸エチルおよびヘキサンを加え、析出した結晶を濾取することで目的物のアルコールが79.5 g、収率87%（第１〜２工程通算）で得られた。
1H-NMR (DMSO-d6) δppm: 0.78-1.00 (m, 2H), 1.00-1.32 (m, 3H), 1.37 (s, 9H), 1.65-1.84 (m, 4H), 3.04-3.24 (m, 3H), 4.32-4.42 (m, 1H), 6.66 (d, 1H, J = 7.8 Hz).

第３工程

原料アルコール (79.5 g, 347 mmol)をテトラヒドロフラン800 mlに溶解させ、トリエチルアミン(72.5 ml, 520 mmol)、メタンスルホニルクロライド(32.2 ml, 416 mmol)を氷冷下攪拌しながら順に加え、1.5時間反応させた。反応液をクエン酸水（クエン酸一水和物30g, 水500 ml）にあけ、pH4とし、酢酸エチルで抽出後、有機層を水洗し無水硫酸マグネシウムで乾燥した。溶媒を減圧下留去する途中に析出した結晶を濾取し、ヘキサンで洗浄することでメシレートを100 g得た。得られたメシレートをジメチルホルムアミド100 mlに溶解させ、アジ化ナトリウム(63.7 g, 980 mmol)を加え、80℃で2時間反応させた。反応液を水にあけ、酢酸エチルで抽出した。有機層を水洗し、無水硫酸マグネシウムで乾燥し、溶媒を減圧下留去することで目的物のアジドが定量的(crude重量85.4 g)に得られた。
¹H-NMR (DMSO-d6) δppm: 0.90-1.21 (m, 4H), 1.32-1.50 (m, 1H), 1.37 (s, 9H), 1.65-1.84 (m, 4H), 3.06-3.24 (m, 3H), 6.71 (d, 1H, J = 8.1 Hz).

第４工程

第３工程で得られたアジドを室温でテトラヒドロフラン900 mlに溶解させ、トリフェニルホスフィン(103 g, 392 mmol)、水(90 ml)を順に加え、80℃で1.5時間反応させた。溶媒770 mlを留去し、水300ml、酢酸エチル400 ml、2N塩酸150 mlを順に加え、pH2.5とし、分液抽出を行なった。有機層を2N塩酸で逆抽出した。酢酸エチルで洗浄した後、水層をアルカリ性とし、酢酸エチル及びクロロホルムで何度も抽出を行なった。有機層を合わせ、無水硫酸マグネシウムで乾燥した。溶媒を減圧下留去し、残渣にヘキサンを加え、析出した結晶を濾取し、ヘキサンで洗浄することで目的物のアミンが41.7 g、収率53%（第３〜４工程通算）で得られた。
¹H-NMR (DMSO-d6) δppm: 0.77-0.96 (m, 2H), 1.00-1.18 (m, 3H), 1.37 (s, 9H), 1.67-1.82 (m, 4H), 2.30-2.38 (m, 2H), 2.90-3.60 (m, 2H), 3.05-3.22 (m, 1H), 6.66 (d, 1H, J = 7.2 Hz).

第５工程

原料アミン(37.5 g, 164 mmol)をテトラヒドロフラン400 mlに懸濁させ、トリエチルアミン(91.7 ml, 656 mmol)、イソプロピルスルホニルクロライド(32.2 ml, 416 mmol)を順に-55〜-40℃で攪拌しながらゆっくり加え、0℃まで徐々に昇温しながら6時間反応させた。反応液を氷冷の希酸水溶液にあけ、酢酸エチルで抽出した。有機層を水洗し、無水硫酸マグネシウムで乾燥した。溶媒を減圧下留去し、残渣にイソプロピルエーテルを加え、析出した結晶を濾取し、イソプロピルエーテルで洗浄することで目的物のスルホンアミドが43.1 g、収率79%で得られた。
¹H-NMR (DMSO-d6) δppm: 0.79-0.98 (m, 2H), 1.00-1.36 (m, 3H), 1.20 (d, 6H, J = 6.6 Hz), 1.37 (s, 9H), 1.70-1.84 (m, 4H), 2.72-2.80 (m, 2H), 3.04-3.22 (m, 2H), 6.68 (d, 1H, J = 8.1 Hz), 6.94 (t, 1H, J = 6.0 Hz).

第６工程

Boc保護された原料アミン(43.0 g, 128 mmol)をメタノール200 mlに懸濁させ、4N 塩酸-ジオキサン溶液(96 ml, 384 mmol) を氷冷下攪拌しながら加え、20分間反応させた後、さらに室温で3時間反応させた。反応液を再び氷冷し、イソプロピルエーテル220 mlを加え、30分間攪拌した後、析出した結晶を濾取し、イソプロピルエーテルで洗浄することで目的物のアミン塩酸塩が30.8 g、収率89%で得られた。
¹H-NMR (DMSO-d6) δppm: 0.85-1.02 (m, 2H), 1.20 (d, 6H, J = 6.6 Hz), 1.20-1.40 (m, 3H), 1.75-1.84 (m, 2H), 1.90-2.00 (m, 2H), 2.73-2.82 (m, 2H), 2.83-2.97 (m, 1H), 3.08-3.20 (m, 1H), 7.01 (t, 1H, J = 5.7 Hz), 8.01 (s, 3H).

第７工程

アミン塩酸塩(1.4 g, 5.16 mmol)と2-クロロベンゾチアゾール(2.63 g, 15.5 mmol)をN-メチルピロリドン15 mlに懸濁させ、N,N-ジイソプロピルエチルアミン(4.50 ml, 25.8 mmol)を加え、2本の反応管へ封管後、マイクロウェーブ反応装置を用いて30分間220℃の条件で反応を行なった。2本の反応管から反応液を水へあけ、酢酸エチルで抽出した。有機層を水洗し、無水硫酸ナトリウムで乾燥した。溶媒を減圧下留去し、残渣をシリカゲルクロマトグラフィにより精製すると目的物化合物（Ij-62）が1.5 g、収率79 %で得られた。 Example 3 First Step of Synthesis of Compound (Ij-62)

Raw material amine (132 g, 401 mmol) was suspended in 1000 ml of dichloromethane under ice-cooling, triethylamine (123 ml, 882 mmol) and (Boc) ₂ O (101 ml, 440 mmol) were added in this order and reacted for 10 minutes. . Thereafter, the mixture was further reacted at room temperature for 2 hours, and the solvent was distilled off. The residue was poured into citric acid water (citric acid monohydrate 50 g, water 400 ml), adjusted to pH 4, and extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure to obtain the desired product quantitatively.
¹ H-NMR (DMSO-d6) δppm: 1.06-1.25 (m, 2H), 1.25-1.43 (m, 2H), 1.37 (s, 9H), 1.75-1.94 (m, 4H), 2.19 (tt, 1H , J = 11.7, 3.9 Hz), 3.07-3.24 (m, 1H), 3.58 (s, 3H), 6.74 (d, 1H, J = 6.6 Hz).

Second step

Lithium aluminum hydride (18.3 g, 483 mmol) was suspended in 800 ml of tetrahydrofuran, and a solution of the ester obtained in the first step in tetrahydrofuran (300 ml) was slowly added over 1 hour with stirring under ice cooling. After reacting for 10 minutes under ice cooling, the reaction was further allowed to proceed for 2.5 hours at room temperature. The reaction mixture was ice-cooled again, a mixture of water and tetrahydrofuran (1: 1, 36 ml), 2N aqueous sodium hydroxide solution (18 ml) and water (18 ml) were added in this order, and the mixture was stirred for 20 min. Thereafter, the mixture was further stirred at room temperature for 1.5 hours, the precipitate was removed by filtration, and the filtrate was concentrated under reduced pressure. Ethyl acetate and hexane were added to the residue, and the precipitated crystals were collected by filtration to obtain 79.5 g of the target alcohol in a yield of 87% (total of the first and second steps).
1H-NMR (DMSO-d6) δppm: 0.78-1.00 (m, 2H), 1.00-1.32 (m, 3H), 1.37 (s, 9H), 1.65-1.84 (m, 4H), 3.04-3.24 (m, 3H), 4.32-4.42 (m, 1H), 6.66 (d, 1H, J = 7.8 Hz).

Third step

Raw alcohol (79.5 g, 347 mmol) was dissolved in 800 ml of tetrahydrofuran, triethylamine (72.5 ml, 520 mmol) and methanesulfonyl chloride (32.2 ml, 416 mmol) were added in order with stirring under ice-cooling and allowed to react for 1.5 hours. It was. The reaction solution was poured into aqueous citric acid (citric acid monohydrate 30 g, water 500 ml), adjusted to pH 4, extracted with ethyl acetate, the organic layer was washed with water and dried over anhydrous magnesium sulfate. Crystals precipitated while the solvent was distilled off under reduced pressure were collected by filtration and washed with hexane to obtain 100 g of mesylate. The obtained mesylate was dissolved in 100 ml of dimethylformamide, sodium azide (63.7 g, 980 mmol) was added, and the mixture was reacted at 80 ° C. for 2 hours. The reaction mixture was poured into water and extracted with ethyl acetate. The organic layer was washed with water, dried over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure to quantitatively obtain the target azide (crude weight 85.4 g).
¹ H-NMR (DMSO-d6) δppm: 0.90-1.21 (m, 4H), 1.32-1.50 (m, 1H), 1.37 (s, 9H), 1.65-1.84 (m, 4H), 3.06-3.24 (m , 3H), 6.71 (d, 1H, J = 8.1 Hz).

4th process

The azide obtained in the third step was dissolved in 900 ml of tetrahydrofuran at room temperature, triphenylphosphine (103 g, 392 mmol) and water (90 ml) were sequentially added, and the mixture was reacted at 80 ° C. for 1.5 hours. 770 ml of the solvent was distilled off, and 300 ml of water, 400 ml of ethyl acetate and 150 ml of 2N hydrochloric acid were added in this order to adjust the pH to 2.5, followed by liquid separation extraction. The organic layer was back extracted with 2N hydrochloric acid. After washing with ethyl acetate, the aqueous layer was made alkaline and extracted several times with ethyl acetate and chloroform. The organic layers were combined and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, hexane was added to the residue, the precipitated crystals were collected by filtration, and washed with hexane to obtain 41.7 g of the target amine in a yield of 53% (total 3rd to 4th steps). It was.
¹ H-NMR (DMSO-d6) δppm: 0.77-0.96 (m, 2H), 1.00-1.18 (m, 3H), 1.37 (s, 9H), 1.67-1.82 (m, 4H), 2.30-2.38 (m , 2H), 2.90-3.60 (m, 2H), 3.05-3.22 (m, 1H), 6.66 (d, 1H, J = 7.2 Hz).

5th process

The raw material amine (37.5 g, 164 mmol) was suspended in 400 ml of tetrahydrofuran, and triethylamine (91.7 ml, 656 mmol) and isopropylsulfonyl chloride (32.2 ml, 416 mmol) were slowly stirred in this order at -55 to -40 ° C. In addition, the reaction was allowed to proceed for 6 hours while gradually raising the temperature to 0 ° C. The reaction solution was poured into an ice-cooled dilute aqueous acid solution and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous magnesium sulfate. The solvent was distilled off under reduced pressure, isopropyl ether was added to the residue, and the precipitated crystals were collected by filtration and washed with isopropyl ether to obtain 43.1 g of the desired sulfonamide in a yield of 79%.
¹ H-NMR (DMSO-d6) δppm: 0.79-0.98 (m, 2H), 1.00-1.36 (m, 3H), 1.20 (d, 6H, J = 6.6 Hz), 1.37 (s, 9H), 1.70- 1.84 (m, 4H), 2.72-2.80 (m, 2H), 3.04-3.22 (m, 2H), 6.68 (d, 1H, J = 8.1 Hz), 6.94 (t, 1H, J = 6.0 Hz).

6th process

Boc-protected raw amine (43.0 g, 128 mmol) was suspended in 200 ml of methanol, 4N hydrochloric acid-dioxane solution (96 ml, 384 mmol) was added with stirring under ice cooling, and the mixture was reacted for 20 minutes. Furthermore, it was made to react at room temperature for 3 hours. The reaction solution was ice-cooled again, 220 ml of isopropyl ether was added, and the mixture was stirred for 30 minutes.The precipitated crystals were collected by filtration and washed with isopropyl ether to obtain 30.8 g of the target amine hydrochloride, yield 89% Was obtained.
¹ H-NMR (DMSO-d6) δppm: 0.85-1.02 (m, 2H), 1.20 (d, 6H, J = 6.6 Hz), 1.20-1.40 (m, 3H), 1.75-1.84 (m, 2H), 1.90-2.00 (m, 2H), 2.73-2.82 (m, 2H), 2.83-2.97 (m, 1H), 3.08-3.20 (m, 1H), 7.01 (t, 1H, J = 5.7 Hz), 8.01 ( s, 3H).

7th process

Amine hydrochloride (1.4 g, 5.16 mmol) and 2-chlorobenzothiazole (2.63 g, 15.5 mmol) are suspended in 15 ml of N-methylpyrrolidone, and N, N-diisopropylethylamine (4.50 ml, 25.8 mmol) is added. After sealing in two reaction tubes, the reaction was carried out at 220 ° C. for 30 minutes using a microwave reactor. The reaction solution was poured into water from two reaction tubes and extracted with ethyl acetate. The organic layer was washed with water and dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and the residue was purified by silica gel chromatography to obtain 1.5 g of the desired compound (Ij-62) in a yield of 79%.

¹H-NMR (DMSO-d6) δppm: 0.80-0.98 (m, 2H), 1.02-1.18 (m, 2H), 1.17 (t, 3H, J = 7.2 Hz), 1.22-1.34 (m, 1H), 1.37 (s, 9H), 1.68-1.82 (m, 4H), 2.68-2.78 (m, 2H), 2.96 (q, 2H, J = 7.2 Hz), 3.04-3.22 (m, 1H), 6.68 (d, 1H, J = 8.1 Hz), 6.94 (t, 1H, J = 6.0 Hz). In the fifth step, ethanesulfonyl chloride was reacted instead of isopropylsulfonyl chloride to obtain the following compound in which R ¹ is an ethyl group.

¹ H-NMR (DMSO-d6) δppm: 0.80-0.98 (m, 2H), 1.02-1.18 (m, 2H), 1.17 (t, 3H, J = 7.2 Hz), 1.22-1.34 (m, 1H), 1.37 (s, 9H), 1.68-1.82 (m, 4H), 2.68-2.78 (m, 2H), 2.96 (q, 2H, J = 7.2 Hz), 3.04-3.22 (m, 1H), 6.68 (d, 1H, J = 8.1 Hz), 6.94 (t, 1H, J = 6.0 Hz).

1H-NMR (DMSO-d6) δppm: 0.79-1.00 (m, 2H), 1.01-1.20 (m, 2H), 1.22-1.34 (m, 1H), 1.25 (s, 9H), 1.37 (s, 9H), 1.70-1.86 (m, 4H), 2.81-2.90 (m, 2H), 3.04-3.22 (m, 1H), 6.68 (d, 1H, J = 8.1 Hz), 6.83 (t, 1H, J = 6.0 Hz). In the fifth step, tert-butylsulfinyl chloride was reacted instead of isopropylsulfonyl chloride, and then oxidized using mCPBA to obtain the following compound in which R ¹ is a tert-butyl group (WO2001037826, Example 3). reference).

1H-NMR (DMSO-d6) δppm: 0.79-1.00 (m, 2H), 1.01-1.20 (m, 2H), 1.22-1.34 (m, 1H), 1.25 (s, 9H), 1.37 (s, 9H) , 1.70-1.86 (m, 4H), 2.81-2.90 (m, 2H), 3.04-3.22 (m, 1H), 6.68 (d, 1H, J = 8.1 Hz), 6.83 (t, 1H, J = 6.0 Hz ).

H-NMR (DMSO-d6) δppm: 0.84-1.02 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.20-1.40 (m, 3H), 1.74-1.82 (m, 2H), 1.90-2.00 (m, 2H), 2.72-2.80 (m, 2H), 2.83-2.96 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 7.04 (t, 1H, J = 6.0 Hz), 8.03 (s, 3H).

Ｒ^１がtert-ブチル基の場合

H-NMR (DMSO-d6) δppm: 0.84-1.04 (m, 2H), 1.16-1.38 (m, 3H), 1.26 (s, 9H), 1.74-1.84 (m, 2H), 1.92-2.02 (m, 2H), 2.82-2.98 (m, 3H), 6.90 (d, 1H, J = 6.0 Hz), 8.01 (s, 3H). By using the above compound, the following compound in which R ¹ is an ethyl group or a tert-butyl group was obtained in the sixth step.
When R ¹ is an ethyl group

H-NMR (DMSO-d6) δppm: 0.84-1.02 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.20-1.40 (m, 3H), 1.74-1.82 (m, 2H), 1.90 -2.00 (m, 2H), 2.72-2.80 (m, 2H), 2.83-2.96 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 7.04 (t, 1H, J = 6.0 Hz), 8.03 (s, 3H).

When R ¹ is a tert-butyl group

H-NMR (DMSO-d6) δppm: 0.84-1.04 (m, 2H), 1.16-1.38 (m, 3H), 1.26 (s, 9H), 1.74-1.84 (m, 2H), 1.92-2.02 (m, 2H), 2.82-2.98 (m, 3H), 6.90 (d, 1H, J = 6.0 Hz), 8.01 (s, 3H).

  The following compounds synthesized in the same manner are also included in the present invention.

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2 H), 1.05-1.15 (m, 6H), 1.25 (s, 9H,), 1.15-1.32 (m, 3H), 1.41 (m, 1H), 1.75-1.98 (m, 4H), 2.11 (m, 1H), 2.58-3.38 (m, 5H), 3.58-3.76 (m, 2H), 5.17 (m, 1H), 6.25-6.92 (m, 5H) 融点：147-149℃

化合物Ia-140

¹H-NMR (CDCl₃) δ: 1.02-1.20 (m, 2 H), 1.17-1.32 (m, 2 H), 1.37 (d, 6H, J = 6.9 Hz), 1.46-1.70 (m, 4H), 1.86-1.95 (m, 2H), 2.08-2.18 (m, 2H), 3.01 (d, 2H, J = 6.9 Hz), 3.13 (m, 1H), 3.25 (m, 1H), 3.87 (d, 1H, J = 8.4 Hz) , 6.61(d, 2H, J = 8.7 Hz) , 7.39 (d, 2H, J = 8.7 Hz)

化合物Ia-141

¹H-NMR (CDCl₃) δ: 1.00-1.30 (m, 4 H), 1.37 (d, 6H, J = 6.9 Hz), 1.59 (m, 1H), 1.87-1.98 (m, 2H), 1.99-2.18 (m, 5H), 2.85 (q, 3H, J = 7.5 Hz), 2.97 (d, 2H, J = 6.9 Hz), 3.12 (m, 1H), 3.23 (m, 1H), 3.88 (d, 1H, J = 8.1 Hz) , 6.53 (d, 1H, J = 7.8 Hz) , 6.63 (brs, 1H), 7.04 (d, 1H, J = 7.8 Hz) Mass： 351[M+H]

化合物Ia-178

¹H-NMR (CDCl₃) δ: 1.08-1.36 (m, 4 H), 1.39 (s, 9H), 1.59 (m, 1H), 1.90-1.99 (m, 2H), 2.16-2.26 (m, 2H), 3.17-3.34 (m,3H), 3.69 (d, 1H, J = 9.3 Hz), 6.68 (d, 1H, J = 9.3 Hz), 7.77 (dd, 1H, J = 2.1 Hz and 9.3 Hz), 8.49 (brs, 1H) Mass：394[M+H]⁺

化合物Ib-138

¹H-NMR (CDCl₃) δ: 1.02-1.34 (m, 4 H), 1.37 (d, 6H, J = 6.6 Hz), 1.57 (m, 1H), 1.87-1.97 (m, 2H), 2.07-2.18 (m, 2H), 2.93 (d, 2H, J = 6.6 Hz), 3.13 (m, 1H), 3.25 (m, 1H), 3.99 (d, 1H, J = 8.4 Hz) , 6.38 (m, 1H) , 6.49 (brs, 1H), 6.97 (q, 1H, J = 9.3 Hz) Mass：347[M+H]

化合物Ii-2

¹H-NMR (DMSO-d₆) δ: 0.91-1.06 (m, 2H), 1.12-1.28 (m, 11H), 1.31-1.47 (m, 1H), 1.75-1.94 (m, 4H), 2.19 (t, 2H, J = 11.3 Hz), 2.79 (t, 2H, J = 6.0 Hz), 2.93-3.08 (m, 1H), 2.97 (q, 2H, J = 7.42 Hz), 3.46 (m, 2H), 3.57-3.69 (m, 2H), 5.71 (t, 1H, J = 5.2 Hz), 5.77 (d, 1H, J = 11.5 Hz), 5.88-5.96 (m, 2H), 7.01 (d, 1H, J = 7.4 Hz).

化合物Ii-3

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2 H), 1.15-1.21 (m, 1H), 1.27 (s, 9H), 1.40-1.49 (m, 2H), 1.82 (d, 2H, J = 11.6 Hz), 1.92 (d, 2H, J = 11.6 Hz), 2.79-2.84 (m, 2H), 2.97-3.10 (m, 1H), 3.24 (s, 3H), 3.55-3.62 (m, 2H), 3.84-3.91 (m, 2H), 5.50-5.59 (m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.4 Hz), 6.97 (d, 1H, J = 8.4 Hz). 融点：166-168℃

化合物Ii-4

¹H-NMR (DMSO-d₆) δ: 0.87 (t, 3H, J = 7.2 Hz), 0.93-1.06 (m, 2H), 1.13-1.21 (m, 1H), 1.26 (s, 9H), 1.37-1.49 (m, 2H), 1.61-1.72 (m, 2H), 1.82 (d, 2H, J = 12.0 Hz), 1.91 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.97-3.08 (m, 1H), 3.61-3.71 (m, 2H), 5.52-5.60 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.73 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 8.8 Hz). 融点：185-186℃

化合物Ii-5

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2H), 1.26 (s, 9H), 1.28-1.31 (m, 1H), 1.35-1.47 (m, 8H), 1.81 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.77-2.84 (m, 2H), 2.96-3.07 (m, 1H), 4.30-4.42 (m, 1H), 5.51-5.64 (m, 1H), 6.39 (d, 1H, J = 8.0 Hz), 6.55 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz), 7.07 (d, 1H, J = 8.8 Hz). 融点：156-157℃

化合物Ii-6

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.19-1.25 (m, 4H), 1.26 (s, 9H), 1.38-1.49 (m, 2H), 1.82 (d, 2H, J = 8.8 Hz), 1.91 (d, 2H, J = 8.8 Hz), 2.79-2.84 (m, 2H), 2.97-3.07 (m, 1H), 3.69-3.80 (m, 2H), 5.51-5.63 (m, 1H), 6.41 (d, 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 8.8 Hz). 融点：178-179℃

化合物Ii-7

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.19-1.22 (m, 1H), 1.26 (s, 9H), 1.38-1.48 (m, 2H), 1.82 (d, 2H, J = 11.6 Hz), 1.91 (d, 2H, J = 11.6 Hz), 2.79-2.84 (m, 2H), 2.95-3.09 (m, 1H), 3.25 (s, 3H), 5.52-5.60 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.4 Hz), 6.92 (d, 1H, J = 8.4 Hz). 融点：206-207℃

化合物Ii-8

¹H-NMR (DMSO-d₆) δ: 0.91-1.05 (m, 2H), 1.16-1.24 (m, 1H), 1.26 (s, 9H), 1.37-1.47 (m, 2H), 1.81 (d, 2H, J = 12.8 Hz), 1.90 (d, 2H, J = 12.8 Hz), 2.75-2.81 (m, 2H), 2.96-3.08 (m, 1H), 5.45-5.52 (m, 1H), 6.33 (d, 1H, J = 8.4 Hz), 6.50 (s, 1H), 6.68-6.80 (m, 2H), 11.02 (brs, 1H). 融点：213-214℃

化合物Ii-9

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2 H), 1.17-1.30 (m, 8H), 1.44 (brs, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.89 (d, 2H, J = 12.4 Hz), 2.78-2.82 (m, 2H), 2.97-3.15 (m, 2H), 3.23 (s, 3H), 3.55-3.62 (m, 2H), 3.83-3.90 (m, 2H), 5.52-5.59 (m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.55 (s, 1H), 6.92 (d, 1H, J = 8.0 Hz), 6.97 (d, 1H, J = 8.4 Hz). 融点：120-121℃

化合物Ii-10

¹H-NMR (DMSO-d₆) δ: 0.88 (t, 3H, J = 7.2 Hz), 0.93-1.08 (m, 2H), 1.17-1.30 (m, 8H), 1.44 (brs, 1H), 1.52-1.61 (m, 2H), 1.83 (d, 2H, J = 12.0 Hz), 1.90 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.98-3.15 (m, 2H), 3.62-3.71 (m, 2H), 5.52-5.60 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.57 (s, 1H), 6.92 (d, 1H, J = 8.0 Hz), 6.97 (d, 1H, J = 8.4 Hz). 融点：144-145℃

化合物Ii-11

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.15-1.30 (m, 8H), 1.33-1.50 (m, 7H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.86 (m, 2H), 2.96-3.14 (m, 2H), 4.30-4.45 (m, 1H), 5.50-5.61 (m, 1H), 6.40 (d, 1H, J = 7.6 Hz), 6.55 (s, 1H), 6.92 (d, 1H, J = 7.2 Hz), 7.07 (d, 1H, J = 7.6 Hz). 融点：137-138℃

化合物Ii-12

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.14-1.30 (m, 11H), 1.36-1.50 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.85 (m, 2H), 2.97-3.15 (m, 2H), 3.69-3.79 (m, 2H), 5.52-5.60 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.92 (d, 1H, J = 7.2 Hz), 6.98 (d, 1H, J = 8.4 Hz). 融点：158-159℃

化合物Ii-13

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.12-1.30 (m, 8H), 1.34-1.51 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.77-2.83 (m, 2H), 2.95-3.12 (m, 2H), 3.25 (s, 3H), 5.51-5.59 (m, 1H), 6.41 (d, 1H, J = 8.8 Hz), 6.56 (s, 1H), 6.86-6.97 (m, 2H). 融点：157-158℃

化合物Ii-14

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2 H), 1.12-1.30 (m, 5H), 1.38-1.50 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.77-2.85 (m, 2H), 2.90-3.09 (m, 3H), 3.23 (s, 3H), 3.55-3.61 (m, 2H), 3.84-3.91 (m, 2H), 5.52-5.60 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.55 (s, 1H), 6.89-7.00 (m, 2H). 融点：150-151℃

化合物Ii-15

¹H-NMR (DMSO-d₆) δ: 0.88 (s, 3H), 0.90 (s, 3H), 0.92-1.08 (m, 2H), 1.12-1.30 (m, 5H), 1.35-1.51 (m, 1H), 1.83 (d, 2H, J = 12.4 Hz), 1.89 (d, 2H, J = 12.4 Hz), 2.00-2.16 (m, 1H), 2.77-2.84 (m, 2H), 2.90-3.10 (m, 3H), 3.42-3.55 (m, 2H), 5.50-5.65 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.88-7.01 (m, 2H) 融点：132-133℃

化合物Ii-16

¹H-NMR (DMSO-d₆) δ: 0.87 (t, 3H, J = 6.8 Hz), 0.90-1.08 (m, 2H), 1.10-1.28 (m, 5H), 1.35-1.50 (m, 1H), 1.59-1.72 (m, 2H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.77-2.85 (m, 2H), 2.90-3.09 (m, 3H), 3.61-3.71 (m, 2H), 5.52-5.61 (m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.97 (d, 2H, J = 8.0 Hz). 融点：136-137℃

化合物Ii-17

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.12-1.28 (m, 5H), 1.33-1.50 (m, 7H), 1.81 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.90-3.08 (m, 3H), 4.28-4.44 (m, 1H), 5.49-5.79 (m, 1H), 6.39 (d, 1H, J = 8.0 Hz), 6.55 (s, 1H), 6.97 (d, 1H, J = 7.6 Hz), 7.07 (d, 1H, J = 8.0 Hz). 融点：124-125℃

化合物Ii-18

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.12-1.29 (m, 8H), 1.36-1.51 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.86 (m, 2H), 2.90-3.09 (m, 3H), 3.68-3.80 (m, 2H), 5.51-5.61 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.57 (s, 1H), 6.97 (d, 2H, J = 8.4 Hz). 融点：163-164℃

化合物Ii-19

¹H-NMR (DMSO-d₆) δ: 0.89-1.08 (m, 2H), 1.11-1.30 (m, 5H), 1.35-1.51 (m, 1H), 1.82 (d, 2H, J = 10.8 Hz), 1.89 (d, 2H, J = 10.8 Hz), 2.75-2.88 (m, 2H), 2.89-3.10 (m, 3H), 3.25 (s, 3H), 5.48-5.60 (m, 1H), 6.42 (d, 1H, J = 7.6 Hz), 6.56 (s, 1H), 6.92 (d, 1H, J = 7.6 Hz), 6.98 (d, 1H, J = 5.6 Hz). 融点：189-190℃

化合物Ii-20

¹H-NMR (DMSO-d₆) δ: 0.95-1.13 (m, 2H), 1.31-1.59 (m, 10H), 1.73-1.92 (m, 4H), 2.12-2.26 (m, 2H), 2.84 (d, 2H, J = 6.0 Hz), 3.07-3.30 (m, 4H), 4.30-4.46 (m, 1H), 5.64 (brs, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.57 (s, 1H), 7.08 (d, 1H, J = 8.4 Hz). 融点：165-166℃

化合物Ii-21

¹H-NMR (DMSO-d₆) δ: 0.86-1.25 (m, 10H), 1.40 (d, 3H, J = 6.9Hz), 1.52 (m, 1H), 1.82-1.93 (m, 4H), 2.95-3.00 (m, 5H), 3.63-3.91 (m, 2H), 4.61-4.68 (m, 1H), 6.73 (brs, 2H), 7.01 (d, 2H, J = 7.8Hz), 7.11 (d, 1H, J = 8.1Hz,).

化合物Ii-22

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2 H), 1.15-1.34 (m, 5H), 1.36-1.43 (m, 9H), 1.53 (m, 1H), 1.82.1-93 (m, 4H), 2.94-3.01 (m, 6H), 4.52 (m, 1H), 4.63 (m, 1H), 6.73 (brs, 2H), 7.02 (d, 1H, J = 7.5Hz), 7.21-7.25 (m, 1H).

化合物Ii-23

¹H-NMR (DMSO-d₆) δ: 0.86-1.04 (m, 4 H), 1.25 (s, 10H), 1.30 (s, 6H), 1.38 (s, 3H), 1.40 (s, 3H), 178-1.92 (m 4H), 2.76-2.80 (m, 2H), 3.03 (m, 1H), 4.54-4.63 (m, 1H), 5.57 (m, 1H), 6.16 (s, 1H), 6.22 (d, 1H, J = 8.4Hz), 6.76 (d, 1H, J = 8.4Hz), 6.98 (d, 1H, J = 8.4Hz).

化合物Ii-24

¹H-NMR (DMSO-d₆) δ: 0.98-1.11 (m, 5 H), 1.15-1.31 (m, 20H), 1.57 (m, 1H), 1.82.1-93 (m, 4H), 2.74-2.81 (m, 1H), 3.01-3.06 (m, 2H), 3.35 (m, 1H), 3.40 (m, 1H), 4.04-4.17 (m, 3H), 6.77 (d, 1H, J = 9.0Hz),

化合物Ii-25

¹H-NMR (DMSO-d₆) δ: 0.98-1.20 (m, 13 H), 1.30 (d, 3H, J = 3H), 1.59 (m, 1H), 1.81-1.91 (m, 4H), 2.73-2.83 (m, 1H), 2.94-3.04 (m, 4H), 3.35-3.45 (m, 2H), 4.08-4.19 (m, 3H), 6.88 (brs, 3H), 7.03 (d, 1H, J = 8.4Hz).

化合物Ii-26

¹H-NMR (DMSO-d₆) δ: 1.02-1.10 (m, 2H), 1.19-1.32 (m, 2H), 1.26 (s, 9H), 1.55 (m, 1H), 1.86-1.93 (m, 4H), 3.01-3.04 (m, 3H), 6.76 (d, 1H, J = 8.7 Hz), 7.03 (m, 1H), 7.37-7.43 (m, 3H), 7.76-7.80 (m, 1H), 8.20-8.23 (m, 1H), 8.34-8.40 (m, 1H), 8.78-8.79 (m, 1H)

化合物Ii-27

¹H-NMR (DMSO-d₆) δ: 1.03-1.10 (m, 2H), 1.20-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.53 (m, 1H), 1.88 (m, 4H), 2.99-3.15 (m, 3H), 7.33-7.35 (m, 3H), 7.71-7.75 (m, 1H), 8.16-8.18 (m, 1H), 829-8.32 (m, 1H), 8.76-8.78 (m, 1H)

化合物Ii-28

¹H-NMR (DMSO-d₆) δ: 1.04-1.11 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J =7.2 Hz), 1.59 (m, 1H), 1.87-1.91 (m, 4H), 2.93-3.08 (m, 2H), 2.97 (q, 2H, J =7.2 Hz), 3.06-3.08 (m, 2H), 7.01 (m, 1H), 7.17 (d, 1H, J =7.5Hz), 7.43 (d, 1H, J =7.5Hz), 7.50-7.57 (m, 2H), 7.80-7.84 (m, 1H), 8.25-8.27 (m, 1H), 8.39-8.44 (m, 1H), 8.80-8.82 (m, 1H)

化合物Ii-29

¹H-NMR (DMSO-d₆) δ: 0.99-1.10 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J =7.5 Hz), 1.52 (m, 1H), 1.84-1.91 (m, 4H), 2.94-3.01 (m, 5H), 6.88 (m, 1H), 7.00 (d, 1H, J =7.8 Hz), 7.26-7.28 (m, 2H), 7.38 (m, 1H), 7.76 (d, 1H, J = 3.3. Hz), 7.90 (d, 1H, J =3.3 Hz)

化合物Ii-30

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2 H), 1.18-1.33 (m, 2H), 1.26 (s, 9H), 1.45 (m, 1H), 1.78-1.97 (m, 4 H), 2.86-2.94 (m, 2H), 2.95-3.10 (m, 1H), 5.91 (m, 1H), 6.55 (d, 1H, J = 7.6 Hz), 6.63-6.71 (m, 2H), 6.73 (d, 1H, J = 8.0 Hz), 7.06 (s, 1H), 7.15 (t, 1H, J = 8.0 Hz), 7.60 (s, 1H), 8.11 (s, 1H), 8.31 (s, 1H)

化合物Ii-31

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2 H), 1.13-1.28 (m, 2H), 1.26 (s, 9H), 1.43 (m, 1H), 1.76-1.97 (m, 4 H), 2.83-3.18 (m, 3H), 5.79 (m, 1H), 6.21 (s, 2H), 6.44 (d, 1H, J = 6.8 Hz), 6.58-6.67 (m, 2H), 6.73 (d, 1H, J = 8.0 Hz), 7.10 (t, 1H, J = 8.0 Hz), 7.21 (s, 2H) 融点：205-206℃

化合物Ii-32

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2 H), 1.05-1.28 (m, 11H), 1.41 (m, 1H), 1.75-1.92 (m, 4 H), 2.11 (t, 2H, J = 10.0 Hz), 2.73-2.82 (m, 2H), 2.91-3.08 (m, 3H), 3.24 (d, 2H, J = 11.2 Hz), 3.62-3.72 (m, 2H), 5.07 (m, 1H), 6.47 (d, 2H, J = 7.2 Hz), 6.72 (d, 2H, J = 7.2 Hz), 6.97 (d, 1H, J = 7.6 Hz) 融点：165-166℃

化合物Ii-33

¹H-NMR (DMSO-d₆) δ: 0.91-1.06 (m, 2H), 1.15-1.26 (m, 8H), 1.33-1.48 (m, 1H), 1.71-1.93 (m, 4H), 2.88 (d, 2H, J = 6.5 Hz), 2.93-3.15 (m, 2H), 5.70 (brs, 2H), 6.63 (d, 2H, J = 9.1 Hz), 6.93-6.96 (m, 1H), 7.38-7.42 (m, 2H), 7.57 (d, 2H, J = 9.1 Hz), 7.88-7.93 (m, 2H)

化合物Ii-34

¹H-NMR (DMSO-d₆) δ: 0.98-1.02 (m, 2H), 1.16-1.18 (m, 5H), 1.42 (s, 1H), 1.75-1.91 (m, 4H), 2.88 (d, 2H, J = 6.6 Hz), 2.96 (q, 3H, J = 7.3 Hz), 6.63 (d, 2H, J = 8.9 Hz), 6.99-7.02 (m, 1H), 7.38-7.41 (m, 2H), 7.57 (d, 2H, J = 8.9 Hz), 7.89-7.92 (m, 2H).

化合物Ii-35

¹H-NMR (DMSO-d₆) δ: 0.90-1.52 (m, 5H), 1.19 (t, 3H, J = 7.2 Hz), 1.75-1.96 (m, 4H), 2.50-3.10 (m, 3H), 2.62 (q, 2H, J = 7.2 Hz), 5.55-5.70 (m, 1H ), 6.57 (d, 2H, J = 8.7 Hz), 6.80-7.04 (m, 4H), 7.01 (d, 1H, J = 7.8 Hz), 7.34 (d, 2H, J = 8.7 Hz)

化合物Ii-36

¹H-NMR (DMSO-d₆) δ: 0.90-1.50 (m, 5H), 1.19 (t, 3H, J = 7.2 Hz), 1.75-1.95 (m, 4H), 2.70-3.10 (m, 3H), 2.97 (q, 2H, J = 7.2 Hz), 3.70 (s, 3H), 5.40-5.50 (m, 1H ), 6.53 (d, 2H, J = 8.7 Hz), 6.74 (d, 2H, J = 8.7 Hz), 6.78-6.90 (m, 4H), 6.99 (d, 1H, J = 7.8 Hz)

化合物Ii-37

¹H-NMR (CDCl₃) δ: 1.02-1.32 (m, 4 H), 139 (s, 9H,), 1.58 (m, 1H), 1.86-1.96 (m, 2H), 2.12-2.22 (m, 2H), 3.02 (d, 2H, J = 6.6 Hz), 3.25 (m, 1H), 3.67 (d, 1H, J = 9.3 Hz) , 6.67(d, 2H, J = 8.7 Hz) , 7.41 (d, 2H, J = 8.7 Hz) Mass：393[M+H]

化合物Ii-38

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.17-1.26 (m, 2H), 1.19 (t, 3H, J = 7.1 Hz), 1.43 (s, 1H), 1.77-1.85 (m, 2H), 1.85-1.94 (m, 2H), 2.82 (t, 1H, J = 5.8 Hz), 2.98 (m, 1H), 2.97 (q, 2H, J = 7.1 Hz), 5.87 (m, 1H), 6.56 (d, 2H, J = 8.6 Hz), 6.98 (d, 1H, J = 7.6 Hz), 7.02 (d, 2H, J = 8.6 Hz).

化合物Ii-39

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.19-1.35 (m, 2H), 1.29 (s, 9H), 1.46 (s, 1H), 1.73-1.98 (m, 4H), 2.93 (m, 1H), 3.04 (m, 1H), 6.60-6.69 (m, 2H), 6.75 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 7.6 Hz), 7.49 (d, 1H, J = 8.8 Hz), 8.05 (s, 1H).

化合物Ii-40

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.16-1.29 (m, 2H), 1.19 (t, 3H, J = 7.3 Hz), 1.45 (s, 1H), 1.76-1.94 (m, 4H), 1.76 (s, 2H), 2.93 (t, 2H, J = 5.8 Hz), 2.97 (q, 2H, J = 7.3 Hz), 6.66 (s, 1H), 6.94-7.01 (m, 2H), 7.49 (d, 1H, J = 8.6 Hz), 8.04 (s, 1H).

化合物Ii-41

¹H-NMR (DMSO-d₆) δ: 0.91-1.05 (m, 2H), 1.17-1.33 (m, 2H), 1.26 (s, 9H), 1.35-1.48 (m, 1H), 1.76-1.86 (m, 2H), 1.86-1.95 (m, 2H), 2.76-2.82 (m, 1H), 2.96-3.08 (m, 1H), 3.71 (s, 3H), 5.21-5.30 (m, 1H), 6.57 (d, 1H, J = 8.6 Hz), 6.73 (d, 1H, J = 8.6 Hz), 7.02 (dd, 1H, J = 8.6, 2.3 Hz), 7.44 (d, 1H, J = 2.3 Hz).

化合物Ii-42

¹H-NMR (DMSO-d₆) δ: 0.98-1.01 (m, 2H), 1.18-1.28 (m, 2H), 1.19 (t, 3H, J = 7.1 Hz), 1.42 (s, 1H), 1.76-1.85 (m, 2H), 1.85-1.93 (m, 2H), 2.79 (t, 2H, J = 5.9 Hz), 2.97 (q, 2H, J = 7.1 Hz), 3.02 (m, 1H), 3.71 (s, 3H), 5.26 (m, 1H), 6.58 (d, 1H, J = 8.6 Hz), 6.98 (d, 2H, J = 7.8 Hz), 7.02 (d, 2H, J = 8.6 Hz), 7.44 (br s, 1H).

化合物Ii-43

¹H-NMR (DMSO-d₆) δ: 0.98-1.06 (m, 2H), 1.16-1.25 (m, 2H), 1.18 (t, 3H, J =7.5 Hz), 1.51 (m, 1H), 1.83-1.91 (m, 4H), 2.85 (t, 2H, J = 6.3 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.04(m, 1H), 3.56 (s, 3H), 5.46 (t, 1H, J = 6.3 Hz), 5.76 (s, 1H), 6.49 (d, 1H, J = 7.8 Hz), 7.21 (t, 1H, J = 7.5Hz), 7.32 (t, 2H, J = 7.5 Hz), 7.68 (d, 2H, J = 7.5 Hz)

化合物Ii-44

¹H-NMR (DMSO-d₆)δ: 0.96-1.05 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.24 (m, 2H), 1.48 (m, 1H), 1.76-1.91 (m, 4H), 2.91 (d, 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.2 Hz), 6.35 (s, 1H), 6.99 (d, 1H, J = 7.8 Hz), 7.46-7.49 (m, 3H), 7.73-7.76 (m, 2H)

化合物Ii-45

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.15-1.22 (m, 1H), 1.26 (s, 9H), 1.37-1.51 (m, 2H), 1.81 (d, 2H, J = 11.6 Hz), 1.91 (d, 2H, J = 11.6 Hz), 2.76-2.86 (m, 2H), 2.97-3.08 (m, 1H), 3.35 (s, 3H), 5.82-5.91 (m, 1H), 6.26 (d, 1H, J = 13.6 Hz), 6.39 (s, 1H), 6.73 (brs, 1H). 融点：215-216℃

化合物Ii-46

¹H-NMR (CDCl₃) δ: 1.02-1.32 (m, 4H), 1.24 (d, 6H, J = 6.0 Hz), 1.39 (s, 9H), 1.54 (m, 1H), 1.84-1.94 (m, 2H), 2.12-2.22 (m, 2H), 2.39 (t, 2H, J = 10.5 Hz), 2.94 (d, 2H, J = 6.9 Hz), 3.24 (m, 1H), 3.38 (d, 1H, J = 9.6 Hz), 3.61 (d, 1H, J = 9.6 Hz), 3.72-4.00 (m, 2H), 5.83-5.94 (m, 1H), 5.96-6.10 (m, 2H).

化合物Ii-47

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.16-1.34 (m, 11H), 1.40 (m, 1H), 1.79 (d, 2H, J = 12.5 Hz), 1.90 (d, 2H, J = 11.9 Hz), 2.82 (t, 2H, J = 5.5 Hz), 3.01 (m, 1H), 6.12-6.18 (m, 3H), 6.30 (t, 1H, J = 5.5 Hz), 6.76 (d, 1H, J = 8.7 Hz).

化合物Ii-48

¹H-NMR (CDCl₃) δ: 1.00-1.28 (m, 4H), 1.39 (s, 9H), 1.56 (m, 1H), 1.91 (d, 2H, J = 12.4 Hz), 2.08-2.21 (m, 4H), 2.58 (t, 2H, J = 8.1 Hz), 2.97 (d, 2H, J = 6.0 Hz), 3.23 (m, 1H), 3.70 (d, 1H, J = 9.4 Hz), 3.80 (t, 2H, J = 7.1 Hz), 6.66 (d, 2H, J = 8.7 Hz), 7.36 (d, 2H, J = 8.7 Hz).

化合物Ii-49

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.17-1.33 (m, 11H), 1.41 (m, 1H), 1.80 (d, 2H, J = 12.9 Hz), 1.90 (d, 2H, J = 11.4 Hz), 2.82 (t, 2H, J = 6.1 Hz), 3.01 (m, 1H), 6.07 (t, 1H, J = 5.3 Hz), 6.34-6.43 (m, 2H), 6.51 (dd, 1H, J1 = 8.2 Hz, J2 = 1.8 Hz), 6.75 (d, 1H, J = 8.5 Hz), 7.11 (t, 1H, 8.2 Hz).

化合物Ii-50

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.14-1.31 (m, 8H), 1.43 (m, 1H), 1.76-1.94 (m, 4H), 2.82 (t, 2H, J = 6.0 Hz), 2.95-3.16 (m, 2H), 5.90 (t, 1H, J = 5.5 Hz), 6.56 (d, 2H, J = 8.7 Hz), 6.95 (d, 1H, J = 7.9 Hz), 7.03 (d, 2H, J = 8.6 Hz).

化合物Ii-51

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.13-1.31 (m, 8H), 1.42 (m, 1H), 1.76-1.94 (m, 4H), 2.83 (t, 2H, J = 6.0 Hz), 2.95-3.16 (m, 2H), 6.07 (t, 1H, J = 5.4 Hz), 6.36-6.46 (m, 2H), 6.53 (dd, 1H, J1 = 8.1 Hz, J2 = 1.9 Hz), 6.95 (d, 1H, J = 7.9 Hz), 7.12 (d, 1H, J = 8.1 Hz).

化合物Ii-52

¹H-NMR (DMSO-d₆) δ: 0.91-1.10 (m, 2H), 1.19-1.37 (m, 11H), 1.45 (m, 1H), 1.78-1.90 (m, 4H), 2.84 (t, 2H, J = 6.0 Hz), 3.04 (m, 1H), 4.64 (q, 2H, J = 9.0 Hz), 5.73 (t, 1H, J = 5.4 Hz), 6.13-6.21 (m, 2H), 6.26 (d, 1H, J = 7.2 Hz), 6.78 (d, 1H, J = 8.4 Hz), 6.99 (t, 1H, 8.0 Hz).

化合物Ii-53

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.13-1.30 (m, 8H), 1.42 (m, 1H), 1.75-1.93 (m, 4H), 2.80 (t, 2H, J = 6.2 Hz), 2.93-3.16 (m, 2H), 5.66 (t, 1H, J = 5.5 Hz), 6.53 (d, 2H, J = 9.1 Hz), 6.89 (d, 2H, J = 8.8 Hz), 6.92 (t, 1H, J_H-F = 75 Hz), 6.94 (d, 1H, J = 8.0 Hz).

化合物Ii-54

¹H-NMR (DMSO-d₆) δ: 0.88-1.05 (m, 2H), 1.14-1.32 (m, 11H), 1.41 (m, 1H), 1.75-1.94 (m, 4H), 2.77 (t, 2H, J = 6.0 Hz), 3.01 (m, 1H), 4.54 (q, 2H, J = 9.0 Hz), 5.33 (t, 1H, J = 5.8 Hz), 6.49 (d, 2H, J = 8.8 Hz), 6.75 (d, 1H, J = 8.8 Hz), 6.80 (d, 2H, J = 8.8 Hz).

化合物Ii-55

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.14-1.31 (m, 8H), 1.40 (m, 1H), 1.74-1.93 (m, 4H), 2.79 (t, 2H, J = 5.9 Hz), 2.94-3.15 (m, 6H), 3.69 (t, 4H, J = 4.8 Hz), 5.70-5.94 (m, 4H), 6.94 (d, 1H, J = 8.0 Hz).

化合物Ii-56

¹H-NMR (DMSO-d₆) δ: 0.98-1.14 (m, 2H), 1.15-1.32 (m, 5H), 1.54 (m, 1H), 1.83-1.96 (m, 4H), 2.89-3.10 (m, 5H), 6.17 (t, 1H, J = 5.2 Hz), 6.63 (d, 1H, J = 2.2 Hz), 7.02 (d, 1H, J = 7.7 Hz), 7.21 (dd, 1H, J1 = 9.1 Hz, J2 = 2.5 Hz), 7.27 (dd, 1H, J1 = 8.2 Hz, J2 = 4.4 Hz), 7.67 (d, 1H, J = 9.1 Hz), 7.97 (d, 1H, J = 8.2 Hz), 8.45 (dd, 1H, J1 = 4.3 Hz, J2 = 1.5 Hz).

化合物Ii-57

¹H-NMR (DMSO-d₆) δ: 0.97-1.14 (m, 2H), 1.17-1.34 (m, 8H), 1.54 (m, 1H), 1.83-1.96 (m, 4H), 2.94 (t, 2H, J = 6.0 Hz), 2.99-3.18 (m, 2H), 6.17 (t, 1H, J = 5.4 Hz), 6.63 (d, 1H, J = 2.5 Hz), 6.96 (d, 1H, J = 7.7 Hz), 7.21 (dd, 1H, J1 = 9.1 Hz, J2 = 2.5 Hz), 7.27 (dd, 1H, J1 = 8.2 Hz, J2 = 4.1 Hz), 7.67 (d, 1H, J = 9.1 Hz), 7.97 (d, 1H, J = 8.0 Hz), 8.45 (dd, 1H, J1 = 4.3 Hz, J2 = 1.5 Hz).

化合物Ii-58

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.12-1.29 (m, 5H), 1.40 (m, 1H), 1.74-1.93 (m, 4H), 2.80 (t, 2H, J = 5.9 Hz), 2.92-3.07 (m, 7H), 3.69 (t, 4H, J = 4.8 Hz), 5.69-5.95 (m, 4H), 6.99 (d, 1H, J = 7.7 Hz).

化合物Ii-59

¹H-NMR (DMSO-d₆) δ: 0.94-1.11 (m, 2H), 1.14-1.30 (m, 5H), 1.47 (m, 1H), 1.78-1.95 (m, 4H), 2.88-3.09 (m, 5H), 3.80 (s, 3H), 6.09 (t, 1H, J = 5.6 Hz), 6.81-6.86 (m, 1H), 6.96 (dd, 1H, J1 = 8.8 Hz, J2 = 2.8 Hz), 7.01 (d, 1H, J = 7.4 Hz), 7.29 (t, 1H, J = 8.0 Hz), 7.45-7.51 (m, 2H), 7.66 (d, 1H, J = 8.5 Hz), 8.04 (d, 1H, J = 2.8 Hz).

化合物Ii-60

¹H-NMR (DMSO-d₆) δ: 1.03 (m, 2H), 1.19 (t, 2H, J = 7.8 Hz), 1.21 (m, 2H), 1.46 (m, 1H), 1.76-1.95 (m, 4H), 2.90 (t, 2H, J = 5.8 Hz), 2.97 (q, 2H, J = 7.3 Hz), 3.03 (m, 1H), 3.80 (s, 3H), 5.95 (m, 1H), 6.90 (m, 1H), 6.98 (d, 1H, J = 7.8 Hz), 6.98 (dd, 1H, J = 7.8, 7.8 Hz), 7.06 (d, 1H, J = 8.6 Hz), 7.26 (dd, 1H, J = 7.8, 7.8 Hz), 7.61 (d, 1H, J = 8.6 Hz), 7.69 (d, 1H, J = 7.8 Hz), 8.03 (s, 1H).

化合物Ii-61

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.18-1.29 (m,2H), 1.19 (t, 3H, J = 7.6 Hz), 1.47 (m, 1H), 1.87 (m, 5H), 2.90 (t, 2H, J = 6.3 Hz), 2.97 (q, 2H, J = 7.6 Hz), 3.02 (m, 1H), 5.98 (m, 1H), 6.63 (d, 2H, J = 8.3 Hz), 6.98 (d, 1H, J = 7.3 Hz), 7.14 (m, 1H), 7.73 (s, 2H), 7.83 (d, 2H, J = 8.3 Hz), 8.52 (d, 1H, J = 4.0 Hz).

化合物Ii-62

¹H-NMR (DMSO-d₆) δ: 0.98-1.01 (m, 2H), 1.20 (s, 9H), 1.20-1.37 (m, 2H), 1.42 (m, 1H), 1.76-1.96 (m, 4H), 2.28-2.37 (m, 2H), 2.75-2.85 (m, 2H), 3.02 (m, 1H), 3.36 (t, 2H, J = 7.8 Hz), 3.57 (t, 2H, J = 6.3 Hz), 5.66 (m, 1H), 6.54 (d, 2H, J = 8.0 Hz), 6.73 (d, 1H, J = 8.6 Hz), 7.00 (d, 1H, J = 8.0 Hz).

化合物Ii-63

¹H-NMR (DMSO-d₆) δ: 0.96-1.14 (m, 2H), 1.14-1.32 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.50 (m, 1H), 1.76-1.96 (m, 4H), 2.91-3.10 (m, 3H), 2.97 (q, 2H, J = 7.2 Hz), 6.28 (m, 1H), 7.02 (d, 1H, J = 7.8 Hz), 7.32-7.46 (m, 3H), 8.20 (d, 1H, J = 6.9 Hz), 8.22 (s, 2H).

化合物Ii-64

¹H-NMR (DMSO-d₆) δ: 1.03-1.15 (m, 2H), 1.18-1.29 (m, 2H), 1.24 (d, 6H, J = 6.3 Hz), 1.52 (m, 1H), 1.86-1.94 (m, 2H), 2.10-2.19 (m, 2H), 2.40 (t, 2H, J = 6.0 Hz), 2.95 (d, 2H, J = 6.0 Hz), 3.23 (m, 1H), 3.40 (d, 2H, J = 11.4 Hz), 3.75-3.85 (m, 2H), 3.86 (d, 1H, J = 9.3 Hz), 6.14 (d, 1H, J = 8.5 Hz), 6.15 (s, 1H), 6.29 (d, 1H, J = 8.5 Hz), 7.06 (d, 1H, J = 8.5 Hz).

化合物Ii-65

¹H-NMR (CDCl₃) δ:1.08-1.16 (m, 2H), 1.14 (d, 6H, J = 6.8 Hz), 1.21-1.30 (m, 2H), 1.29 (s, 9H), 1.78 (t, 2H, J = 10.6 Hz), 1.83-1.92 (m, 2H), 2.11-2.19 (m, 2H), 2.78 (d, 2H, J = 10.6 Hz), 3.06 (s, 2H), 3.23 (m, 1H), 3.38 (s, 2H), 3.70-3.80 (m, 2H), 4.02 (d, 1H, J = 9.9 Hz), 5.37 (s, 1H), 6.30 (s, 1H).

化合物Ii-66

¹H-NMR (DMSO-d₆) δ: 1.01-1.12 (m, 2H), 1.20-1.34 (m, 2H), 1.27 (s, 9H), 1.54 (m, 1H), 1.82-1.99 (m, 4H), 2.91-2.98 (m, 2H), 3.06 (m ,1H), 6.17 (s, 1H), 6.63 (s, 1H), 6.78 (d, 1H, J = 9.0 Hz), 7.20 (m, 1H), 7.27 (m, 1H), 7.77 (d, 1H, J = 9.0 Hz), 7.98 (d, 1H, J = 9.0 Hz), 8.54 (s, 1H).

化合物Ii-67

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 1.88-1.96 (m, 2H), 2.78-2.86 (m, 2H), 3.02 (m ,1H), 5.89 (s, 1H), 6.56 (d, 1H, J = 8.4 Hz), 6.76 (d, 1H, J = 8.4 Hz), 7.02 (d, 1H, J = 8.4 Hz).

化合物Ii-68

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.19 (s, 9H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.80-1.96 (m, 4H), 2.77 (s, 2H), 3.04 (m, 1H), 5.29 (s, 1H), 6.44 (d, 1H, J = 7.2 Hz), 6.68 (d, 1H, J = 7.2 Hz), 6.75 (d, 1H, J = 8.4 Hz).

化合物Ii-69

¹H-NMR (DMSO-d₆) δ: 0.95-1.10 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.47 (m, 1H), 1.80-1.88 (m, 2H), 1.88-1.95 (m, 2H), 2.88-2.95 (m, 2H), 3.02 (s, 1H), 6.07 (m, 1H), 6.77 (d, 1H, J = 8.4 Hz), 6.97 (d, 1H, J = 7.6 Hz), 7.26 (t, 1H, J = 7.6 Hz), 7.35-7.42 (m, 2H), 7.46 (d, 1H, J = 8.4 Hz), 7.91 (d, 1H, J = 7.6 Hz), 8.04 (s, 1H).

化合物Ii-70

¹H-NMR (DMSO-d₆) δ: 0.93-1.05 (m, 2H), 1.10-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.78-1.86 (m, 2H), 1.86-1.95 (m, 2H), 2.78-2.83 (m, 2H), 3.03 (m, 1H), 4.80 (q, 2H, J = 9.2 Hz), 5.48 (t, 1H, J = 5.6 Hz), 6.69-6.76 (m, 2H), 7.08 (dd, 1H, J = 8.8, 2.4 Hz), 7.45 (d, 1H, J = 2.4 Hz).

化合物Ii-71

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.20-1.32 (m, 2H), 1.27 (s, 9H), 1.82-1.88 (m, 2H), 1.88-1.97 (m, 2H), 2.83-2.88 (m, 2H), 3.04 (m, 1H), 5.82 (s, 1H), 6.69 (m, 1H), 6.76 (d, 1H, J = 8.8 Hz), 7.12 (dd, 1H, J = 9.2, 8.8 Hz), 7.37 (m, 1H), 7.87 (d, 1H, J = 2.8 Hz), 7.99 (s, 1H).

化合物Ii-72

化合物Ii-73

化合物Ii-74

化合物Ii-75

化合物Ii-76

化合物Ii-77

化合物Ii-78

化合物Ii-79

化合物Ii-80

化合物Ii-81

化合物Ii-82

化合物Ii-83

化合物Ii-84

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2H), 1.14-1.30 (t, 3H, J = 7.5 Hz ), 1.41 (m, 1H), 1.73-1.94 (m, 4H), 2.34-2.46 (m, 2H), 2.85 (t, 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.25 (t, 2H, J = 7.5 Hz), 3.53 (t, 2H, J = 6.6 Hz), 6.27 (d, 2H, J = 11.7 Hz), 6.52 (t, 1H, J = 5.1 Hz), 7.00 (d, 1H, J = 7.2 Hz).

化合物Ii-85

化合物Ii-86

化合物Ii-87

化合物Ii-88

化合物Ii-89

化合物Ii-90

化合物Ii-91

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.13 (d, 6H, J = 6.0 Hz), 1.18-1.30 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.40 (m, 1H), 1.76-1.83 (m, 2H), 1.83-1.93 (m, 2H), 2.19 (dd, 1H, J = 11.2, 11.2 Hz), 2.76-2.82 (m, 2H), 3.01 (m, 1H), 3.09 (m, 1H), 3.45 (d, 2H, J = 11.2 Hz), 3.58-3.69 (m, 2H), 5.67 (m, 1H), 5.77 (d, 1H, J = 12.0 Hz), 5.90 (s, 1H), 5.91 (m, 1H), 6.91 (d, 1H, J = 7.6 Hz).

化合物Ii-92

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.14-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.75-1.92 (m, 4H), 2.78-2.83 (m, 2H), 2.95-3.18 (m, 6H), 3.66-3.72 (m, 4H), 5.75 (brs, 1H), 6.00 (s, 1H), 6.04 (s, 1H), 6.11 (s, 1H), 6.95 (d, 1H, J = 9.0 Hz).

化合物Ii-93

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.13-1.27 (m, 5H), 1.42 (m, 1H), 1.74-1.93 (m, 4H), 2.30-2.40 (m, 2H), 2.81 (d, 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.49 (t, 2H, J = 7.5 Hz), 3.66 (t, 2H, J = 6.6 Hz), 5.00-5.50 (brs, 2H), 6.07-6.15 (m, 2H), 6.25(s, 1H), 7.00 (d, 1H, J = 6.6Hz).

化合物Ii-94

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.15-1.32 (m, 5H), 1.21 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.74-1.93 (m, 4H), 2.30-2.42 (m, 2H), 2.81 (d, 2H, J = 6.6 Hz), 2.92-3.18 (m, 2H), 3.49 (t, 2H, J = 7.5 Hz), 3.66 (t, 2H, J = 6.6 Hz), 4.70-5.30 (brs, 2H), 6.05-6.16 (m, 2H), 6.25 (s, 1H), 6.95 (d, 1H, J = 8.1Hz).

化合物Ii-95

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.16-1.31 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.73-1.94 (m, 4H), 2.34-2.46 (m, 2H), 2.84 (t, 2H, J = 6.0 Hz), 2.94-3.16 (m, 2H), 3.28 (t, 2H, J = 7.5 Hz), 3.53 (t, 2H, J = 6.6 Hz), 6.27 (d, 2H, J = 11.7 Hz), 6.52 (t, 1H, J = 5.4 Hz), 6.94 (d, 1H, J = 7.8 Hz).

化合物Ii-96

¹H-NMR (DMSO-d₆) δ: 0.91-1.04 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.40 (m, 1H), 1.76-1.95 (m, 4H), 2.77-2.83 (m, 2H), 2.99-3.04 (m, 5H), 3.67-3.72 (m, 4H), 5.71 (m, 1H), 5.79 (d, 1H, J = 11.7 Hz), 5.89 (s, 1H), 5.90 (m, 1H), 6.72 (d, 1H, J = 8.4 Hz).

化合物Ii-97

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.41 (m, 1H), 1.77-1.93 (m, 4H), 2.78-2.83 (m, 2H), 2.97-3.05 (m, 5H), 3.68-3.72 (m, 4H), 5.36 (m, 1H), 6.04 (d, 1H, J = 8.0 Hz), 6.10 (s, 1H), 6.11 (d, 1H, J = 8.0 Hz), 6.72 (d, 1H, J = 8.0 Hz), 6.89 (dd, 1H, J = 8.0, 8.0 Hz).

化合物Ii-98

¹H-NMR (DMSO-d₆) δ: 0.92-1.04 (m, 2H), 1.17-1.29 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.41 (m, 1H), 1.75-1.92 (m, 4H), 2.77-2.83 (m, 2H), 2.95-3.05 (m, 5H), 3.09 (m, 1H), 3.67-3.72 (m, 4H), 5.36 (m, 1H), 6.04 (d, 1H, J = 8.0 Hz), 6.10 (s, 1H), 6.11 (d, 1H, J = 8.0 Hz), 6.89 (dd, 1H, J = 8.0, 8.0 Hz), 6.92 (d, 1H, J = 8.0 Hz).

化合物Ii-99

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.15-1.31 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.47-1.62 (m, 6H), 1.74-1.94 (m, 4H), 2.78 (t, 2H, J = 6.0 Hz), 2.93-3.16 (m, 6H), 5.64-5.76 (m, 2H), 5.83-5.92 (m, 2H), 6.94 (d, 1H, J = 7.8 Hz).

化合物Ii-100

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.74-1.96 (m, 8H), 2.79 (t, 2H, J = 6.0 Hz), 2.93-3.18 (m, 6H), 5.48-5.67 (m, 4H), 6.94 (d, 1H, J = 8.1 Hz).

化合物Ii-101

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.13-1.29 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.39 (m, 1H), 1.47-1.62 (m, 6H), 1.75-1.94 (m, 4H), 2.79 (t, 2H, J = 6.0 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.03-3.10 (m, 4H), 5.64-5.75 (m, 2H), 5.83-5.91 (m, 2H), 7.00 (d, 1H, J = 7.8 Hz).

化合物Ii-102

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.13-1.29 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.41 (m, 1H), 1.74-1.96 (m, 8H), 2.79 (t, 2H, J = 6.0 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.09-3.19 (m, 4H), 5.46-5.66 (m, 4H), 6.99 (d, 1H, J = 7.2 Hz).

化合物Ii-103

¹H-NMR (DMSO-d₆) δ: 0.91-1.03 (m, 2H), 1.16-1.29 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.40 (m, 1H), 1.75-1.92 (m, 4H), 2.20 (s, 3H), 2.35-2.43 (m, 4H), 2.75-2.82 (m, 2H), 2.88-3.13 (m, 6H), 5.67 (m, 1H), 5.76 (d, 1H, J = 11.2 Hz), 5.82-5.92 (m, 2H), 6.91 (d, 1H, J = 8.0 Hz).

化合物Ii-104

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 2H), 1.19-1.32 (m, 2H), 1.26 (s, 9H), 1.39 (m, 1H), 1.75-1.95 (m, 4H), 2.19 (s, 3H), 2.38-2.42 (m, 4H), 2.77-2.83 (m, 5H), 2.98-3.09 (m, 5H), 5.67 (m, 1H), 5.76 (d, 1H, J = 11.2 Hz), 5.88 (m, 1H), 5.88 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz).

化合物Ii-105

¹H-NMR (DMSO-d₆) δ: 0.95-1.09 (m, 2H), 1.18-1.31 (m, 2H), 1.22 (d, 6H, J = 6.8 Hz), 1.44 (m, 1H), 1.78-1.93 (m, 4H), 2.87-2.92 (m, 2H), 3.03 (m, 1H), 3.10 (m, 1H), 6.13 (m, 1H), 6.21 (m, 1H), 6.22 (s, 2H), 6.51 (s, 1H), 6.52 (d, 1H, J = 8.0 Hz), 6.92 (d, 1H, J = 8.0 Hz), 7.26 (s, 2H).

化合物Ii-106

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.17-1.29 (m, 5H), 1.40-1.68 (m, 3H), 1.80-1.92 (m, 2H), 2.90 (t, 2H, J = 6.0 Hz), 2.94-3.06 (m, 3H), 6.12-6.22 (m, 4H), 6.50-6.54 (m, 2H), 6.94-7.00 (m, 1H), 7.26-7.27 (m, 2H).

化合物Ii-107

¹H-NMR (DMSO-d₆) δ: 0.91-1.03 (m, 2H), 1.16-1.29 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.40 (m, 1H), 1.74-1.92 (m, 4H), 2.75-2.81 (m, 2H), 2.84 (s, 3H), 3.00 (m, 1H), 3.09 (m, 1H), 3.25 (s, 3H), 3.35-3.47 (m, 4H), 5.59-5.67 (m, 4H), 6.91 (d, 1H, J = 8.0 Hz).

化合物Ii-108

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.18-1.32 (m, 2H), 1.26 (s, 9H), 1.40 (m, 1H), 1.75-1.94 (m, 4H), 2.75-2.81 (m, 2H), 2.83 (s, 3H), 3.01 (m, 1H), 3.25 (s, 3H), 3.34-3.47 (m, 4H), 5.58-5.70 (m, 4H), 6.72 (d, 1H, J = 8.4 Hz).

化合物Ii-109

¹H-NMR (DMSO-d₆) δ: 0.90-1.51 (m, 10H), 1.21 (d, 6H, J = 6.9 Hz), 1.56-1.67 (m, 3H), 1.71-1.93 (m, 6H), 2.64 (s, 3H), 2.78 (t, 2H, J = 6.0 Hz), 2.93-3.17 (m, 2H), 3.44 (m, 1H), 5.56-5.77 (m, 4H), 6.94 (d, 1H, J = 7.8 Hz).

化合物Ii-110

¹H-NMR (DMSO-d₆) δ: 0.83-1.01 (m, 2H), 1.00-1.40 (m, 3H), 1.21 (d, 6H, J = 6.9 Hz), 1.68-1.91 (m, 4H), 2.73 (t, 2H, J = 6.0 Hz), 2.90-3.15 (m, 2H), 2.95 (s, 3H), 4,48 (s, 2H), 5.60-5.72 (m, 4H), 6.94 (d, 1H, J = 7.8 Hz), 7.15-7.35 (m, 5H).

化合物Ii-111

¹H-NMR (DMSO-d₆) δ: 0.97-1.14 (m, 2H), 1.14-1.33 (m, 5H), 1.45-1.61 (m, 1H), 1.81-1.96 (m, 4H), 2.90-3.10 (m, 5H), 6.34 (t, 1H, J = 5.2 Hz), 6.51 (d, 1H, J = 2.2 Hz), 6.99-7.07 (m, 2H), 7.36 (dd, 1H, J = 8.2, 4.1 Hz), 8.02 (d, 1H, J = 8.5 Hz), 8.48 (dd, 1H, J = 4.1, 1.4 Hz).

化合物Ii-112

¹H-NMR (DMSO-d₆) δ: 0.97-1.13 (m, 2H), 1.17-1.34 (m, 8H), 1.45-1.59 (m, 1H), 1.81-1.99 (m, 4H), 2.94 (t, 2H, J = 5.9 Hz), 2.99-3.21 (m, 2H), 6.33 (t, 1H, J = 5.4 Hz), 6.51 (d, 1H, J = 2.2 Hz), 6.96 (d, 1H, J = 7.7 Hz), 7.02 (dd, 1H, J = 13.5, 2.2 Hz), 7.36 (dd, 1H, J = 8.2, 4.1 Hz), 8.02 (d, 1H, J = 8.5 Hz), 8.48 (dd, 1H, J = 4.1, 1.4 Hz).

化合物Ii-113

¹H-NMR (DMSO-d₆) δ: 0.93-1.13 (m, 2H), 1.15-1.34 (m, 8H), 1.39-1.57 (m, 1H), 1.79-1.95 (m, 4H), 2.87 (t, 2H, J = 6.2 Hz), 2.94-3.16 (m, 2H), 3.54 (s, 3H), 5.66 (t, 1H, J = 5.5 Hz), 6.49 (d, 1H, J = 9.6 Hz), 6.73 (d, 1H, J = 2.8 Hz), 6.91-7.02 (m, 2H), 7.29 (d, 1H, J = 9.3 Hz), 7.72 (d, 1H, J = 9.3 Hz).

化合物Ii-114

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.14-1.33 (m, 8H), 1.41-1.56 (m, 1H), 1.79-1.94 (m, 4H), 2.89 (t, 2H, J = 6.0 Hz), 2.95-3.16 (m, 2H), 6.00 (t, 1H, J = 5.4 Hz), 6.84 (dd, 1H, J = 8.8, 2.2 Hz), 6.95 (d, 1H, J = 8.0 Hz), 7.07 (d, 1H, J = 2.2 Hz), 7.72 (d, 1H, J = 8.8 Hz), 8.86 (s, 1H).

化合物Ii-115

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 4H), 1.26 (s, 9H), 1.40-1.51 (m, 1H), 1.84 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.85-2.90 (m, 2H), 2.97-3.06 (m, 1H), 5.93-5.99 (m, 1H), 6.63-6.79 (m, 3H), 7.40 (d, 1H, J = 8.8 Hz), 8.32 (s, 1H).

化合物Ii-116

¹H-NMR (DMSO-d₆) δ: 0.95-1.07 (m, 4H), 1.26 (s, 9H), 1.39-1.47 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.87-2.93 (m, 2H), 2.98-3.06 (m, 1H), 3.37 (s, 3H), 6.27 (s, 1H), 6.55 (d, 1H, J = 8.8 Hz), 6.73 (d, 1H, J = 8.8 Hz), 6.80 (t, 1H, J = 5.2 Hz), 7.32 (d, 1H, J = 8.8 Hz).

化合物Ii-117

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 4H), 1.20 (s, 3H), 1.22 (s, 3H), 1.39-1.51 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.88 (d, 2H, J = 12.4 Hz), 2.87-2.94 (m, 2H), 2.97-3.07 (m, 1H), 3.08-3.14 (m, 1H), 3.37 (s, 3H), 6.27 (s, 1H), 6.55 (d, 1H, J = 8.4 Hz), 6.82 (t, 1H, J = 5.6 Hz), 6.94 (d, 1H, J = 8.0 Hz), 7.32 (d, 1H, J = 8.4 Hz).

化合物Ii-118

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 4H), 1.26 (s, 9H), 1.38-1.50 (m, 1H), 1.83 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.80-2.86 (m, 2H), 2.96-3.06 (m, 1H), 3.26 (s, 3H), 5.58-5.65 (m, 1H), 6.27 (d, 1H, J = 8.4 Hz), 6.38 (s, 1H), 6.75 (d, 1H, J = 8.4 Hz), 6.99 (d, 1H, J = 8.4 Hz).

化合物Ii-119

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 4H), 1.26 (s, 9H), 1.39-1.50 (m, 1H), 1.84 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.81-2.89 (m, 2H), 2.96-3.07 (m, 1H), 3.51 (s, 3H), 5.79-5.84 (m, 1H), 6.60 (s, 1H), 6.75 (d, 1H, J = 8.8 Hz), 7.03 (d, 1H, J = 8.8 Hz), 7.19 (d, 1H, J = 8.8 Hz).

化合物Ii-120

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 4H), 1.26 (s, 9H), 1.37-1.40 (m, 1H), 1.42 (s, 3H), 1.44 (s, 3H), 1.83 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.79-2.96 (m, 2H), 2.97-3.07 (m, 1H), 4.33-4.46 (m, 1H), 5.50-5.59 (m, 1H), 6.25 (d, 1H, J = 8.8 Hz), 6.57 (s, 1H), 6.75 (d, 1H, J = 8.4 Hz), 7.00 (d, 1H, J = 8.4 Hz).

化合物Ii-121

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.26 (s, 9H), 1.36-1.49 (m, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.80-2.87 (m, 2H), 2.95-3.97 (m, 1H), 3.27 (s, 3H), 5.85-5.92 (m, 1H), 6.33 (s, 1H), 6.36 (s, 1H), 6.75 (d, 1H, J = 8.8 Hz).

化合物Ii-122

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 4H), 1.26 (s, 9H), 1.38-1.41 (m, 1H), 1.42 (s, 3H), 1.43 (s, 3H), 1.82 (d, 2H, J = 11.8 Hz), 1.90 (d, 2H, J = 11.8 Hz), 2.83-2.88 (m, 2H), 2.98-3.06 (m, 1H), 4.33-4.47 (m, 1H), 6.35 (s, 1H), 6.54 (s, 1H), 6.76 (d, 1H, J = 8.4 Hz), 8.32 (s, 1H).

化合物Ii-123

¹H-NMR (DMSO-d₆) δ: 0.93-1.06 (m, 4H), 1.22 (s, 3H), 1.24 (s, 3H), 1.26 (s, 9H), 1.39-1.50 (m, 1H), 1.81 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.87-2.93 (m, 2H), 2.96-3.07 (m, 1H), 4.39-4.47 (m, 1H), 6.30 (s, 1H), 6.54 (d, 1H, J = 8.8 Hz), 6.77 (d, 1H, J = 8.8 Hz), 6.86 (t, 1H, J = 5.2 Hz), 7.32 (d, 1H, J = 8.4 Hz).

化合物Ii-124

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 4H), 1.26 (s, 9H), 1.36-1.51 (m, 1H), 1.79 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.80-2.86 (m, 2H), 3.01 (s, 3H), 3.02-3.05 (m, 1H), 3.49 (t, 2H, J = 4.8 Hz), 4.26 (t, 2H, J = 4.8 Hz), 6.02 (s, 1H), 6.20 (t, 1H, J = 5.6 Hz), 6.31 (d, 1H, J = 8.8 Hz), 6.74 (d, 1H, J = 8.8 Hz), 7.43 (d, 1H, J = 8.4 Hz).

化合物Ii-125

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 4H), 1.08 (t, 3H, J = 7.2 Hz), 1.25 (s, 9H), 1.35-1.42 (m, 1H), 1.79 (d, 2H, J = 12.0 Hz), 1.90 (d, 2H, J = 12.0 Hz), 2.80-2.86 (m, 2H), 2.96-3.05 (m, 1H), 3.42-3.51 (m, 4H), 4.20-4.26 (m, 2H), 6.03 (s, 1H), 6.20 (s, 1H), 6.31 (d, 1H, J = 8.8 Hz), 6.75 (d, 1H, J = 8.8 Hz), 7.42 (d, 1H, J = 8.8 Hz).

化合物Ii-126

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 4H), 1.09 (s, 3H), 1.11 (s, 3H), 1.25 (s, 9H), 1.43−1.55 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.0 Hz), 2.84 (m, 2H), 2.97-3.08 (m, 1H), 3.37 (t, 2H, J = 5.2 Hz), 4.18 (t, 2H, J = 5.2 Hz), 4.71-4.80 (m, 1H), 6.05 (s, 1H), 6.19 (t, 1H, J = 5.2 Hz), 6.32 (d, 1H, J = 8.8 Hz), 6.74 (d, 1H, J = 8.4 Hz), 7.18 (d, 1H, J = 8.4 Hz).

化合物Ii-127

¹H-NMR (DMSO-d₆) δ: 0.94-1.12 (m, 2H), 1.14-1.39 (m, 5H), 1.34-1.56 (m, 1H), 1.70-1.97 (m, 4H), 2.87-3.10 (m, 5H), 6.17 (t, 1H, J = 5.2 Hz), 6.94-7.06 (m, 2H), 7.35-7.47 (m, 4H), 7.75-7.80 (m, 1H), 8.07 (d, 1H, J = 3.0 Hz).

化合物Ii-128

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.14-1.31 (m, 5H), 1.31-1.55 (m, 1H), 1.70-1.96 (m, 4H), 2.89-3.09 (m, 5H), 6.24 (t, 1H, J = 5.4 Hz), 6.94-7.05 (m, 2H), 7.24 (d, 1H, J = 6.9 Hz), 7.52 (t, 1H, J = 8.0 Hz), 7.75 (d, 1H, J = 8.8 Hz), 7.88-7.97 (m, 2H), 8.07 (d, 1H, J = 2.5 Hz).

化合物Ii-129

¹H-NMR (DMSO-d₆) δ: 0.98-1.12 (m, 2H), 1.18-1.30 (m, 2H), 1.19 (t, 3H, J = 6.8 Hz), 1.48 (m, 1H), 1.79-1.95 (m, 4H), 2.92-3.09 (m, 3H), 2.97 (q, 2H, J = 6.8 Hz), 6.27 (m, 1H), 7.01 (d, 1H, J = 8.0 Hz), 7.39-7.47 (m, 2H), 7.56 (m, 1H), 8.18-8.25 (m, 2H), 8.23 (s, 2H).

化合物Ii-130

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.15-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.45-1.64 (m, 1H), 1.78-1.96 (m, 4H), 2.97 (q, 2H, J = 7.2 Hz), 2.95-3.15 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 6.94-7.02 (m, 2H), 7.38 (t, 1H, J = 6.0 Hz), 7.46 (t, 2H, J = 7.5 Hz), 7.78 (d, 1H, J = 9.0 Hz), 7.96 (d, 2H, J = 9.0 Hz).

化合物Ii-131

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.15-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.48-1.62 (m, 1H), 1.78-1.96 (m, 4H), 2.98 (q, 2H, J = 7.2 Hz), 2.94-3.10 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.02 (d, 1H, J = 9.0 Hz), 7.10 (t, 1H, J = 5.4 Hz), 7.22 (td, 1H, J = 9.0, 3.0 Hz), 7.47-7.56 (m, 1H), 7.77-7.88 (m, 3H).

化合物Ii-132

¹H-NMR (DMSO-d₆) δ: 0.96-1.13 (m, 2H), 1.15-1.32 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.48-1.65 (m, 1H), 1.78-1.96 (m, 4H), 2.98 (q, 2H, J = 7.2 Hz), 2.94-3.12 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.01 (d, 1H, J = 6.0 Hz), 7.09 (t, 1H, J = 5.4 Hz), 7.27-7.35 (m, 2H), 7.42-7.50 (m, 1H), 7.57 (dd, 1H, J = 9.0, 3.0 Hz), 7.86 (td, 1H, J = 7.5, 3.0 Hz).

化合物Ii-133

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.58 (m, 1H), 1.72-1.94 (m, 4H), 2.95-3.20 (m, 4H), 4.89-4.98 (m, 2H), 6.65 (brs, 1H), 6.92 (d, 1H, J = 9.0 Hz), 6.91-6.98 (m, 1H), 7.03 (d, 1H, J = 9.0 Hz).

化合物Ii-134

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.58 (m, 1H), 1.72-1.94 (m, 4H), 2.92-3.20 (m, 4H), 6.74 (t, 1H, J = 6.0 Hz), 6.94 (t, 1H, J = 6.0 Hz), 6.97 (s, 1H), 7.08-7.24 (m, 5H).

化合物Ii-135

¹H-NMR (DMSO-d₆) δ: 0.95-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.48-1.60 (m, 1H), 1.76-1.94 (m, 4H), 2.92-3.10 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.18-3.30 (m, 2H), 6.89 (d, 1H, J = 9.6 Hz), 7.02 (brs, 1H), 7.11 (t, 1H, J = 5.4 Hz), 7.42-7.56 (m, 2H), 7.85 (d, 1H, J = 9.6 Hz), 7.93 (d, 1H, J = 7.5 Hz), 8.03 (s, 1H).

化合物Ii-136

¹H-NMR (DMSO-d₆) δ: 0.98-1.12 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.48-1.62 (m, 1H), 1.78-1.96 (m, 4H), 2.92-3.12 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.22-3.32 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.01 (d, 1H, J = 7.5 Hz), 7.20 (t, 1H, J = 6.0 Hz), 7.62 (s, 1H), 7.91 (d, 1H, J = 9.0 Hz), 8.02 (s, 2H).

化合物Ii-137

¹H-NMR (DMSO-d₆) δ: 0.95-1.12 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.65-1.95 (m, 5H), 2.93-3.12 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.25-3.40 (m, 2H), 5.07-5.16 (m, 2H), 7.01 (d, 1H, J = 7.5 Hz), 7.25 (t, 1H, J = 6.0 Hz), 7.92-8.03 (m, 3H), 8.33 (d, 1H, J = 6.0 Hz).

化合物Ii-138

¹H-NMR (DMSO-d₆) δ: 0.91-1.26 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.36-1.43 (m, 1H), 1.78-1.90 (m, 4H), 2.90-3.07 (m, 3H), 2.96 (q, 2H, J = 7.5 Hz), 5.69 (t, 1H, J = 5.7 Hz), 5.81 (d, 1H, J = 2.4 Hz), 7.00 (d, 1H, J = 7.8 Hz), 7.16-7.39 (m, 3H), 7.73-7.79 (m, 1H), 7.86-7.88 (m, 1H).

化合物Ii-139

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.20 (s, 3H), 1.22 (s, 3H), 1.40−1.52 (m, 1H), 1.81 (d, 2H, J = 12.4 Hz), 1.88 (d, 2H, J = 12.4 Hz), 2.90-2.98 (m, 2H), 2.99-3.13 (m, 2H), 5.68 (t, 1H, J = 5.6 Hz), 5.81 (s, 1H), 6.93 (d, 1H, J = 8.8 Hz), 7.16-7.40 (m, 3H), 7.76 (t, 1H, J = 8.0 Hz), 7.87 (s, 1H).

化合物Ii-140

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.26 (s, 9H), 1.40−1.49 (m, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.90-2.99 (m, 2H), 3.01-3.06 (m, 1H), 5.67 (t, 1H, J = 6.0 Hz), 5.81 (s, 1H), 6.74 (d, 1H, J = 8.4 Hz), 7.14-7.40 (m, 3H), 7.76 (t, 1H, J = 8.4 Hz), 7.87 (s, 1H).

化合物Ii-141

¹H-NMR (DMSO-d₆) δ: 0.97-1.06 (m, 2H), 1.18-1.27 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.45-1.59 (m, 1H), 1.76-1.81 (m, 2H), 1.87-1.91 (m, 2H), 2.97-3.09 (m, 1H), 3.10-3.13 (m, 1H), 3.17-3.22 (m, 2H), 6.94-7.02 (m, 2H), 6.98 (td, 1H, J = 7.8, 1.2 Hz), 7.36 (dd, 1H, J = 7.8, 0.6 Hz), 7.65 (dd, 1H, J = 7.8, 0.6 Hz), 8.00-8.05 (m, 1H).

化合物Ii-142

¹H-NMR (DMSO-d₆) δ: 0.96-1.04 (m, 2H), 1.18-1.28 (m, 2H), 1.20 (d, 6H, J = 6.9 Hz), 1.43-1.59 (m, 1H), 1.74-1.79 (m, 2H), 1.85-1.90 (m, 2H), 2.92-3.07 (m, 1H), 3.09-3.18 (m, 3H), 6.92-6.99 (m, 2H), 7.10 (td, 1H, J = 7.8, 1.2 Hz), 7.21 (dd, 1H, J = 7.8, 0.6 Hz), 7.31 (dd, 1H, J = 7.8, 0.6 Hz), 7.89-7.97 (m, 1H).

化合物Ii-143

¹H-NMR (DMSO-d₆)δ: 0.97-1.07 (m, 2H), 1.17-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.57 (m, 1H), 1.73-1.78 (m, 2H), 1.86-1.90 (m, 2H), 2.93-3.02 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.11 (t, 2H, J = 6.3 Hz), 6.91-7.02 (m, 2H), 7.19 (dd, 1H, J = 8.4, 4.8 Hz), 7.34 (dd, 1H, J = 9.3, 2.4 Hz), 8.00 (t, 1H, J = 6.0 Hz).

化合物Ii-144

¹H-NMR (DMSO-d₆)δ: 0.97-1.08 (m, 2H), 1.16-1.24 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.59 (m, 1H), 1.74-1.80 (m, 2H), 1.85-1.90 (m, 2H), 2.92-3.03 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 3.18 (t, 2H, J = 6.3 Hz), 6.99-7.07 (m, 2H), 7.33 (dd, 1H, J = 9.0, 4.8 Hz), 7.58 (dd, 1H, J = 8.7, 2.7 Hz), 8.00 (t, 1H, J = 5.4 Hz).

化合物Ii-145

¹H-NMR (DMSO-d₆) δ: 0.97-1.09 (m, 2H), 1.17-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.72-1.81 (m, 2H), 1.85-1.92 (m, 2H), 2.95-3.06 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 3.19 (t, 2H, J = 6.0 Hz), 7.01 (d, 1H, J = 8.1 Hz), 7.20-7.23 (m, 1H), 7.33 (dd, 1H, J = 8.7, 0.6 Hz), 7.58 (dd, 1H, J = 2.1, 0.9 Hz), 8.11-8.18 (m, 1H).

化合物Ii-146

¹H-NMR (DMSO-d₆) δ: 0.98-1.06 (m, 2H), 1.15-1.21 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.58 (m, 1H), 1.70-1.81 (m, 2H), 1.82-1.96 (m, 2H), 2.93-3.00 (m, 3H), 3.13-3.19 (m, 2H), 6.98-7.02 (m, 2H), 7.26-7.27 (m, 1H), 7.32-7.35 (m, 1H), 8.18-8.21 (m, 1H).

化合物Ii-147

¹H-NMR (DMSO-d₆) δ: 0.98-1.04 (m, 2H), 1.16-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.73-1.78 (m, 2H), 1.86-1.89 (m, 2H), 2.93-3.00 (m, 3H), 3.11-3.15 (m, 2H), 6.72-6.79 (m, 1H), 7.00-7.08 (m, 2H), 7.29-7.34 (m, 1H), 8.13-8.16 (m, 1H).

化合物Ii-148

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.15-1.26 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.45-1.58 (m, 1H), 1.72-1.80 (m, 2H), 1.84-1.92 (m, 2H), 2.96 (q, 2H, J = 7.2 Hz), 2.96-3.05 (m, 1H), 3.09-3.16 (m, 2H), 6.99 (d, 1H, J = 8.0 Hz), 7.13 (dd, 1H, J = 8.0, 2.0 Hz), 7.20 (d, 1H, J = 8.4 Hz), 7.49 (d, 1H, J = 2.0 Hz), 8.11 (t, 1H, J = 6.0 Hz).

化合物Ii-149

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.74-1.80 (m, 2H), 1.86-1.91 (m, 2H), 2.93-3.01 (m, 3H), 3.17-3.22 (m, 2H), 7.00-7.05 (m, 2H), 7.37-7.39 (m, 1H), 7.65-7.68 (m, 1H), 8.22-8.26 (m, 1H).

化合物Ii-150

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.29 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.44-1.60 (m, 1H), 1.74-1.80 (m, 2H), 1.86-1.91 (m, 2H), 2.95-3.17 (m, 2H), 3.21-3.27 (m, 2H), 6.95-6.98 (m, 1H), 8.10 (dd, 1H, J = 8.4, 2.7 Hz), 8.19 (dd, 1H, J = 3.0, 1.5 Hz), 8.44-8.47 (m, 1H).

化合物Ii-151

¹H-NMR (DMSO-d₆) δ: 0.99-1.04 (m, 2H), 1.15-1.23 (m, 2H), 1.21 (d, 6H, J = 6.3 Hz), 1.43-1.59 (m, 1H), 1.73-1.81 (m, 2H), 1.85-1.91 (m, 2H), 2.97-3.18 (m, 2H), 3.21-3.29 (m, 2H), 6.95-6.98 (m, 1H), 8.20-8.23 (m, 2H), 8.58-8.61 (m, 1H).

化合物Ii-152

¹H-NMR (DMSO-d₆) δ: 0.96-1.04 (m, 2H), 1.15-1.26 (m, 2H), 1.25 (s, 9H), 1.56-1.62 (m, 1H), 1.78-1.83 (m, 2H), 1.87-1.93 (m, 2H), 2.98-3.08 (m, 1H), 3.17 (t, 2H, J = 6.3 Hz), 3.48 (s, 3H), 6.47 (d, 2H, J = 8.7 Hz), 6.89-6.96 (m, 2H), 7.11-7.19 (m, 2H).

化合物Ii-153

¹H-NMR (DMSO-d₆) δ: 0.95-1.04 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.41 (m, 1H), 1.71-1.94 (m, 4H), 2.80-2.89 (m, 2H), 2.92-3.10 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz), 3.21-3.30 (m, 2H), 6.25-6.35 (m, 2H), 6.39 (dd, 1H, J = 8.4, 2.1 Hz), 7.01 (d, 1H, J = 7.5 Hz), 7.01 (dd, 1H, J = 8.4, 8.4 Hz).

化合物Ii-154

¹H-NMR (DMSO-d₆) δ: 0.91-1.09 (m, 2H), 1.16-1.28 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.42 (m, 1H), 1.74-1.95 (m, 4H), 2.80-3.16 (m, 9H), 2.97 (q, 2H, J = 7.5 Hz), 6.24-6.36 (m, 2H), 6.30 (dd, 1H, J = 8.4, 2.1 Hz), 7.10 (dd, 1H, J = 8.4, 2.1 Hz), 7.05 (d, 1H, J = 8.4 Hz).

化合物Ii-155

化合物Ii-156

化合物Ii-157

化合物Ii-158

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.10-1.30 (m, 5H), 1.41 (m, 1H), 1.76-1.94 (m, 4H), 2.74-2.83 (m, 2H), 2.83 (s, 3H), 2.90-3.08 (m, 3H), 2.96 (s, 3H), 5.68 (m, 1H), 6.39 (m, 1H), 6.58 (m, 1H), 6.95 (dd, 1H, J = 8.4, 8.4 Hz), 7.00 (d, 1H, J = 7.8 Hz).

化合物Ii-159

化合物Ii-160

化合物Ii-161

化合物Ii-162

化合物Ii-163

化合物Ii-164

化合物Ii-165

化合物Ii-166

化合物Ii-167

化合物Ii-168

化合物Ii-169

化合物Ii-170

化合物Ii-171

化合物Ii-172

化合物Ii-173

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz),1.43 (m, 1H), 1.76-1.85 (m, 2H), 1.85-1.93 (m, 2H), 2.76-2.82 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 2.97 (t, 2H, J = 7.2 Hz), 3.00 (m, 1H), 3.64-3.70 (m, 4H), 6.33 (m, 1H), 6.37 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 7.00 (d, 1H, J = 7.8 Hz), 7.28 (d, 1H, J = 8.4 Hz).

化合物Ii-174

化合物Ii-175

化合物Ii-176

化合物Ii-177

化合物Ii-178

化合物Ii-179

化合物Ii-180

化合物Ii-181

化合物Ii-182

化合物Ii-183

化合物Ii-184

化合物Ii-185

化合物Ii-186

化合物Ii-187

化合物Ii-188

化合物Ii-189

化合物Ii-190

化合物Ii-191

化合物Ii-192

化合物Ii-193

化合物Ii-194

化合物Ii-195

化合物Ii-196

化合物Ii-197

化合物Ii-198

化合物Ii-199

化合物Ii-200

化合物Ii-201

化合物Ii-202

化合物Ii-203

化合物Ii-204

化合物Ii-205

化合物Ii-206

Compound I-72

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2 H), 1.05-1.15 (m, 6H), 1.25 (s, 9H,), 1.15-1.32 (m, 3H), 1.41 (m, 1H), 1.75-1.98 ( m, 4H), 2.11 (m, 1H), 2.58-3.38 (m, 5H), 3.58-3.76 (m, 2H), 5.17 (m, 1H), 6.25-6.92 (m, 5H) Melting point: 147-149 ℃

Compound Ia-140

¹H-NMR (CDCl_Three) δ: 1.02-1.20 (m, 2 H), 1.17-1.32 (m, 2 H), 1.37 (d, 6H, J = 6.9 Hz), 1.46-1.70 (m, 4H), 1.86-1.95 (m, 2H), 2.08-2.18 (m, 2H), 3.01 (d, 2H, J = 6.9 Hz), 3.13 (m, 1H), 3.25 (m, 1H), 3.87 (d, 1H, J = 8.4 Hz), 6.61 (d, 2H, J = 8.7 Hz), 7.39 (d, 2H, J = 8.7 Hz)

Compound Ia-141

¹H-NMR (CDCl_Three) δ: 1.00-1.30 (m, 4 H), 1.37 (d, 6H, J = 6.9 Hz), 1.59 (m, 1H), 1.87-1.98 (m, 2H), 1.99-2.18 (m, 5H), 2.85 (q, 3H, J = 7.5 Hz), 2.97 (d, 2H, J = 6.9 Hz), 3.12 (m, 1H), 3.23 (m, 1H), 3.88 (d, 1H, J = 8.1 Hz), 6.53 (d, 1H, J = 7.8 Hz), 6.63 (brs, 1H), 7.04 (d, 1H, J = 7.8 Hz) Mass: 351 [M + H]

Compound Ia-178

¹H-NMR (CDCl_Three) δ: 1.08-1.36 (m, 4 H), 1.39 (s, 9H), 1.59 (m, 1H), 1.90-1.99 (m, 2H), 2.16-2.26 (m, 2H), 3.17-3.34 (m , 3H), 3.69 (d, 1H, J = 9.3 Hz), 6.68 (d, 1H, J = 9.3 Hz), 7.77 (dd, 1H, J = 2.1 Hz and 9.3 Hz), 8.49 (brs, 1H) Mass : 394 [M + H]⁺  

Compound Ib-138

¹H-NMR (CDCl_Three) δ: 1.02-1.34 (m, 4 H), 1.37 (d, 6H, J = 6.6 Hz), 1.57 (m, 1H), 1.87-1.97 (m, 2H), 2.07-2.18 (m, 2H), 2.93 (d, 2H, J = 6.6 Hz), 3.13 (m, 1H), 3.25 (m, 1H), 3.99 (d, 1H, J = 8.4 Hz), 6.38 (m, 1H), 6.49 (brs, 1H ), 6.97 (q, 1H, J = 9.3 Hz) Mass: 347 [M + H]

Compound Ii-2

¹H-NMR (DMSO-d₆) δ: 0.91-1.06 (m, 2H), 1.12-1.28 (m, 11H), 1.31-1.47 (m, 1H), 1.75-1.94 (m, 4H), 2.19 (t, 2H, J = 11.3 Hz) , 2.79 (t, 2H, J = 6.0 Hz), 2.93-3.08 (m, 1H), 2.97 (q, 2H, J = 7.42 Hz), 3.46 (m, 2H), 3.57-3.69 (m, 2H), 5.71 (t, 1H, J = 5.2 Hz), 5.77 (d, 1H, J = 11.5 Hz), 5.88-5.96 (m, 2H), 7.01 (d, 1H, J = 7.4 Hz).

Compound Ii-3

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2 H), 1.15-1.21 (m, 1H), 1.27 (s, 9H), 1.40-1.49 (m, 2H), 1.82 (d, 2H, J = 11.6 Hz), 1.92 (d, 2H, J = 11.6 Hz), 2.79-2.84 (m, 2H), 2.97-3.10 (m, 1H), 3.24 (s, 3H), 3.55-3.62 (m, 2H), 3.84-3.91 ( m, 2H), 5.50-5.59 (m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.4 Hz), 6.97 (d, 1H , J = 8.4 Hz). Melting point: 166-168 ° C

Compound Ii-4

¹H-NMR (DMSO-d₆) δ: 0.87 (t, 3H, J = 7.2 Hz), 0.93-1.06 (m, 2H), 1.13-1.21 (m, 1H), 1.26 (s, 9H), 1.37-1.49 (m, 2H), 1.61 -1.72 (m, 2H), 1.82 (d, 2H, J = 12.0 Hz), 1.91 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.97-3.08 (m, 1H), 3.61-3.71 (m, 2H), 5.52-5.60 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.73 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 8.8 Hz). Melting point: 185-186 ° C

Compound Ii-5

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2H), 1.26 (s, 9H), 1.28-1.31 (m, 1H), 1.35-1.47 (m, 8H), 1.81 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.77-2.84 (m, 2H), 2.96-3.07 (m, 1H), 4.30-4.42 (m, 1H), 5.51-5.64 (m, 1H), 6.39 (d , 1H, J = 8.0 Hz), 6.55 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz), 7.07 (d, 1H, J = 8.8 Hz). Melting point: 156-157 ° C

Compound Ii-6

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.19-1.25 (m, 4H), 1.26 (s, 9H), 1.38-1.49 (m, 2H), 1.82 (d, 2H, J = 8.8 Hz), 1.91 (d, 2H, J = 8.8 Hz), 2.79-2.84 (m, 2H), 2.97-3.07 (m, 1H), 3.69-3.80 (m, 2H), 5.51-5.63 (m, 1H), 6.41 (d , 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 8.8 Hz). Melting point: 178-179 ° C

Compound Ii-7

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.19-1.22 (m, 1H), 1.26 (s, 9H), 1.38-1.48 (m, 2H), 1.82 (d, 2H, J = 11.6 Hz), 1.91 (d, 2H, J = 11.6 Hz), 2.79-2.84 (m, 2H), 2.95-3.09 (m, 1H), 3.25 (s, 3H), 5.52-5.60 (m, 1H), 6.41 (d, 1H , J = 8.4 Hz), 6.56 (s, 1H), 6.72 (d, 1H, J = 8.4 Hz), 6.92 (d, 1H, J = 8.4 Hz). Melting point: 206-207 ° C

Compound Ii-8

¹H-NMR (DMSO-d₆) δ: 0.91-1.05 (m, 2H), 1.16-1.24 (m, 1H), 1.26 (s, 9H), 1.37-1.47 (m, 2H), 1.81 (d, 2H, J = 12.8 Hz), 1.90 (d, 2H, J = 12.8 Hz), 2.75-2.81 (m, 2H), 2.96-3.08 (m, 1H), 5.45-5.52 (m, 1H), 6.33 (d, 1H, J = 8.4 Hz), 6.50 (s, 1H), 6.68-6.80 (m, 2H), 11.02 (brs, 1H). Melting point: 213-214 ° C

Compound Ii-9

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2 H), 1.17-1.30 (m, 8H), 1.44 (brs, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.89 (d, 2H, J = 12.4 Hz), 2.78-2.82 (m, 2H), 2.97-3.15 (m, 2H), 3.23 (s, 3H), 3.55-3.62 (m, 2H), 3.83-3.90 (m, 2H), 5.52-5.59 ( m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.55 (s, 1H), 6.92 (d, 1H, J = 8.0 Hz), 6.97 (d, 1H, J = 8.4 Hz). Melting points: 120-121 ℃

Compound Ii-10

¹H-NMR (DMSO-d₆) δ: 0.88 (t, 3H, J = 7.2 Hz), 0.93-1.08 (m, 2H), 1.17-1.30 (m, 8H), 1.44 (brs, 1H), 1.52-1.61 (m, 2H), 1.83 (d, 2H, J = 12.0 Hz), 1.90 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.98-3.15 (m, 2H), 3.62-3.71 (m, 2H), 5.52-5.60 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.57 (s, 1H), 6.92 (d, 1H, J = 8.0 Hz), 6.97 (d, 1H, J = 8.4 Hz) ). Melting point: 144-145 ℃

Compound Ii-11

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.15-1.30 (m, 8H), 1.33-1.50 (m, 7H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.86 (m, 2H), 2.96-3.14 (m, 2H), 4.30-4.45 (m, 1H), 5.50-5.61 (m, 1H), 6.40 (d, 1H, J = 7.6 Hz ), 6.55 (s, 1H), 6.92 (d, 1H, J = 7.2 Hz), 7.07 (d, 1H, J = 7.6 Hz). Melting point: 137-138 ° C

Compound Ii-12

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.14-1.30 (m, 11H), 1.36-1.50 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.85 (m, 2H), 2.97-3.15 (m, 2H), 3.69-3.79 (m, 2H), 5.52-5.60 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz ), 6.56 (s, 1H), 6.92 (d, 1H, J = 7.2 Hz), 6.98 (d, 1H, J = 8.4 Hz). Melting point: 158-159 ° C

Compound Ii-13

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.12-1.30 (m, 8H), 1.34-1.51 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.77-2.83 (m, 2H), 2.95-3.12 (m, 2H), 3.25 (s, 3H), 5.51-5.59 (m, 1H), 6.41 (d, 1H, J = 8.8 Hz), 6.56 (s, 1H), 6.86-6.97 (m, 2H). Melting point: 157-158 ° C

Compound Ii-14

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2 H), 1.12-1.30 (m, 5H), 1.38-1.50 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.77-2.85 (m, 2H), 2.90-3.09 (m, 3H), 3.23 (s, 3H), 3.55-3.61 (m, 2H), 3.84-3.91 (m, 2H), 5.52- 5.60 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.55 (s, 1H), 6.89-7.00 (m, 2H). Melting point: 150-151 ° C

Compound Ii-15

¹H-NMR (DMSO-d₆) δ: 0.88 (s, 3H), 0.90 (s, 3H), 0.92-1.08 (m, 2H), 1.12-1.30 (m, 5H), 1.35-1.51 (m, 1H), 1.83 (d, 2H, J = 12.4 Hz), 1.89 (d, 2H, J = 12.4 Hz), 2.00-2.16 (m, 1H), 2.77-2.84 (m, 2H), 2.90-3.10 (m, 3H), 3.42-3.55 (m , 2H), 5.50-5.65 (m, 1H), 6.40 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 6.88-7.01 (m, 2H) Melting point: 132-133 ° C

Compound Ii-16

¹H-NMR (DMSO-d₆) δ: 0.87 (t, 3H, J = 6.8 Hz), 0.90-1.08 (m, 2H), 1.10-1.28 (m, 5H), 1.35-1.50 (m, 1H), 1.59-1.72 (m, 2H) , 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.77-2.85 (m, 2H), 2.90-3.09 (m, 3H), 3.61-3.71 (m, 2H ), 5.52-5.61 (m, 1H), 6.40 (d, 1H, J = 8.0 Hz), 6.56 (s, 1H), 6.97 (d, 2H, J = 8.0 Hz). Melting point: 136-137 ° C

Compound Ii-17

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.12-1.28 (m, 5H), 1.33-1.50 (m, 7H), 1.81 (d, 2H, J = 12.0 Hz), 1.88 (d, 2H, J = 12.0 Hz), 2.78-2.84 (m, 2H), 2.90-3.08 (m, 3H), 4.28-4.44 (m, 1H), 5.49-5.79 (m, 1H), 6.39 (d, 1H, J = 8.0 Hz ), 6.55 (s, 1H), 6.97 (d, 1H, J = 7.6 Hz), 7.07 (d, 1H, J = 8.0 Hz). Melting point: 124-125 ° C

Compound Ii-18

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.12-1.29 (m, 8H), 1.36-1.51 (m, 1H), 1.82 (d, 2H, J = 12.0 Hz), 1.89 (d, 2H, J = 12.0 Hz), 2.78-2.86 (m, 2H), 2.90-3.09 (m, 3H), 3.68-3.80 (m, 2H), 5.51-5.61 (m, 1H), 6.41 (d, 1H, J = 8.4 Hz ), 6.57 (s, 1H), 6.97 (d, 2H, J = 8.4 Hz). Melting point: 163-164 ° C

Compound Ii-19

¹H-NMR (DMSO-d₆) δ: 0.89-1.08 (m, 2H), 1.11-1.30 (m, 5H), 1.35-1.51 (m, 1H), 1.82 (d, 2H, J = 10.8 Hz), 1.89 (d, 2H, J = 10.8 Hz), 2.75-2.88 (m, 2H), 2.89-3.10 (m, 3H), 3.25 (s, 3H), 5.48-5.60 (m, 1H), 6.42 (d, 1H, J = 7.6 Hz), 6.56 (s, 1H), 6.92 (d, 1H, J = 7.6 Hz), 6.98 (d, 1H, J = 5.6 Hz). Melting point: 189-190 ° C

Compound Ii-20

¹H-NMR (DMSO-d₆) δ: 0.95-1.13 (m, 2H), 1.31-1.59 (m, 10H), 1.73-1.92 (m, 4H), 2.12-2.26 (m, 2H), 2.84 (d, 2H, J = 6.0 Hz) , 3.07-3.30 (m, 4H), 4.30-4.46 (m, 1H), 5.64 (brs, 1H), 6.41 (d, 1H, J = 8.4 Hz), 6.57 (s, 1H), 7.08 (d, 1H , J = 8.4 Hz). Melting point: 165-166 ° C

Compound Ii-21

¹H-NMR (DMSO-d₆) δ: 0.86-1.25 (m, 10H), 1.40 (d, 3H, J = 6.9Hz), 1.52 (m, 1H), 1.82-1.93 (m, 4H), 2.95-3.00 (m, 5H), 3.63 -3.91 (m, 2H), 4.61-4.68 (m, 1H), 6.73 (brs, 2H), 7.01 (d, 2H, J = 7.8Hz), 7.11 (d, 1H, J = 8.1Hz,).

Compound Ii-22

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2 H), 1.15-1.34 (m, 5H), 1.36-1.43 (m, 9H), 1.53 (m, 1H), 1.82.1-93 (m, 4H), 2.94 -3.01 (m, 6H), 4.52 (m, 1H), 4.63 (m, 1H), 6.73 (brs, 2H), 7.02 (d, 1H, J = 7.5Hz), 7.21-7.25 (m, 1H).

Compound Ii-23

¹H-NMR (DMSO-d₆) δ: 0.86-1.04 (m, 4 H), 1.25 (s, 10H), 1.30 (s, 6H), 1.38 (s, 3H), 1.40 (s, 3H), 178-1.92 (m 4H), 2.76 -2.80 (m, 2H), 3.03 (m, 1H), 4.54-4.63 (m, 1H), 5.57 (m, 1H), 6.16 (s, 1H), 6.22 (d, 1H, J = 8.4Hz), 6.76 (d, 1H, J = 8.4Hz), 6.98 (d, 1H, J = 8.4Hz).

Compound Ii-24

¹H-NMR (DMSO-d₆) δ: 0.98-1.11 (m, 5 H), 1.15-1.31 (m, 20H), 1.57 (m, 1H), 1.82.1-93 (m, 4H), 2.74-2.81 (m, 1H), 3.01 -3.06 (m, 2H), 3.35 (m, 1H), 3.40 (m, 1H), 4.04-4.17 (m, 3H), 6.77 (d, 1H, J = 9.0Hz),

Compound Ii-25

¹H-NMR (DMSO-d₆) δ: 0.98-1.20 (m, 13 H), 1.30 (d, 3H, J = 3H), 1.59 (m, 1H), 1.81-1.91 (m, 4H), 2.73-2.83 (m, 1H), 2.94 -3.04 (m, 4H), 3.35-3.45 (m, 2H), 4.08-4.19 (m, 3H), 6.88 (brs, 3H), 7.03 (d, 1H, J = 8.4Hz).

Compound Ii-26

¹H-NMR (DMSO-d₆) δ: 1.02-1.10 (m, 2H), 1.19-1.32 (m, 2H), 1.26 (s, 9H), 1.55 (m, 1H), 1.86-1.93 (m, 4H), 3.01-3.04 (m, 3H), 6.76 (d, 1H, J = 8.7 Hz), 7.03 (m, 1H), 7.37-7.43 (m, 3H), 7.76-7.80 (m, 1H), 8.20-8.23 (m, 1H), 8.34 -8.40 (m, 1H), 8.78-8.79 (m, 1H)

Compound Ii-27

¹H-NMR (DMSO-d₆) δ: 1.03-1.10 (m, 2H), 1.20-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.53 (m, 1H), 1.88 (m, 4H), 2.99-3.15 (m, 3H), 7.33-7.35 (m, 3H), 7.71-7.75 (m, 1H), 8.16-8.18 (m, 1H), 829-8.32 (m, 1H), 8.76-8.78 (m, 1H)

Compound Ii-28

¹H-NMR (DMSO-d₆) δ: 1.04-1.11 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.59 (m, 1H), 1.87-1.91 (m, 4H), 2.93 -3.08 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.06-3.08 (m, 2H), 7.01 (m, 1H), 7.17 (d, 1H, J = 7.5 Hz), 7.43 ( d, 1H, J = 7.5Hz), 7.50-7.57 (m, 2H), 7.80-7.84 (m, 1H), 8.25-8.27 (m, 1H), 8.39-8.44 (m, 1H), 8.80-8.82 ( m, 1H)

Compound Ii-29

¹H-NMR (DMSO-d₆) δ: 0.99-1.10 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.52 (m, 1H), 1.84-1.91 (m, 4H), 2.94 -3.01 (m, 5H), 6.88 (m, 1H), 7.00 (d, 1H, J = 7.8 Hz), 7.26-7.28 (m, 2H), 7.38 (m, 1H), 7.76 (d, 1H, J = 3.3.Hz), 7.90 (d, 1H, J = 3.3 Hz)

Compound Ii-30

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2 H), 1.18-1.33 (m, 2H), 1.26 (s, 9H), 1.45 (m, 1H), 1.78-1.97 (m, 4 H), 2.86-2.94 ( m, 2H), 2.95-3.10 (m, 1H), 5.91 (m, 1H), 6.55 (d, 1H, J = 7.6 Hz), 6.63-6.71 (m, 2H), 6.73 (d, 1H, J = 8.0 Hz), 7.06 (s, 1H), 7.15 (t, 1H, J = 8.0 Hz), 7.60 (s, 1H), 8.11 (s, 1H), 8.31 (s, 1H)

Compound Ii-31

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2 H), 1.13-1.28 (m, 2H), 1.26 (s, 9H), 1.43 (m, 1H), 1.76-1.97 (m, 4 H), 2.83-3.18 ( m, 3H), 5.79 (m, 1H), 6.21 (s, 2H), 6.44 (d, 1H, J = 6.8 Hz), 6.58-6.67 (m, 2H), 6.73 (d, 1H, J = 8.0 Hz ), 7.10 (t, 1H, J = 8.0 Hz), 7.21 (s, 2H) Melting point: 205-206 ° C

Compound Ii-32

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 2 H), 1.05-1.28 (m, 11H), 1.41 (m, 1H), 1.75-1.92 (m, 4 H), 2.11 (t, 2H, J = 10.0 Hz) , 2.73-2.82 (m, 2H), 2.91-3.08 (m, 3H), 3.24 (d, 2H, J = 11.2 Hz), 3.62-3.72 (m, 2H), 5.07 (m, 1H), 6.47 (d , 2H, J = 7.2 Hz), 6.72 (d, 2H, J = 7.2 Hz), 6.97 (d, 1H, J = 7.6 Hz) Melting point: 165-166 ° C

Compound Ii-33

¹H-NMR (DMSO-d₆) δ: 0.91-1.06 (m, 2H), 1.15-1.26 (m, 8H), 1.33-1.48 (m, 1H), 1.71-1.93 (m, 4H), 2.88 (d, 2H, J = 6.5 Hz) , 2.93-3.15 (m, 2H), 5.70 (brs, 2H), 6.63 (d, 2H, J = 9.1 Hz), 6.93-6.96 (m, 1H), 7.38-7.42 (m, 2H), 7.57 (d , 2H, J = 9.1 Hz), 7.88-7.93 (m, 2H)

Compound Ii-34

¹H-NMR (DMSO-d₆) δ: 0.98-1.02 (m, 2H), 1.16-1.18 (m, 5H), 1.42 (s, 1H), 1.75-1.91 (m, 4H), 2.88 (d, 2H, J = 6.6 Hz), 2.96 (q, 3H, J = 7.3 Hz), 6.63 (d, 2H, J = 8.9 Hz), 6.99-7.02 (m, 1H), 7.38-7.41 (m, 2H), 7.57 (d, 2H, J = 8.9 Hz), 7.89-7.92 (m, 2H).

Compound Ii-35

¹H-NMR (DMSO-d₆) δ: 0.90-1.52 (m, 5H), 1.19 (t, 3H, J = 7.2 Hz), 1.75-1.96 (m, 4H), 2.50-3.10 (m, 3H), 2.62 (q, 2H, J = 7.2 Hz), 5.55-5.70 (m, 1H), 6.57 (d, 2H, J = 8.7 Hz), 6.80-7.04 (m, 4H), 7.01 (d, 1H, J = 7.8 Hz), 7.34 (d, (2H, J = 8.7 Hz)

Compound Ii-36

¹H-NMR (DMSO-d₆) δ: 0.90-1.50 (m, 5H), 1.19 (t, 3H, J = 7.2 Hz), 1.75-1.95 (m, 4H), 2.70-3.10 (m, 3H), 2.97 (q, 2H, J = 7.2 Hz), 3.70 (s, 3H), 5.40-5.50 (m, 1H), 6.53 (d, 2H, J = 8.7 Hz), 6.74 (d, 2H, J = 8.7 Hz), 6.78-6.90 (m, 4H), 6.99 (d, 1H, J = 7.8 Hz)

Compound Ii-37

¹H-NMR (CDCl_Three) δ: 1.02-1.32 (m, 4 H), 139 (s, 9H,), 1.58 (m, 1H), 1.86-1.96 (m, 2H), 2.12-2.22 (m, 2H), 3.02 (d, 2H, J = 6.6 Hz), 3.25 (m, 1H), 3.67 (d, 1H, J = 9.3 Hz), 6.67 (d, 2H, J = 8.7 Hz), 7.41 (d, 2H, J = 8.7 Hz) Mass: 393 [M + H]

Compound Ii-38

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.17-1.26 (m, 2H), 1.19 (t, 3H, J = 7.1 Hz), 1.43 (s, 1H), 1.77-1.85 (m, 2H), 1.85 -1.94 (m, 2H), 2.82 (t, 1H, J = 5.8 Hz), 2.98 (m, 1H), 2.97 (q, 2H, J = 7.1 Hz), 5.87 (m, 1H), 6.56 (d, 2H, J = 8.6 Hz), 6.98 (d, 1H, J = 7.6 Hz), 7.02 (d, 2H, J = 8.6 Hz).

Compound Ii-39

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.19-1.35 (m, 2H), 1.29 (s, 9H), 1.46 (s, 1H), 1.73-1.98 (m, 4H), 2.93 (m, 1H) , 3.04 (m, 1H), 6.60-6.69 (m, 2H), 6.75 (d, 1H, J = 8.8 Hz), 6.97 (d, 1H, J = 7.6 Hz), 7.49 (d, 1H, J = 8.8 Hz), 8.05 (s, 1H).

Compound Ii-40

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.16-1.29 (m, 2H), 1.19 (t, 3H, J = 7.3 Hz), 1.45 (s, 1H), 1.76-1.94 (m, 4H), 1.76 (s, 2H), 2.93 (t, 2H, J = 5.8 Hz), 2.97 (q, 2H, J = 7.3 Hz), 6.66 (s, 1H), 6.94-7.01 (m, 2H), 7.49 (d, 1H, J = 8.6 Hz), 8.04 (s, 1H).

Compound Ii-41

¹H-NMR (DMSO-d₆) δ: 0.91-1.05 (m, 2H), 1.17-1.33 (m, 2H), 1.26 (s, 9H), 1.35-1.48 (m, 1H), 1.76-1.86 (m, 2H), 1.86-1.95 ( m, 2H), 2.76-2.82 (m, 1H), 2.96-3.08 (m, 1H), 3.71 (s, 3H), 5.21-5.30 (m, 1H), 6.57 (d, 1H, J = 8.6 Hz) , 6.73 (d, 1H, J = 8.6 Hz), 7.02 (dd, 1H, J = 8.6, 2.3 Hz), 7.44 (d, 1H, J = 2.3 Hz).

Compound Ii-42

¹H-NMR (DMSO-d₆) δ: 0.98-1.01 (m, 2H), 1.18-1.28 (m, 2H), 1.19 (t, 3H, J = 7.1 Hz), 1.42 (s, 1H), 1.76-1.85 (m, 2H), 1.85 -1.93 (m, 2H), 2.79 (t, 2H, J = 5.9 Hz), 2.97 (q, 2H, J = 7.1 Hz), 3.02 (m, 1H), 3.71 (s, 3H), 5.26 (m, 1H), 6.58 (d, 1H, J = 8.6 Hz), 6.98 (d, 2H, J = 7.8 Hz), 7.02 (d, 2H, J = 8.6 Hz), 7.44 (br s, 1H).

Compound Ii-43

¹H-NMR (DMSO-d₆) δ: 0.98-1.06 (m, 2H), 1.16-1.25 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.51 (m, 1H), 1.83-1.91 (m, 4H), 2.85 (t, 2H, J = 6.3 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.04 (m, 1H), 3.56 (s, 3H), 5.46 (t, 1H, J = 6.3 Hz), 5.76 (s, 1H), 6.49 (d, 1H, J = 7.8 Hz), 7.21 (t, 1H, J = 7.5 Hz), 7.32 (t, 2H, J = 7.5 Hz), 7.68 (d, 2H, J = 7.5 Hz)

Compound Ii-44

¹H-NMR (DMSO-d₆) δ: 0.96-1.05 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.24 (m, 2H), 1.48 (m, 1H), 1.76-1.91 (m, 4H), 2.91 (d , 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.2 Hz), 6.35 (s, 1H), 6.99 (d, 1H, J = 7.8 Hz), 7.46-7.49 (m, 3H), 7.73 -7.76 (m, 2H)

Compound Ii-45

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.15-1.22 (m, 1H), 1.26 (s, 9H), 1.37-1.51 (m, 2H), 1.81 (d, 2H, J = 11.6 Hz), 1.91 (d, 2H, J = 11.6 Hz), 2.76-2.86 (m, 2H), 2.97-3.08 (m, 1H), 3.35 (s, 3H), 5.82-5.91 (m, 1H), 6.26 (d, 1H , J = 13.6 Hz), 6.39 (s, 1H), 6.73 (brs, 1H). Melting point: 215-216 ° C

Compound Ii-46

¹H-NMR (CDCl_Three) δ: 1.02-1.32 (m, 4H), 1.24 (d, 6H, J = 6.0 Hz), 1.39 (s, 9H), 1.54 (m, 1H), 1.84-1.94 (m, 2H), 2.12-2.22 (m, 2H), 2.39 (t, 2H, J = 10.5 Hz), 2.94 (d, 2H, J = 6.9 Hz), 3.24 (m, 1H), 3.38 (d, 1H, J = 9.6 Hz), 3.61 (d, 1H, J = 9.6 Hz), 3.72-4.00 (m, 2H), 5.83-5.94 (m, 1H), 5.96-6.10 (m, 2H).

Compound Ii-47

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.16-1.34 (m, 11H), 1.40 (m, 1H), 1.79 (d, 2H, J = 12.5 Hz), 1.90 (d, 2H, J = 11.9 Hz) ), 2.82 (t, 2H, J = 5.5 Hz), 3.01 (m, 1H), 6.12-6.18 (m, 3H), 6.30 (t, 1H, J = 5.5 Hz), 6.76 (d, 1H, J = 8.7 Hz).

Compound Ii-48

¹H-NMR (CDCl_Three) δ: 1.00-1.28 (m, 4H), 1.39 (s, 9H), 1.56 (m, 1H), 1.91 (d, 2H, J = 12.4 Hz), 2.08-2.21 (m, 4H), 2.58 (t , 2H, J = 8.1 Hz), 2.97 (d, 2H, J = 6.0 Hz), 3.23 (m, 1H), 3.70 (d, 1H, J = 9.4 Hz), 3.80 (t, 2H, J = 7.1 Hz ), 6.66 (d, 2H, J = 8.7 Hz), 7.36 (d, 2H, J = 8.7 Hz).

Compound Ii-49

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.17-1.33 (m, 11H), 1.41 (m, 1H), 1.80 (d, 2H, J = 12.9 Hz), 1.90 (d, 2H, J = 11.4 Hz) ), 2.82 (t, 2H, J = 6.1 Hz), 3.01 (m, 1H), 6.07 (t, 1H, J = 5.3 Hz), 6.34-6.43 (m, 2H), 6.51 (dd, 1H, J1 = 8.2 Hz, J2 = 1.8 Hz), 6.75 (d, 1H, J = 8.5 Hz), 7.11 (t, 1H, 8.2 Hz).

Compound Ii-50

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.14-1.31 (m, 8H), 1.43 (m, 1H), 1.76-1.94 (m, 4H), 2.82 (t, 2H, J = 6.0 Hz), 2.95 -3.16 (m, 2H), 5.90 (t, 1H, J = 5.5 Hz), 6.56 (d, 2H, J = 8.7 Hz), 6.95 (d, 1H, J = 7.9 Hz), 7.03 (d, 2H, J = 8.6 Hz).

Compound Ii-51

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.13-1.31 (m, 8H), 1.42 (m, 1H), 1.76-1.94 (m, 4H), 2.83 (t, 2H, J = 6.0 Hz), 2.95 -3.16 (m, 2H), 6.07 (t, 1H, J = 5.4 Hz), 6.36-6.46 (m, 2H), 6.53 (dd, 1H, J1 = 8.1 Hz, J2 = 1.9 Hz), 6.95 (d, 1H, J = 7.9 Hz), 7.12 (d, 1H, J = 8.1 Hz).

Compound Ii-52

¹H-NMR (DMSO-d₆) δ: 0.91-1.10 (m, 2H), 1.19-1.37 (m, 11H), 1.45 (m, 1H), 1.78-1.90 (m, 4H), 2.84 (t, 2H, J = 6.0 Hz), 3.04 (m, 1H), 4.64 (q, 2H, J = 9.0 Hz), 5.73 (t, 1H, J = 5.4 Hz), 6.13-6.21 (m, 2H), 6.26 (d, 1H, J = 7.2 Hz) , 6.78 (d, 1H, J = 8.4 Hz), 6.99 (t, 1H, 8.0 Hz).

Compound Ii-53

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.13-1.30 (m, 8H), 1.42 (m, 1H), 1.75-1.93 (m, 4H), 2.80 (t, 2H, J = 6.2 Hz), 2.93 -3.16 (m, 2H), 5.66 (t, 1H, J = 5.5 Hz), 6.53 (d, 2H, J = 9.1 Hz), 6.89 (d, 2H, J = 8.8 Hz), 6.92 (t, 1H, J_HF = 75 Hz), 6.94 (d, 1H, J = 8.0 Hz).

Compound Ii-54

¹H-NMR (DMSO-d₆) δ: 0.88-1.05 (m, 2H), 1.14-1.32 (m, 11H), 1.41 (m, 1H), 1.75-1.94 (m, 4H), 2.77 (t, 2H, J = 6.0 Hz), 3.01 (m, 1H), 4.54 (q, 2H, J = 9.0 Hz), 5.33 (t, 1H, J = 5.8 Hz), 6.49 (d, 2H, J = 8.8 Hz), 6.75 (d, 1H, J = 8.8 Hz), 6.80 (d, 2H, J = 8.8 Hz).

Compound Ii-55

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.14-1.31 (m, 8H), 1.40 (m, 1H), 1.74-1.93 (m, 4H), 2.79 (t, 2H, J = 5.9 Hz), 2.94 -3.15 (m, 6H), 3.69 (t, 4H, J = 4.8 Hz), 5.70-5.94 (m, 4H), 6.94 (d, 1H, J = 8.0 Hz).

Compound Ii-56

¹H-NMR (DMSO-d₆) δ: 0.98-1.14 (m, 2H), 1.15-1.32 (m, 5H), 1.54 (m, 1H), 1.83-1.96 (m, 4H), 2.89-3.10 (m, 5H), 6.17 (t, 1H, J = 5.2 Hz), 6.63 (d, 1H, J = 2.2 Hz), 7.02 (d, 1H, J = 7.7 Hz), 7.21 (dd, 1H, J1 = 9.1 Hz, J2 = 2.5 Hz), 7.27 (dd, 1H, J1 = 8.2 Hz, J2 = 4.4 Hz), 7.67 (d, 1H, J = 9.1 Hz), 7.97 (d, 1H, J = 8.2 Hz), 8.45 (dd, 1H, J1 = 4.3 Hz , J2 = 1.5 Hz).

Compound Ii-57

¹H-NMR (DMSO-d₆) δ: 0.97-1.14 (m, 2H), 1.17-1.34 (m, 8H), 1.54 (m, 1H), 1.83-1.96 (m, 4H), 2.94 (t, 2H, J = 6.0 Hz), 2.99 -3.18 (m, 2H), 6.17 (t, 1H, J = 5.4 Hz), 6.63 (d, 1H, J = 2.5 Hz), 6.96 (d, 1H, J = 7.7 Hz), 7.21 (dd, 1H, J1 = 9.1 Hz, J2 = 2.5 Hz), 7.27 (dd, 1H, J1 = 8.2 Hz, J2 = 4.1 Hz), 7.67 (d, 1H, J = 9.1 Hz), 7.97 (d, 1H, J = 8.0 Hz ), 8.45 (dd, 1H, J1 = 4.3 Hz, J2 = 1.5 Hz).

Compound Ii-58

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.12-1.29 (m, 5H), 1.40 (m, 1H), 1.74-1.93 (m, 4H), 2.80 (t, 2H, J = 5.9 Hz), 2.92 -3.07 (m, 7H), 3.69 (t, 4H, J = 4.8 Hz), 5.69-5.95 (m, 4H), 6.99 (d, 1H, J = 7.7 Hz).

Compound Ii-59

¹H-NMR (DMSO-d₆) δ: 0.94-1.11 (m, 2H), 1.14-1.30 (m, 5H), 1.47 (m, 1H), 1.78-1.95 (m, 4H), 2.88-3.09 (m, 5H), 3.80 (s, 3H), 6.09 (t, 1H, J = 5.6 Hz), 6.81-6.86 (m, 1H), 6.96 (dd, 1H, J1 = 8.8 Hz, J2 = 2.8 Hz), 7.01 (d, 1H, J = 7.4 Hz), 7.29 (t, 1H, J = 8.0 Hz), 7.45-7.51 (m, 2H), 7.66 (d, 1H, J = 8.5 Hz), 8.04 (d, 1H, J = 2.8 Hz).

Compound Ii-60

¹H-NMR (DMSO-d₆) δ: 1.03 (m, 2H), 1.19 (t, 2H, J = 7.8 Hz), 1.21 (m, 2H), 1.46 (m, 1H), 1.76-1.95 (m, 4H), 2.90 (t, 2H , J = 5.8 Hz), 2.97 (q, 2H, J = 7.3 Hz), 3.03 (m, 1H), 3.80 (s, 3H), 5.95 (m, 1H), 6.90 (m, 1H), 6.98 (d , 1H, J = 7.8 Hz), 6.98 (dd, 1H, J = 7.8, 7.8 Hz), 7.06 (d, 1H, J = 8.6 Hz), 7.26 (dd, 1H, J = 7.8, 7.8 Hz), 7.61 (d, 1H, J = 8.6 Hz), 7.69 (d, 1H, J = 7.8 Hz), 8.03 (s, 1H).

Compound Ii-61

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.18-1.29 (m, 2H), 1.19 (t, 3H, J = 7.6 Hz), 1.47 (m, 1H), 1.87 (m, 5H), 2.90 (t , 2H, J = 6.3 Hz), 2.97 (q, 2H, J = 7.6 Hz), 3.02 (m, 1H), 5.98 (m, 1H), 6.63 (d, 2H, J = 8.3 Hz), 6.98 (d , 1H, J = 7.3 Hz), 7.14 (m, 1H), 7.73 (s, 2H), 7.83 (d, 2H, J = 8.3 Hz), 8.52 (d, 1H, J = 4.0 Hz).

Compound Ii-62

¹H-NMR (DMSO-d₆) δ: 0.98-1.01 (m, 2H), 1.20 (s, 9H), 1.20-1.37 (m, 2H), 1.42 (m, 1H), 1.76-1.96 (m, 4H), 2.28-2.37 (m, 2H), 2.75-2.85 (m, 2H), 3.02 (m, 1H), 3.36 (t, 2H, J = 7.8 Hz), 3.57 (t, 2H, J = 6.3 Hz), 5.66 (m, 1H), 6.54 (d, 2H, J = 8.0 Hz), 6.73 (d, 1H, J = 8.6 Hz), 7.00 (d, 1H, J = 8.0 Hz).

Compound Ii-63

¹H-NMR (DMSO-d₆) δ: 0.96-1.14 (m, 2H), 1.14-1.32 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.50 (m, 1H), 1.76-1.96 (m, 4H), 2.91 -3.10 (m, 3H), 2.97 (q, 2H, J = 7.2 Hz), 6.28 (m, 1H), 7.02 (d, 1H, J = 7.8 Hz), 7.32-7.46 (m, 3H), 8.20 ( d, 1H, J = 6.9 Hz), 8.22 (s, 2H).

Compound Ii-64

¹H-NMR (DMSO-d₆) δ: 1.03-1.15 (m, 2H), 1.18-1.29 (m, 2H), 1.24 (d, 6H, J = 6.3 Hz), 1.52 (m, 1H), 1.86-1.94 (m, 2H), 2.10 -2.19 (m, 2H), 2.40 (t, 2H, J = 6.0 Hz), 2.95 (d, 2H, J = 6.0 Hz), 3.23 (m, 1H), 3.40 (d, 2H, J = 11.4 Hz) , 3.75-3.85 (m, 2H), 3.86 (d, 1H, J = 9.3 Hz), 6.14 (d, 1H, J = 8.5 Hz), 6.15 (s, 1H), 6.29 (d, 1H, J = 8.5 Hz), 7.06 (d, 1H, J = 8.5 Hz).

Compound Ii-65

¹H-NMR (CDCl_Three) δ: 1.08-1.16 (m, 2H), 1.14 (d, 6H, J = 6.8 Hz), 1.21-1.30 (m, 2H), 1.29 (s, 9H), 1.78 (t, 2H, J = 10.6 Hz ), 1.83-1.92 (m, 2H), 2.11-2.19 (m, 2H), 2.78 (d, 2H, J = 10.6 Hz), 3.06 (s, 2H), 3.23 (m, 1H), 3.38 (s, 2H), 3.70-3.80 (m, 2H), 4.02 (d, 1H, J = 9.9 Hz), 5.37 (s, 1H), 6.30 (s, 1H).

Compound Ii-66

¹H-NMR (DMSO-d₆) δ: 1.01-1.12 (m, 2H), 1.20-1.34 (m, 2H), 1.27 (s, 9H), 1.54 (m, 1H), 1.82-1.99 (m, 4H), 2.91-2.98 (m, 2H), 3.06 (m, 1H), 6.17 (s, 1H), 6.63 (s, 1H), 6.78 (d, 1H, J = 9.0 Hz), 7.20 (m, 1H), 7.27 (m, 1H), 7.77 (d, 1H, J = 9.0 Hz), 7.98 (d, 1H, J = 9.0 Hz), 8.54 (s, 1H).

Compound Ii-67

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 1.88-1.96 (m, 2H), 2.78-2.86 (m, 2H), 3.02 (m, 1H), 5.89 (s, 1H), 6.56 (d, 1H, J = 8.4 Hz), 6.76 (d, 1H, J = 8.4 Hz), 7.02 (d, 1H, J = 8.4 Hz).

Compound Ii-68

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.19 (s, 9H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.80-1.96 (m, 4H) , 2.77 (s, 2H), 3.04 (m, 1H), 5.29 (s, 1H), 6.44 (d, 1H, J = 7.2 Hz), 6.68 (d, 1H, J = 7.2 Hz), 6.75 (d, 1H, J = 8.4 Hz).

Compound Ii-69

¹H-NMR (DMSO-d₆) δ: 0.95-1.10 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.47 (m, 1H), 1.80-1.88 (m, 2H), 1.88-1.95 (m, 2H), 2.88-2.95 (m, 2H), 3.02 (s, 1H), 6.07 (m, 1H), 6.77 (d, 1H, J = 8.4 Hz), 6.97 (d, 1H, J = 7.6 Hz), 7.26 (t, 1H, J = 7.6 Hz), 7.35-7.42 (m, 2H), 7.46 (d, 1H, J = 8.4 Hz), 7.91 (d, 1H, J = 7.6 Hz), 8.04 (s, 1H ).

Compound Ii-70

¹H-NMR (DMSO-d₆) δ: 0.93-1.05 (m, 2H), 1.10-1.32 (m, 2H), 1.26 (s, 9H), 1.42 (m, 1H), 1.78-1.86 (m, 2H), 1.86-1.95 (m, 2H), 2.78-2.83 (m, 2H), 3.03 (m, 1H), 4.80 (q, 2H, J = 9.2 Hz), 5.48 (t, 1H, J = 5.6 Hz), 6.69-6.76 (m, 2H ), 7.08 (dd, 1H, J = 8.8, 2.4 Hz), 7.45 (d, 1H, J = 2.4 Hz).

Compound Ii-71

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.20-1.32 (m, 2H), 1.27 (s, 9H), 1.82-1.88 (m, 2H), 1.88-1.97 (m, 2H), 2.83-2.88 ( m, 2H), 3.04 (m, 1H), 5.82 (s, 1H), 6.69 (m, 1H), 6.76 (d, 1H, J = 8.8 Hz), 7.12 (dd, 1H, J = 9.2, 8.8 Hz ), 7.37 (m, 1H), 7.87 (d, 1H, J = 2.8 Hz), 7.99 (s, 1H).

Compound Ii-72

Compound Ii-73

Compound Ii-74

Compound Ii-75

Compound Ii-76

Compound Ii-77

Compound Ii-78

Compound Ii-79

Compound Ii-80

Compound Ii-81

Compound Ii-82

Compound Ii-83

Compound Ii-84

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2H), 1.14-1.30 (t, 3H, J = 7.5 Hz), 1.41 (m, 1H), 1.73-1.94 (m, 4H), 2.34-2.46 (m, 2H) , 2.85 (t, 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.25 (t, 2H, J = 7.5 Hz), 3.53 (t, 2H, J = 6.6 Hz), 6.27 (d, 2H, J = 11.7 Hz), 6.52 (t, 1H, J = 5.1 Hz), 7.00 (d, 1H, J = 7.2 Hz).

Compound Ii-85

Compound Ii-86

Compound Ii-87

Compound Ii-88

Compound Ii-89

Compound Ii-90

Compound Ii-91

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.13 (d, 6H, J = 6.0 Hz), 1.18-1.30 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.40 (m, 1H ), 1.76-1.83 (m, 2H), 1.83-1.93 (m, 2H), 2.19 (dd, 1H, J = 11.2, 11.2 Hz), 2.76-2.82 (m, 2H), 3.01 (m, 1H), 3.09 (m, 1H), 3.45 (d, 2H, J = 11.2 Hz), 3.58-3.69 (m, 2H), 5.67 (m, 1H), 5.77 (d, 1H, J = 12.0 Hz), 5.90 (s , 1H), 5.91 (m, 1H), 6.91 (d, 1H, J = 7.6 Hz).

Compound Ii-92

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.14-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.75-1.92 (m, 4H) , 2.78-2.83 (m, 2H), 2.95-3.18 (m, 6H), 3.66-3.72 (m, 4H), 5.75 (brs, 1H), 6.00 (s, 1H), 6.04 (s, 1H), 6.11 (s, 1H), 6.95 (d, 1H, J = 9.0 Hz).

Compound Ii-93

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.13-1.27 (m, 5H), 1.42 (m, 1H), 1.74-1.93 (m, 4H), 2.30-2.40 (m, 2H), 2.81 (d, 2H, J = 6.6 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.49 (t, 2H, J = 7.5 Hz), 3.66 (t, 2H, J = 6.6 Hz) , 5.00-5.50 (brs, 2H), 6.07-6.15 (m, 2H), 6.25 (s, 1H), 7.00 (d, 1H, J = 6.6Hz).

Compound Ii-94

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.15-1.32 (m, 5H), 1.21 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.74-1.93 (m, 4H), 2.30 -2.42 (m, 2H), 2.81 (d, 2H, J = 6.6 Hz), 2.92-3.18 (m, 2H), 3.49 (t, 2H, J = 7.5 Hz), 3.66 (t, 2H, J = 6.6 Hz), 4.70-5.30 (brs, 2H), 6.05-6.16 (m, 2H), 6.25 (s, 1H), 6.95 (d, 1H, J = 8.1 Hz).

Compound Ii-95

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.16-1.31 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.73-1.94 (m, 4H), 2.34-2.46 (m, 2H) , 2.84 (t, 2H, J = 6.0 Hz), 2.94-3.16 (m, 2H), 3.28 (t, 2H, J = 7.5 Hz), 3.53 (t, 2H, J = 6.6 Hz), 6.27 (d, 2H, J = 11.7 Hz), 6.52 (t, 1H, J = 5.4 Hz), 6.94 (d, 1H, J = 7.8 Hz).

Compound Ii-96

¹H-NMR (DMSO-d₆) δ: 0.91-1.04 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.40 (m, 1H), 1.76-1.95 (m, 4H), 2.77-2.83 (m, 2H), 2.99-3.04 (m, 5H), 3.67-3.72 (m, 4H), 5.71 (m, 1H), 5.79 (d, 1H, J = 11.7 Hz), 5.89 (s, 1H), 5.90 (m , 1H), 6.72 (d, 1H, J = 8.4 Hz).

Compound Ii-97

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.20-1.32 (m, 2H), 1.26 (s, 9H), 1.41 (m, 1H), 1.77-1.93 (m, 4H), 2.78-2.83 (m, 2H), 2.97-3.05 (m, 5H), 3.68-3.72 (m, 4H), 5.36 (m, 1H), 6.04 (d, 1H, J = 8.0 Hz), 6.10 (s, 1H), 6.11 (d , 1H, J = 8.0 Hz), 6.72 (d, 1H, J = 8.0 Hz), 6.89 (dd, 1H, J = 8.0, 8.0 Hz).

Compound Ii-98

¹H-NMR (DMSO-d₆) δ: 0.92-1.04 (m, 2H), 1.17-1.29 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.41 (m, 1H), 1.75-1.92 (m, 4H), 2.77 -2.83 (m, 2H), 2.95-3.05 (m, 5H), 3.09 (m, 1H), 3.67-3.72 (m, 4H), 5.36 (m, 1H), 6.04 (d, 1H, J = 8.0 Hz ), 6.10 (s, 1H), 6.11 (d, 1H, J = 8.0 Hz), 6.89 (dd, 1H, J = 8.0, 8.0 Hz), 6.92 (d, 1H, J = 8.0 Hz).

Compound Ii-99

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.15-1.31 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.47-1.62 (m, 6H), 1.74 -1.94 (m, 4H), 2.78 (t, 2H, J = 6.0 Hz), 2.93-3.16 (m, 6H), 5.64-5.76 (m, 2H), 5.83-5.92 (m, 2H), 6.94 (d , 1H, J = 7.8 Hz).

Compound Ii-100

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.74-1.96 (m, 8H), 2.79 (t, 2H, J = 6.0 Hz), 2.93-3.18 (m, 6H), 5.48-5.67 (m, 4H), 6.94 (d, 1H, J = 8.1 Hz).

Compound Ii-101

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 2H), 1.13-1.29 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.39 (m, 1H), 1.47-1.62 (m, 6H), 1.75 -1.94 (m, 4H), 2.79 (t, 2H, J = 6.0 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.03-3.10 (m, 4H), 5.64-5.75 (m, 2H), 5.83-5.91 (m, 2H), 7.00 (d, 1H, J = 7.8 Hz).

Compound Ii-102

¹H-NMR (DMSO-d₆) δ: 0.90-1.07 (m, 2H), 1.13-1.29 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.41 (m, 1H), 1.74-1.96 (m, 8H), 2.79 (t, 2H, J = 6.0 Hz), 2.97 (q, 2H, J = 7.5 Hz), 3.00 (m, 1H), 3.09-3.19 (m, 4H), 5.46-5.66 (m, 4H), 6.99 ( d, 1H, J = 7.2 Hz).

Compound Ii-103

¹H-NMR (DMSO-d₆) δ: 0.91-1.03 (m, 2H), 1.16-1.29 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.40 (m, 1H), 1.75-1.92 (m, 4H), 2.20 (s, 3H), 2.35-2.43 (m, 4H), 2.75-2.82 (m, 2H), 2.88-3.13 (m, 6H), 5.67 (m, 1H), 5.76 (d, 1H, J = 11.2 Hz ), 5.82-5.92 (m, 2H), 6.91 (d, 1H, J = 8.0 Hz).

Compound Ii-104

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 2H), 1.19-1.32 (m, 2H), 1.26 (s, 9H), 1.39 (m, 1H), 1.75-1.95 (m, 4H), 2.19 (s, 3H) , 2.38-2.42 (m, 4H), 2.77-2.83 (m, 5H), 2.98-3.09 (m, 5H), 5.67 (m, 1H), 5.76 (d, 1H, J = 11.2 Hz), 5.88 (m , 1H), 5.88 (s, 1H), 6.72 (d, 1H, J = 8.8 Hz).

Compound Ii-105

¹H-NMR (DMSO-d₆) δ: 0.95-1.09 (m, 2H), 1.18-1.31 (m, 2H), 1.22 (d, 6H, J = 6.8 Hz), 1.44 (m, 1H), 1.78-1.93 (m, 4H), 2.87 -2.92 (m, 2H), 3.03 (m, 1H), 3.10 (m, 1H), 6.13 (m, 1H), 6.21 (m, 1H), 6.22 (s, 2H), 6.51 (s, 1H), 6.52 (d, 1H, J = 8.0 Hz), 6.92 (d, 1H, J = 8.0 Hz), 7.26 (s, 2H).

Compound Ii-106

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.17-1.29 (m, 5H), 1.40-1.68 (m, 3H), 1.80-1.92 (m, 2H), 2.90 (t, 2H, J = 6.0 Hz) , 2.94-3.06 (m, 3H), 6.12-6.22 (m, 4H), 6.50-6.54 (m, 2H), 6.94-7.00 (m, 1H), 7.26-7.27 (m, 2H).

Compound Ii-107

¹H-NMR (DMSO-d₆) δ: 0.91-1.03 (m, 2H), 1.16-1.29 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.40 (m, 1H), 1.74-1.92 (m, 4H), 2.75 -2.81 (m, 2H), 2.84 (s, 3H), 3.00 (m, 1H), 3.09 (m, 1H), 3.25 (s, 3H), 3.35-3.47 (m, 4H), 5.59-5.67 (m , 4H), 6.91 (d, 1H, J = 8.0 Hz).

Compound Ii-108

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.18-1.32 (m, 2H), 1.26 (s, 9H), 1.40 (m, 1H), 1.75-1.94 (m, 4H), 2.75-2.81 (m, 2H), 2.83 (s, 3H), 3.01 (m, 1H), 3.25 (s, 3H), 3.34-3.47 (m, 4H), 5.58-5.70 (m, 4H), 6.72 (d, 1H, J = (8.4 Hz).

Compound Ii-109

¹H-NMR (DMSO-d₆) δ: 0.90-1.51 (m, 10H), 1.21 (d, 6H, J = 6.9 Hz), 1.56-1.67 (m, 3H), 1.71-1.93 (m, 6H), 2.64 (s, 3H), 2.78 (t, 2H, J = 6.0 Hz), 2.93-3.17 (m, 2H), 3.44 (m, 1H), 5.56-5.77 (m, 4H), 6.94 (d, 1H, J = 7.8 Hz).

Compound Ii-110

¹H-NMR (DMSO-d₆) δ: 0.83-1.01 (m, 2H), 1.00-1.40 (m, 3H), 1.21 (d, 6H, J = 6.9 Hz), 1.68-1.91 (m, 4H), 2.73 (t, 2H, J = 6.0 Hz), 2.90-3.15 (m, 2H), 2.95 (s, 3H), 4,48 (s, 2H), 5.60-5.72 (m, 4H), 6.94 (d, 1H, J = 7.8 Hz), 7.15-7.35 (m, 5H).

Compound Ii-111

¹H-NMR (DMSO-d₆) δ: 0.97-1.14 (m, 2H), 1.14-1.33 (m, 5H), 1.45-1.61 (m, 1H), 1.81-1.96 (m, 4H), 2.90-3.10 (m, 5H), 6.34 ( t, 1H, J = 5.2 Hz), 6.51 (d, 1H, J = 2.2 Hz), 6.99-7.07 (m, 2H), 7.36 (dd, 1H, J = 8.2, 4.1 Hz), 8.02 (d, 1H , J = 8.5 Hz), 8.48 (dd, 1H, J = 4.1, 1.4 Hz).

Compound Ii-112

¹H-NMR (DMSO-d₆) δ: 0.97-1.13 (m, 2H), 1.17-1.34 (m, 8H), 1.45-1.59 (m, 1H), 1.81-1.99 (m, 4H), 2.94 (t, 2H, J = 5.9 Hz) , 2.99-3.21 (m, 2H), 6.33 (t, 1H, J = 5.4 Hz), 6.51 (d, 1H, J = 2.2 Hz), 6.96 (d, 1H, J = 7.7 Hz), 7.02 (dd, 1H, J = 13.5, 2.2 Hz), 7.36 (dd, 1H, J = 8.2, 4.1 Hz), 8.02 (d, 1H, J = 8.5 Hz), 8.48 (dd, 1H, J = 4.1, 1.4 Hz).

Compound Ii-113

¹H-NMR (DMSO-d₆) δ: 0.93-1.13 (m, 2H), 1.15-1.34 (m, 8H), 1.39-1.57 (m, 1H), 1.79-1.95 (m, 4H), 2.87 (t, 2H, J = 6.2 Hz) , 2.94-3.16 (m, 2H), 3.54 (s, 3H), 5.66 (t, 1H, J = 5.5 Hz), 6.49 (d, 1H, J = 9.6 Hz), 6.73 (d, 1H, J = 2.8 Hz), 6.91-7.02 (m, 2H), 7.29 (d, 1H, J = 9.3 Hz), 7.72 (d, 1H, J = 9.3 Hz).

Compound Ii-114

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.14-1.33 (m, 8H), 1.41-1.56 (m, 1H), 1.79-1.94 (m, 4H), 2.89 (t, 2H, J = 6.0 Hz) , 2.95-3.16 (m, 2H), 6.00 (t, 1H, J = 5.4 Hz), 6.84 (dd, 1H, J = 8.8, 2.2 Hz), 6.95 (d, 1H, J = 8.0 Hz), 7.07 ( d, 1H, J = 2.2 Hz), 7.72 (d, 1H, J = 8.8 Hz), 8.86 (s, 1H).

Compound Ii-115

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 4H), 1.26 (s, 9H), 1.40-1.51 (m, 1H), 1.84 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz) ), 2.85-2.90 (m, 2H), 2.97-3.06 (m, 1H), 5.93-5.99 (m, 1H), 6.63-6.79 (m, 3H), 7.40 (d, 1H, J = 8.8 Hz), 8.32 (s, 1H).

Compound Ii-116

¹H-NMR (DMSO-d₆) δ: 0.95-1.07 (m, 4H), 1.26 (s, 9H), 1.39-1.47 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz) ), 2.87-2.93 (m, 2H), 2.98-3.06 (m, 1H), 3.37 (s, 3H), 6.27 (s, 1H), 6.55 (d, 1H, J = 8.8 Hz), 6.73 (d, 1H, J = 8.8 Hz), 6.80 (t, 1H, J = 5.2 Hz), 7.32 (d, 1H, J = 8.8 Hz).

Compound Ii-117

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 4H), 1.20 (s, 3H), 1.22 (s, 3H), 1.39-1.51 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.88 (d , 2H, J = 12.4 Hz), 2.87-2.94 (m, 2H), 2.97-3.07 (m, 1H), 3.08-3.14 (m, 1H), 3.37 (s, 3H), 6.27 (s, 1H), 6.55 (d, 1H, J = 8.4 Hz), 6.82 (t, 1H, J = 5.6 Hz), 6.94 (d, 1H, J = 8.0 Hz), 7.32 (d, 1H, J = 8.4 Hz).

Compound Ii-118

¹H-NMR (DMSO-d₆) δ: 0.92-1.06 (m, 4H), 1.26 (s, 9H), 1.38-1.50 (m, 1H), 1.83 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz) ), 2.80-2.86 (m, 2H), 2.96-3.06 (m, 1H), 3.26 (s, 3H), 5.58-5.65 (m, 1H), 6.27 (d, 1H, J = 8.4 Hz), 6.38 ( s, 1H), 6.75 (d, 1H, J = 8.4 Hz), 6.99 (d, 1H, J = 8.4 Hz).

Compound Ii-119

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 4H), 1.26 (s, 9H), 1.39-1.50 (m, 1H), 1.84 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz) ), 2.81-2.89 (m, 2H), 2.96-3.07 (m, 1H), 3.51 (s, 3H), 5.79-5.84 (m, 1H), 6.60 (s, 1H), 6.75 (d, 1H, J = 8.8 Hz), 7.03 (d, 1H, J = 8.8 Hz), 7.19 (d, 1H, J = 8.8 Hz).

Compound Ii-120

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 4H), 1.26 (s, 9H), 1.37-1.40 (m, 1H), 1.42 (s, 3H), 1.44 (s, 3H), 1.83 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz), 2.79-2.96 (m, 2H), 2.97-3.07 (m, 1H), 4.33-4.46 (m, 1H), 5.50-5.59 (m, 1H ), 6.25 (d, 1H, J = 8.8 Hz), 6.57 (s, 1H), 6.75 (d, 1H, J = 8.4 Hz), 7.00 (d, 1H, J = 8.4 Hz).

Compound Ii-121

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.26 (s, 9H), 1.36-1.49 (m, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz) ), 2.80-2.87 (m, 2H), 2.95-3.97 (m, 1H), 3.27 (s, 3H), 5.85-5.92 (m, 1H), 6.33 (s, 1H), 6.36 (s, 1H), 6.75 (d, 1H, J = 8.8 Hz).

Compound Ii-122

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 4H), 1.26 (s, 9H), 1.38-1.41 (m, 1H), 1.42 (s, 3H), 1.43 (s, 3H), 1.82 (d, 2H, J = 11.8 Hz), 1.90 (d, 2H, J = 11.8 Hz), 2.83-2.88 (m, 2H), 2.98-3.06 (m, 1H), 4.33-4.47 (m, 1H), 6.35 (s, 1H), 6.54 (s, 1H), 6.76 (d, 1H, J = 8.4 Hz), 8.32 (s, 1H).

Compound Ii-123

¹H-NMR (DMSO-d₆) δ: 0.93-1.06 (m, 4H), 1.22 (s, 3H), 1.24 (s, 3H), 1.26 (s, 9H), 1.39-1.50 (m, 1H), 1.81 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz), 2.87-2.93 (m, 2H), 2.96-3.07 (m, 1H), 4.39-4.47 (m, 1H), 6.30 (s, 1H), 6.54 (d, 1H, J = 8.8 Hz), 6.77 (d, 1H, J = 8.8 Hz), 6.86 (t, 1H, J = 5.2 Hz), 7.32 (d, 1H, J = 8.4 Hz).

Compound Ii-124

¹H-NMR (DMSO-d₆) δ: 0.90-1.05 (m, 4H), 1.26 (s, 9H), 1.36-1.51 (m, 1H), 1.79 (d, 2H, J = 12.4 Hz), 1.90 (d, 2H, J = 12.4 Hz) ), 2.80-2.86 (m, 2H), 3.01 (s, 3H), 3.02-3.05 (m, 1H), 3.49 (t, 2H, J = 4.8 Hz), 4.26 (t, 2H, J = 4.8 Hz) , 6.02 (s, 1H), 6.20 (t, 1H, J = 5.6 Hz), 6.31 (d, 1H, J = 8.8 Hz), 6.74 (d, 1H, J = 8.8 Hz), 7.43 (d, 1H, J = 8.4 Hz).

Compound Ii-125

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 4H), 1.08 (t, 3H, J = 7.2 Hz), 1.25 (s, 9H), 1.35-1.42 (m, 1H), 1.79 (d, 2H, J = 12.0 Hz) ), 1.90 (d, 2H, J = 12.0 Hz), 2.80-2.86 (m, 2H), 2.96-3.05 (m, 1H), 3.42-3.51 (m, 4H), 4.20-4.26 (m, 2H), 6.03 (s, 1H), 6.20 (s, 1H), 6.31 (d, 1H, J = 8.8 Hz), 6.75 (d, 1H, J = 8.8 Hz), 7.42 (d, 1H, J = 8.8 Hz).

Compound Ii-126

¹H-NMR (DMSO-d₆) δ: 0.92-1.02 (m, 4H), 1.09 (s, 3H), 1.11 (s, 3H), 1.25 (s, 9H), 1.43-1-1.55 (m, 1H), 1.80 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.0 Hz), 2.84 (m, 2H), 2.97-3.08 (m, 1H), 3.37 (t, 2H, J = 5.2 Hz), 4.18 (t, 2H, J = 5.2 Hz), 4.71-4.80 (m, 1H), 6.05 (s, 1H), 6.19 (t, 1H, J = 5.2 Hz), 6.32 (d, 1H, J = 8.8 Hz), 6.74 (d, 1H, J = 8.4 Hz), 7.18 (d, 1H, J = 8.4 Hz).

Compound Ii-127

¹H-NMR (DMSO-d₆) δ: 0.94-1.12 (m, 2H), 1.14-1.39 (m, 5H), 1.34-1.56 (m, 1H), 1.70-1.97 (m, 4H), 2.87-3.10 (m, 5H), 6.17 ( t, 1H, J = 5.2 Hz), 6.94-7.06 (m, 2H), 7.35-7.47 (m, 4H), 7.75-7.80 (m, 1H), 8.07 (d, 1H, J = 3.0 Hz).

Compound Ii-128

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.14-1.31 (m, 5H), 1.31-1.55 (m, 1H), 1.70-1.96 (m, 4H), 2.89-3.09 (m, 5H), 6.24 ( t, 1H, J = 5.4 Hz), 6.94-7.05 (m, 2H), 7.24 (d, 1H, J = 6.9 Hz), 7.52 (t, 1H, J = 8.0 Hz), 7.75 (d, 1H, J = 8.8 Hz), 7.88-7.97 (m, 2H), 8.07 (d, 1H, J = 2.5 Hz).

Compound Ii-129

¹H-NMR (DMSO-d₆) δ: 0.98-1.12 (m, 2H), 1.18-1.30 (m, 2H), 1.19 (t, 3H, J = 6.8 Hz), 1.48 (m, 1H), 1.79-1.95 (m, 4H), 2.92 -3.09 (m, 3H), 2.97 (q, 2H, J = 6.8 Hz), 6.27 (m, 1H), 7.01 (d, 1H, J = 8.0 Hz), 7.39-7.47 (m, 2H), 7.56 ( m, 1H), 8.18-8.25 (m, 2H), 8.23 (s, 2H).

Compound Ii-130

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.15-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.45-1.64 (m, 1H), 1.78-1.96 (m, 4H) , 2.97 (q, 2H, J = 7.2 Hz), 2.95-3.15 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 6.94-7.02 (m, 2H ), 7.38 (t, 1H, J = 6.0 Hz), 7.46 (t, 2H, J = 7.5 Hz), 7.78 (d, 1H, J = 9.0 Hz), 7.96 (d, 2H, J = 9.0 Hz).

Compound Ii-131

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.15-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.48-1.62 (m, 1H), 1.78-1.96 (m, 4H) , 2.98 (q, 2H, J = 7.2 Hz), 2.94-3.10 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.02 (d, 1H, J = 9.0 Hz), 7.10 (t, 1H, J = 5.4 Hz), 7.22 (td, 1H, J = 9.0, 3.0 Hz), 7.47-7.56 (m, 1H), 7.77-7.88 (m, 3H).

Compound Ii-132

¹H-NMR (DMSO-d₆) δ: 0.96-1.13 (m, 2H), 1.15-1.32 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.48-1.65 (m, 1H), 1.78-1.96 (m, 4H) , 2.98 (q, 2H, J = 7.2 Hz), 2.94-3.12 (m, 1H), 3.22-3.28 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.01 (d, 1H, J = 6.0 Hz), 7.09 (t, 1H, J = 5.4 Hz), 7.27-7.35 (m, 2H), 7.42-7.50 (m, 1H), 7.57 (dd, 1H, J = 9.0, 3.0 Hz), 7.86 (td, 1H, J = 7.5, 3.0 Hz).

Compound Ii-133

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.58 (m, 1H), 1.72-1.94 (m, 4H) , 2.95-3.20 (m, 4H), 4.89-4.98 (m, 2H), 6.65 (brs, 1H), 6.92 (d, 1H, J = 9.0 Hz), 6.91-6.98 (m, 1H), 7.03 (d , 1H, J = 9.0 Hz).

Compound Ii-134

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.15-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.42-1.58 (m, 1H), 1.72-1.94 (m, 4H) , 2.92-3.20 (m, 4H), 6.74 (t, 1H, J = 6.0 Hz), 6.94 (t, 1H, J = 6.0 Hz), 6.97 (s, 1H), 7.08-7.24 (m, 5H).

Compound Ii-135

¹H-NMR (DMSO-d₆) δ: 0.95-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.48-1.60 (m, 1H), 1.76-1.94 (m, 4H) , 2.92-3.10 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.18-3.30 (m, 2H), 6.89 (d, 1H, J = 9.6 Hz), 7.02 (brs, 1H), 7.11 (t, 1H, J = 5.4 Hz), 7.42-7.56 (m, 2H), 7.85 (d, 1H, J = 9.6 Hz), 7.93 (d, 1H, J = 7.5 Hz), 8.03 (s, 1H ).

Compound Ii-136

¹H-NMR (DMSO-d₆) δ: 0.98-1.12 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.48-1.62 (m, 1H), 1.78-1.96 (m, 4H) , 2.92-3.12 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.22-3.32 (m, 2H), 6.89 (d, 1H, J = 9.0 Hz), 7.01 (d, 1H, J = 7.5 Hz), 7.20 (t, 1H, J = 6.0 Hz), 7.62 (s, 1H), 7.91 (d, 1H, J = 9.0 Hz), 8.02 (s, 2H).

Compound Ii-137

¹H-NMR (DMSO-d₆) δ: 0.95-1.12 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.65-1.95 (m, 5H), 2.93-3.12 (m, 1H) , 2.97 (q, 2H, J = 7.2 Hz), 3.25-3.40 (m, 2H), 5.07-5.16 (m, 2H), 7.01 (d, 1H, J = 7.5 Hz), 7.25 (t, 1H, J = 6.0 Hz), 7.92-8.03 (m, 3H), 8.33 (d, 1H, J = 6.0 Hz).

Compound Ii-138

¹H-NMR (DMSO-d₆) δ: 0.91-1.26 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.36-1.43 (m, 1H), 1.78-1.90 (m, 4H), 2.90-3.07 (m, 3H) , 2.96 (q, 2H, J = 7.5 Hz), 5.69 (t, 1H, J = 5.7 Hz), 5.81 (d, 1H, J = 2.4 Hz), 7.00 (d, 1H, J = 7.8 Hz), 7.16 -7.39 (m, 3H), 7.73-7.79 (m, 1H), 7.86-7.88 (m, 1H).

Compound Ii-139

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.20 (s, 3H), 1.22 (s, 3H), 1.40−1.52 (m, 1H), 1.81 (d, 2H, J = 12.4 Hz), 1.88 (d , 2H, J = 12.4 Hz), 2.90-2.98 (m, 2H), 2.99-3.13 (m, 2H), 5.68 (t, 1H, J = 5.6 Hz), 5.81 (s, 1H), 6.93 (d, 1H, J = 8.8 Hz), 7.16-7.40 (m, 3H), 7.76 (t, 1H, J = 8.0 Hz), 7.87 (s, 1H).

Compound Ii-140

¹H-NMR (DMSO-d₆) δ: 0.90-1.06 (m, 4H), 1.26 (s, 9H), 1.40−1.49 (m, 1H), 1.82 (d, 2H, J = 12.4 Hz), 1.91 (d, 2H, J = 12.4 Hz) ), 2.90-2.99 (m, 2H), 3.01-3.06 (m, 1H), 5.67 (t, 1H, J = 6.0 Hz), 5.81 (s, 1H), 6.74 (d, 1H, J = 8.4 Hz) , 7.14-7.40 (m, 3H), 7.76 (t, 1H, J = 8.4 Hz), 7.87 (s, 1H).

Compound Ii-141

¹H-NMR (DMSO-d₆) δ: 0.97-1.06 (m, 2H), 1.18-1.27 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.45-1.59 (m, 1H), 1.76-1.81 (m, 2H) , 1.87-1.91 (m, 2H), 2.97-3.09 (m, 1H), 3.10-3.13 (m, 1H), 3.17-3.22 (m, 2H), 6.94-7.02 (m, 2H), 6.98 (td, 1H, J = 7.8, 1.2 Hz), 7.36 (dd, 1H, J = 7.8, 0.6 Hz), 7.65 (dd, 1H, J = 7.8, 0.6 Hz), 8.00-8.05 (m, 1H).

Compound Ii-142

¹H-NMR (DMSO-d₆) δ: 0.96-1.04 (m, 2H), 1.18-1.28 (m, 2H), 1.20 (d, 6H, J = 6.9 Hz), 1.43-1.59 (m, 1H), 1.74-1.79 (m, 2H) , 1.85-1.90 (m, 2H), 2.92-3.07 (m, 1H), 3.09-3.18 (m, 3H), 6.92-6.99 (m, 2H), 7.10 (td, 1H, J = 7.8, 1.2 Hz) , 7.21 (dd, 1H, J = 7.8, 0.6 Hz), 7.31 (dd, 1H, J = 7.8, 0.6 Hz), 7.89-7.97 (m, 1H).

Compound Ii-143

¹H-NMR (DMSO-d₆) δ: 0.97-1.07 (m, 2H), 1.17-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.57 (m, 1H), 1.73-1.78 (m, 2H) , 1.86-1.90 (m, 2H), 2.93-3.02 (m, 1H), 2.97 (q, 2H, J = 7.2 Hz), 3.11 (t, 2H, J = 6.3 Hz), 6.91-7.02 (m, 2H ), 7.19 (dd, 1H, J = 8.4, 4.8 Hz), 7.34 (dd, 1H, J = 9.3, 2.4 Hz), 8.00 (t, 1H, J = 6.0 Hz).

Compound Ii-144

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.16-1.24 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.59 (m, 1H), 1.74-1.80 (m, 2H) , 1.85-1.90 (m, 2H), 2.92-3.03 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 3.18 (t, 2H, J = 6.3 Hz), 6.99-7.07 (m, 2H ), 7.33 (dd, 1H, J = 9.0, 4.8 Hz), 7.58 (dd, 1H, J = 8.7, 2.7 Hz), 8.00 (t, 1H, J = 5.4 Hz).

Compound Ii-145

¹H-NMR (DMSO-d₆) δ: 0.97-1.09 (m, 2H), 1.17-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.72-1.81 (m, 2H) , 1.85-1.92 (m, 2H), 2.95-3.06 (m, 1H), 2.97 (q, 2H, J = 7.5 Hz), 3.19 (t, 2H, J = 6.0 Hz), 7.01 (d, 1H, J = 8.1 Hz), 7.20-7.23 (m, 1H), 7.33 (dd, 1H, J = 8.7, 0.6 Hz), 7.58 (dd, 1H, J = 2.1, 0.9 Hz), 8.11-8.18 (m, 1H) .

Compound Ii-146

¹H-NMR (DMSO-d₆) δ: 0.98-1.06 (m, 2H), 1.15-1.21 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.42-1.58 (m, 1H), 1.70-1.81 (m, 2H) , 1.82-1.96 (m, 2H), 2.93-3.00 (m, 3H), 3.13-3.19 (m, 2H), 6.98-7.02 (m, 2H), 7.26-7.27 (m, 1H), 7.32-7.35 ( m, 1H), 8.18-8.21 (m, 1H).

Compound Ii-147

¹H-NMR (DMSO-d₆) δ: 0.98-1.04 (m, 2H), 1.16-1.23 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.73-1.78 (m, 2H) , 1.86-1.89 (m, 2H), 2.93-3.00 (m, 3H), 3.11-3.15 (m, 2H), 6.72-6.79 (m, 1H), 7.00-7.08 (m, 2H), 7.29-7.34 ( m, 1H), 8.13-8.16 (m, 1H).

Compound Ii-148

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.15-1.26 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.45-1.58 (m, 1H), 1.72-1.80 (m, 2H) , 1.84-1.92 (m, 2H), 2.96 (q, 2H, J = 7.2 Hz), 2.96-3.05 (m, 1H), 3.09-3.16 (m, 2H), 6.99 (d, 1H, J = 8.0 Hz ), 7.13 (dd, 1H, J = 8.0, 2.0 Hz), 7.20 (d, 1H, J = 8.4 Hz), 7.49 (d, 1H, J = 2.0 Hz), 8.11 (t, 1H, J = 6.0 Hz) ).

Compound Ii-149

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.43-1.59 (m, 1H), 1.74-1.80 (m, 2H) , 1.86-1.91 (m, 2H), 2.93-3.01 (m, 3H), 3.17-3.22 (m, 2H), 7.00-7.05 (m, 2H), 7.37-7.39 (m, 1H), 7.65-7.68 ( m, 1H), 8.22-8.26 (m, 1H).

Compound Ii-150

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.29 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.44-1.60 (m, 1H), 1.74-1.80 (m, 2H) , 1.86-1.91 (m, 2H), 2.95-3.17 (m, 2H), 3.21-3.27 (m, 2H), 6.95-6.98 (m, 1H), 8.10 (dd, 1H, J = 8.4, 2.7 Hz) , 8.19 (dd, 1H, J = 3.0, 1.5 Hz), 8.44-8.47 (m, 1H).

Compound Ii-151

¹H-NMR (DMSO-d₆) δ: 0.99-1.04 (m, 2H), 1.15-1.23 (m, 2H), 1.21 (d, 6H, J = 6.3 Hz), 1.43-1.59 (m, 1H), 1.73-1.81 (m, 2H) , 1.85-1.91 (m, 2H), 2.97-3.18 (m, 2H), 3.21-3.29 (m, 2H), 6.95-6.98 (m, 1H), 8.20-8.23 (m, 2H), 8.58-8.61 ( m, 1H).

Compound Ii-152

¹H-NMR (DMSO-d₆) δ: 0.96-1.04 (m, 2H), 1.15-1.26 (m, 2H), 1.25 (s, 9H), 1.56-1.62 (m, 1H), 1.78-1.83 (m, 2H), 1.87-1.93 ( m, 2H), 2.98-3.08 (m, 1H), 3.17 (t, 2H, J = 6.3 Hz), 3.48 (s, 3H), 6.47 (d, 2H, J = 8.7 Hz), 6.89-6.96 (m , 2H), 7.11-7.19 (m, 2H).

Compound Ii-153

¹H-NMR (DMSO-d₆) δ: 0.95-1.04 (m, 2H), 1.13-1.30 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.41 (m, 1H), 1.71-1.94 (m, 4H), 2.80 -2.89 (m, 2H), 2.92-3.10 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz), 3.21-3.30 (m, 2H), 6.25-6.35 (m, 2H), 6.39 (dd , 1H, J = 8.4, 2.1 Hz), 7.01 (d, 1H, J = 7.5 Hz), 7.01 (dd, 1H, J = 8.4, 8.4 Hz).

Compound Ii-154

¹H-NMR (DMSO-d₆) δ: 0.91-1.09 (m, 2H), 1.16-1.28 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.42 (m, 1H), 1.74-1.95 (m, 4H), 2.80 -3.16 (m, 9H), 2.97 (q, 2H, J = 7.5 Hz), 6.24-6.36 (m, 2H), 6.30 (dd, 1H, J = 8.4, 2.1 Hz), 7.10 (dd, 1H, J = 8.4, 2.1 Hz), 7.05 (d, 1H, J = 8.4 Hz).

Compound Ii-155

Compound Ii-156

Compound Ii-157

Compound Ii-158

¹H-NMR (DMSO-d₆) δ: 0.91-1.07 (m, 2H), 1.10-1.30 (m, 5H), 1.41 (m, 1H), 1.76-1.94 (m, 4H), 2.74-2.83 (m, 2H), 2.83 (s, 3H), 2.90-3.08 (m, 3H), 2.96 (s, 3H), 5.68 (m, 1H), 6.39 (m, 1H), 6.58 (m, 1H), 6.95 (dd, 1H, J = 8.4, 8.4 Hz), 7.00 (d, 1H, J = 7.8 Hz).

Compound Ii-159

Compound Ii-160

Compound Ii-161

Compound Ii-162

Compound Ii-163

Compound Ii-164

Compound Ii-165

Compound Ii-166

Compound Ii-167

Compound Ii-168

Compound Ii-169

Compound Ii-170

Compound Ii-171

Compound Ii-172

Compound Ii-173

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.15-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.43 (m, 1H), 1.76-1.85 (m, 2H), 1.85 -1.93 (m, 2H), 2.76-2.82 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 2.97 (t, 2H, J = 7.2 Hz), 3.00 (m, 1H), 3.64- 3.70 (m, 4H), 6.33 (m, 1H), 6.37 (d, 1H, J = 8.4 Hz), 6.56 (s, 1H), 7.00 (d, 1H, J = 7.8 Hz), 7.28 (d, 1H , J = 8.4 Hz).

Compound Ii-174

Compound Ii-175

Compound Ii-176

Compound Ii-177

Compound Ii-178

Compound Ii-179

Compound Ii-180

Compound Ii-181

Compound Ii-182

Compound Ii-183

Compound Ii-184

Compound Ii-185

Compound Ii-186

Compound Ii-187

Compound Ii-188

Compound Ii-189

Compound Ii-190

Compound Ii-191

Compound Ii-192

Compound Ii-193

Compound Ii-194

Compound Ii-195

Compound Ii-196

Compound Ii-197

Compound Ii-198

Compound Ii-199

Compound Ii-200

Compound Ii-201

Compound Ii-202

Compound Ii-203

Compound Ii-204

Compound Ii-205

Compound Ii-206

¹H-NMR (DMSO-d₆) δ: 0.98-1.24 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.02-2.14 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.86 (q, 2H, J = 7.2 Hz), 3.64-3.82 (m, 1H), 6.40 (d, 2H, J = 8.1 Hz), 7.01 (d, 2H, J = 7.2 Hz), 7.32-7.50 (m, 4H), 7.99 (d, 2H, J = 6.9 Hz)

化合物Ij-3

¹H-NMR (DMSO-d₆) δ: 0.96-1.26 (m, 4H), 1.18 (t, 3H, J = 7.5 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.02-2.14 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.40-6.50 (m,2H), 6.85-6.92 (m, 1H), 6.97-7.03 (m, 1H), 7.22-7.35 (m, 2H), 7.36-7.46 (m, 2H), 7.88-7.96 (m, 1H)

化合物Ij-4

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.50 (t, 1H, J = 3.9 Hz), 6.53 (s, 1H), 7.00 (t, 1H, J = 5.7 Hz), 7.25 (t, 1H, J = 7.2 Hz), 7.34-7.45 (m, 2H), 7.55 (d, 2H, J = 7.2 Hz), 7.67 (dd, 1H, J = 8.7, 2.7 Hz), 8.29 (d, 1H, J = 2.7 Hz)

化合物Ij-5

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.52 (d, 1H, J = 8.4 Hz), 6.60 (d, 1H, J = 7.8 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.20-7.36 (m, 3H), 7.46 (t, 1H, J = 8.1 Hz), 7.55 (d, 1H, J = 8.7 Hz), 8.15 (s, 1H)

化合物Ij-6

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.51 (d, 1H, J = 8.7 Hz), 6.60 (d, 1H, J = 7.5 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.02-7.12 (m, 1H), 7.36-7.48 (m, 3H), 7.71 (dd, 1H, J = 8.7, 2.1 Hz), 8.33 (d, 1H, J = 2.1 Hz)

化合物Ij-7

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.50 (d, 2H, J = 8.7 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.16-7.26 (m, 2H), 7.52-7.68 (m, 3H), 8.25 (s, 1H)

化合物Ij-8

¹H-NMR (CDCl₃) δ: 1.15-1.26 (m, 4H), 1.40 (t, 3H, J = 7.5 Hz), 1.55-1.58 (m, 1H), 1.93 (d, 2H, J = 9.7 Hz), 2.23 (d, 2H, J = 9.7 Hz), 3.01-3.11 (m, 4H), 3.56-3.61 (m, 1H), 3.84 (s, 3H), 4.34 (t, 1H, J = 6.1 Hz), 4.83-4.86 (m, 1H), 6.46 (d, 1H, J = 8.6 Hz), 6.99 (d, 1H, J = 8.5 Hz), 7.05 (d, 1H, J = 8.5 Hz), 7.29 (s, 1H), 7.30-7.34 (m, 1H), 7.69 (dd, 1H, J = 8.7, 2.4 Hz), 8.25 (s, 1H).

化合物Ij-9

¹H-NMR (CDCl₃) δ: 1.16-1.24 (m, 4H), 1.40 (t, 3H, J = 6.2 Hz), 1.55-1.59 (m, 1H), 1.94 (d, 2H, J = 11.8 Hz), 2.23 (d, 2H, J = 11.8 Hz), 3.03-3.09 (m, 4H), 3.58-3.62 (m, 1H), 3.88 (s, 3H), 4.29 (t, 1H, J = 6.4 Hz), 4.85-4.89 (m, 1H), 6.49 (d, 1H, J = 8.7 Hz), 6.88 (dd, 1H, J = 8.7, 2.2 Hz), 7.04-7.06 (m, 1H), 7.10 (d, 1H, J = 8.7 Hz), 7.36 (t, 1H, J = 7.9 Hz), 7.70 (dd, 1H, J = 8.7, 2.2 Hz), 8.32 (s, 1H).

化合物Ij-10

¹H-NMR (CDCl₃) δ: 1.19-1.30 (m, 4H), 1.41 (t, 3H, J = 6.3 Hz), 1.56-1.59 (m, 1H), 1.94 (d, 2H, J = 11.1 Hz), 2.23 (d, 2H, J = 11.1 Hz), 3.01-3.11 (m, 4H), 3.57-3.61 (m, 1H), 3.87 (s, 3H), 4.27 (t, 1H, J = 6.4 Hz), 4.98 (s, 1H), 6.50 (dd, 1H, J = 8.7, 2.2 Hz), 6.99 (d, 2H, J = 8.9 Hz), 7.43 (d, 2H, J = 8.7 Hz), 7.68 (dd, 1H, J = 8.7, 2.2 Hz), 8.25 (s, 1H).

化合物Ij-11

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2H), 1.09-1.25 (m, 5H), 1.39 (m, 1H), 1.75-1.86 (m, 2H), 1.95-2.07 (m, 2H), 2.34 (s, 3H), 2.78 (t, 2H, J = 6.2 Hz), 2.98 (q, 2H, J = 7.3 Hz), 3.65 (m, 1H), 6.45-6.53 (m, 2H), 7.01 (t, 1H, J = 5.6 Hz), 7.07 (d, 1H, J = 7.1 Hz), 7.23-7.38 (m, 3H), 7.64 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.26 (d, 1H, J = 2.5 Hz).

化合物Ij-12

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2H), 1.09-1.27 (m, 11H), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.2 Hz), 2.84-3.03 (m, 3H), 3.66 (m, 1H), 6.45-6.54 (m, 2H), 7.01 (t, 1H, J = 5.8 Hz), 7.13 (d, 1H, J = 6.9 Hz), 7.27-7.41 (m, 3H), 7.66 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.27 (d, 1H, J = 2.2 Hz).

化合物Ij-13

¹H-NMR (DMSO-d₆) δ: 0.92-1.09 (m, 2H), 1.09-1.25 (m, 5H), 1.39 (m, 1H), 1.76-1.85 (m, 2H), 1.95-2.06 (m, 2H), 2.78 (t, 2H, J = 6.2 Hz), 2.98 (q, 2H, J = 7.3 Hz), 3.68 (m, 1H), 6.52 (d, 1H, J = 8.8 Hz), 6.66 (d, 1H, J = 8.0 Hz), 7.02 (t, 1H, J = 5.5 Hz), 7.23 (d, 1H, J = 8.1 Hz), 7.49-7.55 (m, 2H), 7.62 (d, 1H, J1 = 8.5 Hz), 7.72 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.35 (d, 1H, J = 2.5 Hz).

化合物Ij-14

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.22 (d, 6H, J = 6.4 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.95-2.03 (m, 2H), 2.81 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.60-3.75 (m, 1H), 6.65 (d, 1H, J = 4.8 Hz), 6.70 (s, 1H), 6.88-6.98 (m, 2H), 8.16 (d, 1H, J = 5.2 Hz).

化合物Ij-15

¹H-NMR (CDCl₃) δ: 1.02-1.28 (m, 4H), 1.38 (d, 6H, J = 6.9 Hz), 1.52 (m, 1H), 1.85-1.94 (m, 2H), 2.11-2.21 (m, 2H), 3.01 (t, 2H, J = 6.6 Hz), 3.10-3.25 (m, 1H), 3.38-3.54 (m, 1H), 4.22 (t, 1H, J = 6.3 Hz), 4.58 (d, 1H, J = 7.8 Hz), 6.34 (d, 1H, J = 1.8 Hz), 6.53 (dd, 1H, J = 5.4, 1.8 Hz), 7.93 (d, 1H, J = 5.4 Hz).

化合物Ij-16

¹H-NMR (CDCl₃) δ: 1.03-1.28 (m, 4H), 1.37 (d, 6H, J = 6.9 Hz), 1.52 (m, 1H), 1.84-1.93 (m, 2H), 2.11-2.21 (m, 2H), 3.01 (t, 2H, J = 6.6 Hz), 3.09-3.24 (m, 1H), 3.40-3.54 (m, 1H), 4.26 (t, 1H, J = 6.6 Hz), 4.44 (d, 1H, J = 8.1 Hz), 6.29 (d, 1H, J = 8.7 Hz), 7.33 (dd, 1H, J = 8.7, 2.7 Hz), 7.99 (d, 1H, J = 2.7 Hz).

化合物Ij-17

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.21 (d, 6H, J = 6.8 Hz), 1.36 (m, 1H), 1.76-1.84 (m, 2H), 1.92-2.00 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.08-3.18 (m, 1H), 3.45-3.56 (m, 1H), 6.36 (d, 1H, J = 8.4 Hz), 6.43 (d, 1H, J = 7.2 Hz), 6.75 (d, 1H, J = 7.6 Hz), 6.94 (t, 1H, J = 6.0 Hz), 7.33 (t, 1H, J = 7.6 Hz).

化合物Ij-18

¹H-NMR (DMSO-d₆) δ: 0.98-1.24 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.14 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.64-3.82 (m, 1H), 6.40 (d, 2H, J = 8.4 Hz), 6.95-7.05 (m, 2H), 7.35-7.50 (m, 4H), 7.99 (d, 2H, J = 7.2 Hz)

化合物Ij-19

¹H-NMR (CDCl₃) δ: 1.22-1.38 (m, 4H), 1.38 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.12-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.16 (t, 1H, J = 6.4 Hz), 4.82-4.92 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 7.10-7.20 (m, 2H), 7.23-7.33 (m, 1H), 7.37 (t, 1H, J = 8.0 Hz), 7.65 (d, 1H, J = 8.7 Hz), 8.24 (s, 1H).

化合物Ij-20

¹H-NMR (CDCl₃) δ: 1.22-1.38 (m, 4H), 1.39 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.12-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.16 (t, 1H, J = 6.4 Hz), 4.78-4.88 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 6.98(t, 1H, J = 5.7 Hz), 7.18 (d, 1H, J = 8.0 Hz), 7.23-7.29 (m, 1H), 7.33-7.40 (m, 1H), 7.65 (d, 1H, J = 8.7 Hz), 8.29 (s, 1H).

化合物Ij-21

¹H-NMR (CDCl₃) δ: 1.10-1.30 (m, 4H), 1.38 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.13-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.15 (t, 1H, J = 6.4 Hz), 4.78-4.88 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 7.07-7.14 (m, 2H), 7.40-7.46 (m, 2H), 7.62 (d, 1H, J = 8.7 Hz), 8.23 (s, 1H).

化合物Ij-22

¹H-NMR (DMSO-d₆) δ: 0.95-1.25 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.25-1.50 (br, 1H), 1.81 (d, 2H, J = 11.4 Hz), 2.00 (d, 2H, J = 10.5 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.05-3.22 (m, 1H), 3.58-3.80 (m, 1H), 3.76 (s, 3H), 6.49 (d, 2H, J = 8.7 Hz), 6.50-6.70 (br, 1H), 6.95-7.10 (m, 3H), 7.20-7.32 (m, 2H), 7.51 (d, 1H, J = 7.2Hz), 8.05 (br, 1H). ESI(positive) 418.3 [M+H]+

化合物Ij-23

¹H-NMR (DMSO-d₆) δ: 0.95-1.32 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.25-1.55 (br, 1H), 1.82 (d, 2H, J = 11.4 Hz), 2.01 (d, 2H, J = 10.2 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.05-3.22 (m, 1H), 3.58-3.78 (m, 1H), 3.80 (s, 3H), 6.59 (d, 2H, J = 9.6 Hz), 6.85 (dd, 1H, J = 8.4 Hz, 2.4 Hz), 6.99 (t, 3H, J = 5.7Hz), 7.05-7.18 (m, 2H), 7.32 (d, 1H, J = 7.8Hz), 7.76 (d, 1H, J = 8.4Hz), 8.27 (d, 1H, J = 2.1 Hz). ESI(positive) 418.3 [M+H]+

化合物Ij-24

¹H-NMR (DMSO-d₆) δ: 0.92-1.25 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.28-1.48 (m, 1H), 1.81 (d, 2H, J = 10.8 Hz), 2.00 (d, 2H, J = 9.6 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.08-3.22 (m, 1H), 3.58-3.74 (m, 1H), 3.77 (s, 3H), 6.51 (d, 2H, J = 8.7 Hz), 6.97 (d, 2H, J = 8.7 Hz), 6.98 (brs, 1H), 7.48 (d, 2H, J = 8.7 Hz), 7.63 (dd, 1H, J = 11.4Hz, 2.4Hz), 8.21 (d, 1H, J = 2.4 Hz). ESI(positive) 418.3[M+H]+

化合物Ij-25

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.95-2.05 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.80 (m, 1H), 6.65 (d, 1H, J = 5.4 Hz), 6.70 (s, 1H), 6.87 (t, 1H, J = 6.0 Hz), 6.94 (d, 1H, J = 7.8 Hz), 8.16 (d, 1H, J = 5.4 Hz)

化合物Ij-26

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.94-2.04 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.80 (m, 1H), 6.53 (d, 1H, J = 8.7 Hz), 6.87 (t, 1H, J = 5.7 Hz), 7.19 (d, 1H, J = 7.5 Hz), 7.59 (dd, 1H, J = 9.0, 2.4 Hz), 8.26 (d, 1H, J = 2.4 Hz)

化合物Ij-27

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.26 (s, 9H), 1.38 (m, 1H), 1.76-1.86 (m, 2H), 1.92-2.02 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.40-3.60 (m, 1H), 6.36 (d, 1H, J = 8.1 Hz), 6.43 (d, 1H, J = 6.9 Hz), 6.80 (d, 1H, J = 7.5 Hz), 6.86 (t, 1H, J = 5.4 Hz), 7.34 (t, 1H, J = 8.4 Hz)

化合物Ij-28

¹H-NMR ((DMSO-d₆) δ: 0.93-1.18 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.75-1.86 (m, 2H), 1.94-2.05 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 3.09-3.27 (m, 2H), 6.19 (d, 1H, J = 8.1 Hz), 6.64 (d, 2H, J = 8.7 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.33 (d, 2H, J = 8.7 Hz) Mass：379[M+H]⁺

化合物Ij-29

¹H-NMR (DMSO-d₆) δ: 0.93-1.18 (m, 4H), 1.22 (s, 3H), 1.24 (s, 3H), 1.32-1.49 (m, 2H), 1.82 (d, 2H, J = 11.2 Hz), 2.04 (d, 2H, J = 11.2 Hz), 2.75-2.87 (m, 2H), 3.07-3.28 (m, 2H), 6.64 (s, 1H), 6.96 (s, 1H), 7.10-7.22 (m, 2H), 7.25-7.39 (m, 2H), 7.77-7.90 (m, 2H), 8.63 (s, 1H). 融点：161-162℃

化合物Ij-30

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.86 (m, 2H), 1.94-2.05 (m, 2H), 2.88 (t, 2H, J = 6.3 Hz), 3.19 (m, 1H), 6.19 (d, 1H, J = 7.5 Hz), 6.64 (d, 2H, J = 8.7 Hz), 6.88 (d, 1H, J = 6.0Hz), 7.33 (d, 2H, J = 8.7 Hz) Mass：392M+

化合物Ij-31

¹H-NMR (DMSO-d₆) δ: 0.92-1.16 (m, 4H), 1.26 (s, 9H), 1,36 (m, 1H), 1.72-1.83 (m, 2H), 1.92-2.02 (m, 2H), 2.87 (t, 2H, J = 6.3 Hz), 3.12 (m, 1H), 6.09-6.23 (m, 4H), 6.87 (t, 1H, J = 6.0 Hz) Mass：361[M+H]⁺

化合物Ij-32

¹H-NMR (CDCl₃) δ: 1.00-1.20 (m, 4H), 1.40 (s, 9H), 1.42-1.64 (m, 2H), 1.84-1.95 (m, 2H), 2.09-2.20 (m, 2H), 3.07 (m, 1H), 3.07 (t, 2H, J = 6.3 Hz), 3.90 (m, 1H), 6.10 (dd, 2H, J = 9.6, 5.4 Hz).

化合物Ij-33

¹H-NMR (DMSO-d₆) δ: 0.93-1.21 (m, 5H), 1.28 (s, 9H), 1.33-1.46 (m, 1H), 1.82 (d, 2H, J = 11.6 Hz), 2.04 (d, 2H, J = 11.6 Hz), 2.86-2.95 (m, 2H), 3.03-3.29 (m, 1H), 6.59-6.71 (m, 1H), 6.80-6.92 (m, 1H), 7.09-7.21 (m, 2H), 7.27-7.37 (m, 2H), 7.77-7.88 (m, 2H), 8.58-8.67 (s, 1H). 融点：172-173℃

化合物Ij-34

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24(m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.38 (m, 1H), 1.76-1.86 (m, 2H), 1.92-2.00 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.48-3.60 (m, 1H), 6.95 (t, 1H, J = 5.6 Hz), 7.41 (d, 1H, J = 7.6 Hz), 7.63 (s, 1H), 7.82 (s, 1H).

化合物Ij-35

¹H-NMR (DMSO-d₆) δ: 0.96-1.26 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.92-2.02 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.48-3.62 (m, 1H), 6.87 (t, 1H, J = 6.0 Hz), 7.45 (d, 1H, J = 7.5 Hz), 7.63 (s, 1H), 7.82 (s, 1H)

化合物Ij-36

¹H-NMR (DMSO-d₆) δ: 0.96-1.06 (m, 2H), 1.12-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.39 (m, 1H), 1.78-1.84 (m, 2H), 1.95-1.99 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.10-3.20 (m, 1H), 3.74-3.88 (m, 1H), 6.80 (s, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.93 (d, 2H, J = 7.2 Hz), 8.53 (s, 1H).

化合物Ij-37

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.93 (d, 1H, J = 7.5 Hz), 7.04 (t, 1H, J = 5.7 Hz), 7.26-7.38 (m, 2H), 7.40-7.52 (m, 1H), 7.57 (d, 1H, J = 9.0 Hz), 7.85 (t, 1H, J =7.8 Hz)

化合物Ij-38

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 3.80 (s, 3H), 6.72 (d, 1H, J = 7.8 Hz), 6.77 (d, 1H, J = 9.0 Hz), 6.98-7.10 (m, 2H), 7.12 (d, 1H, J = 8.4 Hz), 7.38 (t, 1H, J = 8.1 Hz), 7.56 (d, 1H, J = 9.3 Hz), 7.61 (d, 1H, J = 7.8 Hz)

化合物Ij-39

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.92 (d, 1H, J = 7.5 Hz), 7.04 (t, 1H, J = 5.7 Hz), 7.21 (t, 1H, J = 8.7 Hz), 7.46-7.56 (m, 1H), 7.75-7.88 (m, 3H)

化合物Ij-40

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.15-1.26 (m, 2H), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.14 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.76-3.87 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.91 (d, 1H, J = 7.5 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.42-7.52 (m, 2H), 7.83 (d, 1H, J = 8.0 Hz), 7.93 (d, 1H, J = 8.0 Hz), 8.02 (s, 1H).

化合物Ij-41

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.20 (t, 3H, J = 7.5 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.76-3.90 (m, 1H), 6.88 (d, 1H, J = 9.3 Hz), 6.97 (d, 1H, J = 7.5 Hz), 7.03 (t, 1H, J = 5.7 Hz), 7.67-7.77 (m, 2H), 7.92 (d, 1H, J = 9.6 Hz), 8.26 (d, 1H, J = 6.9 Hz), 8.33(s, 1H)

化合物Ij-42

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.20 (t, 3H, J= 7.2 Hz), 1.22-1.28 (m, 1H), 1.35-1.50 (m, 2H), 1.84 (d, 2H, J = 12.0 Hz), 2.08 (d, 2H, J = 12.0 Hz), 2.63-2.76 (m, 2H), 2.91-3.03 (m, 2H), 3.75-3.90 (m, 1H), 6.86 (d, 1H, J = 9.2 Hz), 6.93 (d, 1H, J = 7.2 Hz), 6.98-7.07 (m, 1H), 7.36 (d, 1H, J = 7.2 Hz), 7.59 (t, 1H, J = 8.0 Hz), 7.85 (d, 1H, J = 9.2 Hz), 7.91-8.02 (m, 2H). 融点：144-145℃

化合物Ij-43

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.10-1.24 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.98-2.06 (m, 2H), 2.81 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.62-3.74 (m, 1H), 6.84 (d, 1H, J =9.2 Hz), 6.88-6.98 (m, 2H), 7.31 (d, 1H, J = 9.6 Hz).

化合物Ij-44

¹H-NMR (DMSO-d₆) δ: 0.94-1.26 (m, 4H), 1.20 (d, 6H, J = 6.6 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.06-3.20 (m, 1H), 3.72-3.90 (m, 1H), 6.75-6.88 (m, 2H), 6.97 (t, 1H, J = 6.0 Hz), 7.30-7.48 (m, 3H), 7.76 (d, 1H, J = 9.3 Hz), 7.94 (d, 2H, J =8.4 Hz)

化合物Ij-45

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.85 (d, 1H, J = 9.0 Hz), 6.91 (d, 1H, J = 7.5 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.25-7.36 (m, 2H), 7.40-7.50 (m, 1H), 7.57 (d, 1H, J = 6.9 Hz), 7.85 (t, 1H, J =8.1 Hz)

化合物Ij-46

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.85 (d, 1H, J = 9.3 Hz), 6.90 (d, 1H, J = 7.5 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.21 (t, 1H, J = 7.8 Hz), 7.46-7.56 (m, 1H), 7.75-7.86 (m, 3H)

化合物Ij-47

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.81 (d, 1H, J = 7.5 Hz), 6.84 (d, 1H, J = 9.3 Hz), 6.98 (t, 1H, J = 6.3 Hz), 7.25-7.35 (m, 2H), 7.77 (d, 1H, J = 9.3 Hz), 7.96-8.06 (m, 2H)

化合物Ij-48

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.80 (s, 3H), 6.71 (d, 1H, J = 7.8 Hz), 6.76 (d, 1H, J = 9.3 Hz), 6.98 (t, 1H, J = 5.7 Hz), 7.05 (d, 1H, J = 7.2 Hz), 7.12 (d, 1H, J = 7.8 Hz), 7.38 (t, 1H, J = 8.4 Hz), 7.56 (d, 1H, J = 9.3 Hz), 7.62 (d, 1H, J = 6.9 Hz)

化合物Ij-49

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.82 (s, 3H), 6.78-6.88 (m, 2H), 6.92-7.04 (m, 2H), 7.37 (t, 1H, J = 7.5 Hz), 7.46-7.58 (m, 2H), 7.79 (d, 1H, J = 9.3 Hz)

化合物Ij-50

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.80 (s, 3H), 6.70 (d, 1H, J = 7.8 Hz), 6.82 (d, 1H, J = 9.3 Hz), 6.95-7.05 (m, 3H), 7.72 (d, 1H, J = 9.3 Hz), 7.90 (d, 2H, J = 9.0 Hz).

化合物Ij-51

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.07-1.20 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.76-1.85 (m, 2H), 2.02-2.10 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.57-3.68 (m, 1H), 4.89-4.98 (m, 2H), 6.47 (d, 1H, J = 8.0 Hz), 6.88 (d, 1H, J = 7.5 Hz), 6.96 (t, 1H, J = 6.0 Hz), 7.02 (d, 1H, J = 7.5 Hz).

化合物Ij-52

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.07-1.20 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.52-1.74 (m, 6H), 1.77-1.85 (m, 2H), 1.87-1.97 (m, 2H), 2.02-2.09 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.55-3.65 (m, 1H), 5.25-5.32 (m, 1H), 6.19 (d, 1H, J = 8.0 Hz), 6.77 (s, 2H), 6.95 (t, 1H, J = 6.0 Hz).

化合物Ij-53

¹H-NMR (DMSO-d₆) δ: 0.92-1.15 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 1.88-1.95 (m, 4H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.25-3.35 (m, 4H), 3.55-3.65 (m, 1H), 5.80-5.85 (m, 1H), 6.72 (d, 1H, J = 8.0 Hz), 6.80 (d, 1H, J = 8.0 Hz), 6.96 (t, 1H, J = 6.0 Hz).

化合物Ij-54

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 6.56 (d, 1H, J = 8.0 Hz), 6.90-6.98 (m, 2H), 7.03-7.10 (m, 3H), 7.15 (t, 1H, J = 8.0 Hz), 6.38 (t, 2H, J = 8.0 Hz).

化合物Ij-55

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.90-6.98 (m, 2H), 7.05-7.15 (m, 3H), 7.21 (t, 2H, J = 8.0 Hz).

化合物Ij-56

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 3.75 (s, 3H), 6.49 (d, 1H, J = 8.0 Hz), 6.87-6.98 (m, 4H), 7.00-7.07 (m, 3H).

化合物Ij-57

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.27 (s, 9H), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.00-2.10 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.76 (m, 1H), 6.82-6.92 (m, 2H), 6.96 (d, 1H, J = 7.8 Hz), 7.32 (d, 1H, J = 9.6 Hz).

化合物Ij-58

¹H-NMR (DMSO-d₆) δ: 0.99-1.28 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.78-1.86 (m, 2H), 2.04-2.10 (m, 2H), 2.82 (t, 2H, J = 6.1 Hz), 3.06-3.20 (m, 1H), 3.80-3.96 (m, 1H), 6.71 (d, 1H, J = 9.0 Hz), 6.76-6.86 (m, 1H), 6.90-6.98 (m, 1H), 7.10 (t, 1H, J = 8.1 Hz), 7.39-7.50 (m, 2H), 7.56 (d, 1H, J = 7.5 Hz), 7.78 (d, 1H, J = 7.5 Hz).

化合物Ij-59

¹H-NMR (DMSO-d₆) δ: 0.99-1.28 (m, 4H), 1.27 (s, 9H), 1.40 (m, 1H), 1.80-1.85 (m, 2H), 2.04-2.09 (m, 2H), 2.91 (t, 2H, J = 6.1 Hz), 3.80-3.96 (m, 1H), 6.70 (d, 1H, J = 9.0 Hz), 6.81-6.87 (m, 2H), 7.10 (t, 1H, J = 8.1 Hz), 7.39-7.44 (m, 2H), 7.56 (d, 1H, J = 7.5 Hz), 7.79 (d, 1H, J = 7.5 Hz).

化合物Ij-60

¹H-NMR (DMSO-d₆) δ: 0.97-1.09 (m, 2H), 1.23 (d, 6H, J = 6.9 Hz), 1.31-1.50 (m, 2H), 1.82-1.87 (m, 2H), 2.01-2.05 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.11-3.20 (m, 1H), 4.00-4.18 (m, 1H), 6.83 (d, 1H, J = 5.7 Hz), 6.90-7.06 (m, 2H), 7.45 (t, 1H, J = 6.9 Hz), 7.59 (t, 1H, J = 8.1 Hz), 7.67 (d, 1H, J = 8.4 Hz), 7.83 (d, 1H, J = 5.7 Hz), 8.27 (d, 1H, J = 7.5 Hz).

化合物Ij-61

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.28 (s, 9H), 1.29-1.50 (m, 2H), 1.82-1.87 (m, 2H), 2.01-2.05 (m, 2H), 2.91 (t, 2H, J = 7.8 Hz), 4.00-4.18 (m, 1H), 6.82-6.89 (m, 2H), 6.97 (d, 1H, J = 7.5 Hz ), 7.45 (t, 1H, J = 7.2 Hz), 7.59 (t, 1H, J = 8.1 Hz), 7.67 (d, 1H, J = 7.8 Hz), 7.84 (d, 1H, J = 6.0 Hz), 8.27 (d, 1H, J = 8.4 Hz).

化合物Ij-62

¹H-NMR (DMSO-d₆) δ: 0.96-1.14 (m, 2H), 1.18-1.30 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.14 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.58-3.70 (m, 1H), 6.95-7.03 (m, 2H), 7.20 (t, 1H, J = 7.5 Hz ), 7.37 (d, 1H, J = 8.1 Hz), 7.64 (d, 1H, J = 7.5 Hz), 7.92 (d, 1H, J = 7.8 Hz).

化合物Ij-63

¹H-NMR (DMSO-d₆) δ: 1.00 (dd, 2H, J = 24.8, 10.6 Hz), 1.15-1.22 (m, 2H), 1.18 (t, 3H, J = 7.6 Hz), 1.27 (s, 9H), 1.34-1.40 (m, 1H), 1.81 (d, 2H, J = 11.6 Hz), 2.07 (d, 2H, J = 11.6 Hz), 2.60 (q, 2H, J = 7.6 Hz), 2.89 (t, 2H, J = 6.3 Hz), 3.52-3.63 (m, 1H), 6.87 (t, 1H, J = 5.8 Hz), 7.04 (d, 1H, J = 7.9 Hz), 7.27 (d, 1H, J = 8.2 Hz), 7.47 (s, 1H), 7.80 (d, 1H, J = 7.6 Hz).

化合物Ij-64

¹H-NMR (DMSO-d₆) δ: 0.92-1.10 (m, 2H), 1.12-1.25 (m, 2H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.89 (t, 2H, J = 6.0 Hz), 3.50-3.66 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.03 (dd, 1H, J = 8.7, 2.7 Hz), 7.32-7.37 (m, 1H), 7.58 (dd, 1H, J = 8.7, 2.7 Hz), 7.92 (d, 1H, J = 7.2 Hz).

化合物Ij-65

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 24.6, 10.2 Hz), 1.21 (dd, 2H, J = 24.6, 10.2 Hz), 1.27 (s, 9H), 1.34-1.40 (m, 1H), 1.82 (d, 2H, J = 11.2 Hz), 2.08 (d, 2H, J = 11.2 Hz), 2.89 (t, 2H, J = 6.2 Hz), 3.59-3.65 (m, 1H), 6.87 (t, 1H, J = 5.8 Hz), 7.21 (dd, 1H, J = 8.6, 2.4 Hz), 7.34 (d, 1H, J = 8.6 Hz), 7.77 (d, 1H, J = 1.8 Hz), 8.06 (d, 1H, J = 7.6 Hz).

化合物Ij-66

¹H-NMR (CDCl₃) δ: 1.09-1.46 (m, 4H), 1.41 (s, 9H), 1.54 (m, 1H), 1.90-2.00 (m, 2H), 2.24-2.34 (m, 2H), 3.09 (t, 2H, J = 6.6 Hz), 3.46-3.60 (m, 1H), 3.99 (t, 1H, J = 6.6 Hz), 6.58 (brs, 1H), 7.58(s, 2H), 7.85 (s, 1H).

化合物Ij-67

¹H-NMR (DMSO-d₆) δ: 0.90-1.30 (m, 4H), 1.27 (s, 9H), 1.30-1.48 (m, 1H), 1.82 (d, 2H, J = 11.1 Hz), 2.08 (d, 2H, J = 9.6 Hz), 2.89 (t, 2H, J = 6.3 Hz), 3.55-3.70 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.17 (m, 1H), 7.41 (d, 1H, J = 8.7 Hz), 7.77 (d, 1H, J = 1.5 Hz), 8.10 (d, 1H, J = 7.5 Hz). ESI(positive)m/z 466.2 [M+H]+

化合物Ij-68

¹H-NMR (DMSO-d₆) δ: 0.90-1.28 (m, 4H), 1.25 (s, 9H), 1.32 (m, 1H), 1.76-1.82 (m, 2H), 2.00-2.10 (m, 2H), 2.87 (t, 2H, J = 6.6 Hz), 3.50-3.62 (m, 1H), 3.71 (s, 3H), 6.77 (dd, 1H, J = 8.7, 2.7 Hz), 6.84 (t, 1H, J = 5.7 Hz), 7.22-7.28 (m, 2H), 7.66 (d, 1H, J = 7.2 Hz).

化合物Ij-69

¹H-NMR (DMSO-d₆) δ: 0.94-1.10 (m, 2H), 1.12-1.25 (m, 2H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.90 (t, 2H, J = 6.0 Hz), 3.52-3.68 (m, 1H), 3.84 (s, 3H), 6.82 (d, 1H, J = 8.1 Hz), 6.88 (t, 1H, J = 5.4 Hz), 6.95 (t, 1H, J = 7.8 Hz), 7.23 (d, 1H, J = 7.8 Hz), 7.83 (d, 1H, J = 7.8 Hz).

化合物Ij-70

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.17-1.32 (m, 2H), 1.40 (m, 1H), 1.76-1.88 (m, 2H), 2.04-2.14 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.78 (m, 1H), 7.03 (t, 1H, J = 6.3 Hz), 7.45-7.54 (m, 2H), 8.10 (s, 1H), 8.34 (d, 1H, J = 7.2 Hz).

化合物Ij-71

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 26.1, 12.3 Hz), 1.16-1.22 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.35-1.41 (m, 1H), 1.70-1.77 (m, 1H), 1.82 (d, 2H, J = 11.6 Hz), 2.08 (d, 2H, J = 11.6 Hz), 2.81 (t, 2H, J = 6.3 Hz), 3.66-3.72 (m, 1H), 6.99 (t, 1H, J = 6.3 Hz), 7.23 (dd, 1H, J = 8.1, 4.7 Hz), 7.66 (d, 1H, J = 8.1 Hz), 8.07 (d, 1H, J = 4.7 Hz), 8.26 (d, 1H, J = 6.3 Hz).

化合物Ij-72

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 24.8, 11.3 Hz), 1.18-1.23 (m, 2H), 1.27 (s, 9H), 1.36-1.39 (m, 1H), 1.82 (d, 2H, J = 11.5 Hz), 2.08 (d, 2H, J = 11.5 Hz), 2.89 (t, 2H, J = 6.1 Hz), 3.65-3.73 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.23 (dd, 1H, J = 8.1, 4.8 Hz), 7.66 (d, 1H, J = 7.9 Hz), 8.07 (d, 1H, J = 4.7 Hz), 8.26 (d, 1H, J = 7.6 Hz).

化合物Ij-73

¹H-NMR (CDCl₃)δ: 1.09-1.46 (m, 4H), 1.41 (s, 9H), 1.55 (m, 1H), 1.92-2.02 (m, 2H), 2.24-2.34 (m, 2H), 3.09 (t, 2H, J = 6.3 Hz), 3.58-3.72 (m, 1H), 3.98 (t, 1H, J = 6.0 Hz), 6.30 (brs, 1H), 7.62(d, 1H, J = 8.1 Hz), 7.77 (d, 1H, J = 8.4 Hz).

化合物Ij-74

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.12-1.40 (m, 3H), 1.25 (s, 9H), 1.76-1.86 (m, 2H), 1.98-2.10 (m, 2H), 2.87 (d, 2H, J = 6.3 Hz), 3.40-3.56 (m, 1H), 6.85 (brs, 1H), 6.93 (t, 1H, J = 7.5 Hz), 7.07 (t, 1H, J = 7.5 Hz), 7.20 (d, 1H, J = 7.5 Hz), 7.29 (d, 1H, J = 7.8 Hz), 7.79 (brs, 1H).

化合物Ij-75

¹H-NMR (CDCl₃) δ: 1.08-1.26 (m, 2H), 1.36-1.60 (m, 3H), 1.40 (s, 9H), 1.92-2.02 (m, 2H), 2.22-2.32 (m, 2H), 3.08 (t, 2H, J = 6.6 Hz), 3.68-3.80 (m, 1H), 4.03 (t, 1H, J = 6.0 Hz), 7.06 (brs, 1H), 7.20-7.36(m, 3H).

化合物Ij-76

¹H-NMR (DMSO-d₆) δ: 1.02 (dd, 2H, J = 25.2, 12.4 Hz), 1.17 (t, 3H, J = 7.1 Hz), 1.20 (t, 3H, J = 7.3 Hz), 1.26-1.35 (m, 2H), 1.37-1.42 (m, 1H), 1.83 (d, 2H, J = 11.6 Hz), 2.05 (d, 2H, J = 11.6 Hz), 2.80 (t, 2H, J = 6.4 Hz), 2.99 (q, 2H, J = 7.3 Hz), 3.65-3.72 (m, 1H), 4.01 (q, 2H, J = 7.1 Hz), 6.32 (d, 1H, J = 7.9 Hz), 6.86-6.94 (m, 2H), 7.01 (t, 1H, J = 6.0 Hz), 7.12 (d, 1H, J = 6.9 Hz), 7.17 (d, 1H, J = 6.8 Hz).

化合物Ij-77

¹H-NMR (DMSO-d₆) δ: 1.02 (dd, 2H, J = 24.8, 10.8 Hz), 1.19-1.21 (m, 2H), 1.30 (s, 9H), 1.37-1.41 (m, 1H), 1.84 (d, 2H, J = 10.6 Hz), 2.06 (d, 2H, J = 10.6 Hz), 2.92 (t, 2H, J = 6.3 Hz), 3.50-3.52 (m, 1H), 6.42 (d, 1H, J = 8.1 Hz), 6.83 (d, 1H, J = 7.9 Hz), 6.88-6.92 (m, 2H), 7.11-7.14 (m, 2H), 10.58 (s, 1H).

化合物Ij-78

¹H-NMR (DMSO-d₆) δ: 0.97-1.05 (m, 2H), 1.20-1.26 (m, 2H), 1.28 (s, 9H), 1.34-1.38 (m, 1H), 1.84 (d, 2H, J = 11.5 Hz), 2.07 (d, 2H, J = 11.5 Hz), 2.90 (t, 2H, J = 6.1 Hz), 3.47 (s, 3H), 3.63-3.69 (m, 1H), 6.34 (d, 1H, J = 7.6 Hz), 6.87-6.93 (m, 3H), 7.11 (d, 1H, J = 8.4 Hz), 7.17 (d, 1H, J = 8.4 Hz).

化合物Ij-79

¹H-NMR (DMSO-d₆) δ: 1.03 (dd, 2H, J = 23.6, 10.8 Hz), 1.18 (t, 3H, J = 7.5 Hz), 1.25-1.34 (m, 2H), 1.29 (s, 9H), 1.37-1.40 (m, 1H), 1.86 (d, 2H, J = 11.7 Hz), 2.07 (d, 2H, J = 11.7 Hz), 2.92 (t, 2H, J = 6.2 Hz), 3.67-3.73 (m, 1H), 4.03 (q, 2H, J = 7.1 Hz), 6.34 (d, 1H, J = 7.9 Hz), 6.87-6.96 (m, 3H), 7.14 (dd, 1H, J = 8.1, 1.2 Hz), 7.19 (dd, 1H, J = 8.1, 1.2 Hz).

化合物Ij-80

¹H-NMR (DMSO-d₆) δ: 1.00 (dd, 2H, J = 23.2, 11.9 Hz), 1.19-1.25 (m, 2H), 1.28 (s, 9H), 1.33-1.38 (m, 1H), 1.45 (s, 3H), 1.47 (s, 3H), 1.83 (d, 2H, J = 11.1 Hz), 2.07 (d, 2H, J = 11.1 Hz), 2.90 (t, 2H, J = 6.1 Hz), 3.62-3.70 (m, 1H), 4.57-4.66 (m, 1H), 6.21 (d, 1H, J = 7.9 Hz), 6.82-6.94 (m, 3H), 7.18 (d, 1H, J = 7.6 Hz), 7.31 (d, 1H, J = 7.6 Hz).

化合物Ij-81

化合物Ij-82

¹H-NMR (DMSO-d₆) δ: 0.90-1.19 (m, 4H), 1.28 (s, 9H), 1.32-1.45 (m, 1H), 1.80 (d, 2H, J = 11.2 Hz), 1.98 (d, 2H, J = 11.2 Hz), 2.84-2.93 (m, 2H), 3.26 (s, 3H), 3.40-3.53 (m, 1H), 6.29 (d, 1H, J = 8.0 Hz), 6.38 (d, 1H, J = 7.2 Hz), 6.86 (s, 1H), 7.33 (d, 1H, J = 8.4 Hz).

化合物Ij-83

化合物Ij-84

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.75-1.85 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.78 (m, 1H), 6.38 (d, 1H, J = 8.1 Hz), 6.67 (s, 1H), 6.72 (d, 1H, J = 5.4 Hz), 7.00 (t, 1H, J = 6.0 Hz), 7.36-7.54 (m, 3H), 7.62 (d, 2H, J = 6.9 Hz), 8.00 (d, 1H, J = 5.4 Hz)

化合物Ij-85

¹H-NMR (DMSO-d₆) δ: 1.00-1.20 (m, 4H), 1.20 (t, 3H, J = 7.2 Hz), 1.43 (m, 1H), 1.80-1.88 (m, 2H), 2.03-2.13 (m, 2H), 2.81 (t, 3H, J = 6.0 Hz), 3.00 (q, 2H, J = 7.2 Hz), 3.26 (m, 1H), 6.17 (d, 1H, J = 7.6 Hz), 6.57 (s, 1H), 6.96-7.07 (m, 2H), 7.35 (dd, 1H, J = 8.4, 4.0 Hz), 8.02 (d, 1H, J = 8.4 Hz), 8.47 (d, 1H, J = 4.0 Hz).

化合物Ij-86

¹H-NMR (DMSO-d₆) δ: 1.00-1.24 (m, 4H), 1.23 (d, 6H, J = 6.4 Hz), 1.42 (m, 1H), 1.80-1.88 (m, 2H), 2.03-2.12 (m, 2H), 2.79-2.87 (m, 2H), 3.16 (m, 1H), 3.27 (m, 1H), 6.17 (d, 1H, J = 8.0 Hz), 6.57 (s, 1H), 6.99 (d, 1H, J = 8.0 Hz), 7.01 (s, 1H), 7.35 (dd, 1H, J = 8.0, 4.0 Hz), 8.02 (d, 1H, J = 8.0 Hz), 8.47 (d, 1H, J = 2.8 Hz).

化合物Ij-87

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.11-1.25 (m, 2H), 1.20 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.76-1.86 (m, 2H), 1.97-2.04 (m, 2H), 2.73-2.82 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.70 (m, 1H), 6.53 (d, 1H, J = 8.8 Hz), 6.53 (d, 1H, J = 8.8 Hz), 7.01 (t, 1H, J = 6.0 Hz), 7.58 (d, 1H, J = 3.2 Hz), 7.79 (d, 1H, J = 3.2 Hz), 7.86 (d, 1H, J = 8.8 Hz), 8.55 (s, 1H).

化合物Ij-88

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.09-1.20 (m, 2H), 1.19 (t, 6H, J = 7.2 Hz), 1.39 (m, 1H), 1.75-1.83 (m, 2H), 1.95-2.03 (m, 2H), 2.74-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.66 (m, 1H), 6.48 (d, 1H, J = 8.4 Hz), 6.60 (d, 1H, J = 7.6 Hz), 7.00 (t, 1H, J = 5.6 Hz), 7.06 (dd, 1H, J = 4.8, 2.4 Hz), 7.25 (d, 1H, J = 2.4 Hz), 7.37 (d, 1H, J = 4.8 Hz), 7.60 (dd, 1H, J = 8.4, 2.0 Hz), 8.26 (s, 1H).

化合物Ij-89

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.10-1.20 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.76-1.84 (m, 2H), 1.96-2.04 (m, 2H), 2.73-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.65 (m, 1H), 6.41-6.50 (m, 2H), 7.01 (t, 1H, J = 6.0 Hz), 7.44 (d, 1H, J = 4.0 Hz), 7.58 (m, 1H), 7.59 (s, 1H), 7.68 (d, 1H, J = 8.0 Hz), 8.34 (s, 1H).

化合物Ij-90

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.12-1.25 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.94-2.03 (m, 2H), 2.75-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.71 (m, 1H), 6.54 (d, 1H, J = 8.8 Hz), 6.98-7.07 (m, 2H), 7.25 (s, 1H), 7.85 (dd, 1H, J = 8.8, 2.0 Hz), 8.07 (s, 1H), 8.56 (d, 1H, J = 2.0 Hz).

化合物Ij-91

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.11-1.22 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 1.95-2.03 (m, 2H), 2.77-2.83 (m, 2H), 3.14 (m, 1H), 3.72 (m, 1H), 6.53 (d, 1H, J = 8.8 Hz), 6.97 (t, 1H, J = 6.0 Hz), 7.02 (d, 1H, J = 7.6 Hz), 7.25 (s, 1H), 7.84 (dd, 1H, J = 8.8, 2.0 Hz), 8.06 (s, 1H), 8.56 (d, 1H, J = 2.0 Hz).

化合物Ij-92

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.11-1.23 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.37 (m, 1H), 1.75-1.83 (m, 2H), 1.91-1.99 (m, 2H), 2.36-2.42 (m, 2H), 3.12 (m, 1H), 3.70 (m, 1H), 6.49 (d, 1H, J = 9.2 Hz), 6.97 (t, 1H, J = 6.0 Hz), 7.47 (d, 1H, J = 8.0 Hz), 7.62 (d, 1H, J = 8.0 Hz), 8.36 (s, 1H).

化合物Ij-93

¹H-NMR (DMSO-d₆) δ: 0.95-1.13 (m, 4H), 1.23 (d, 6H, J = 6.9 Hz), 1.31-1.44 (m, 1H), 1.78-1.82 (m, 2H), 2.03-2.06 (m, 2H), 2.76-2.82 (m, 2H), 3.10-3.19 (m, 1H), 3.20-3.25 (m, 4H), 3.58-3.65 (m, 1H), 3.69-3.74 (m, 4H), 6.04 (d, 1H, J = 7.5 Hz), 6.72 (d, 1H, J = 9.6 Hz), 6.95-6.99 (m, 1H), 7.10 (d, 1H, J = 9.6 Hz).

化合物Ij-94

¹H-NMR (DMSO-d₆) δ: 0.96-1.42 (m, 5H), 1.22 (d, 6H, J = 6.9 Hz), 1.79-1.83 (m, 2H), 2.03-2.07 (m, 2H), 2.80 (d, 2H, J = 6.3 Hz), 3.10-3.19 (m, 1H), 3.54-3.70 (m, 1H), 3.74 (s, 3H), 6.57-6.64 (m, 3H), 6.72-6.75 (m, 1H), 6.90-7.09 (m, 3H), 7.24-7.30 (m, 1H).

化合物Ij-95

¹H-NMR (DMSO-d₆) δ: 0.93-1.04 (m, 2H), 1.10-1.18 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.34-1.44 (m, 1H), 1.78-1.87 (m, 2H), 2.02-2.12 (m, 2H), 2.77-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.52-3.70 (m, 1H), 6.64 (d, 1H, J = 8.0 Hz), 6.88-7.06 (m, 5H), 7.12 (d, 1H, J = 8.0 Hz), 7.37-7.46 (m, 1H).

化合物Ij-96

¹H-NMR (DMSO-d₆) δ: 0.90-1.04 (m, 2H), 1.05-1.18 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.84 (m, 2H), 1.98-2.08 (m, 2H), 2.76-2.84 (m, 2H), 3.08-3.18 (m, 1H), 3.52-3.64 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.91-7.00 (m, 2H), 7.15-7.38 (m, 5H).

化合物Ij-97

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.25 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.35-1.47 (m, 1H), 1.78-1.87 (m, 2H), 2.02-2.10 (m, 2H), 2.78-2.83 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.70-3.82 (m, 1H), 6.82 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 7.01 (t, 1H, J = 4.5 Hz), 7.13 (d, 1H, J = 4.0 Hz), 7.43 (d, 1H, J = 4.0 Hz), 7.76 (d, 1H, J = 8.0 Hz).

化合物Ij-98

¹H-NMR (DMSO-d₆) δ: 0.97-1.10 (m, 2H), 1.17-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.49 (m, 1H), 1.80-1.88 (m, 2H), 2.04-2.12 (m, 2H), 2.77-2.83 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.88 (m, 1H), 6.85 (d, 1H, J = 8.0 Hz), 6.99-7.05 (m, 2H), 7.61 (s, 1H), 7.90 (d, 1H, J = 8.0 Hz), 8.02 (s, 2H).

化合物Ij-99

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.14-1.26 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.48 (m, 1H), 1.80-1.88 (m, 2H), 2.04-2.13 (m, 2H), 2.77-2.83 (m, 2H), 2.96 (s, 6H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.86 (m, 1H), 6.72-6.78 (m, 2H), 6.82 (d, 1H, J = 8.0 Hz), 7.02 (t, 1H, J = 4.5 Hz), 7.18 (d, 1H, J = 8.0 Hz), 7.26 (t, 1H, J = 8.0 Hz), 7.34 (s, 1H), 7.74 (d, 1H, J = 8.0 Hz).

化合物Ij-100

¹H-NMR (DMSO-d₆)δ: 0.98-1.10 (m, 2H), 1.16-1.27 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.48 (m, 1H), 1.80-1.88 (m, 2H), 2.04-2.13 (m, 2H), 2.77-2.83 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.86 (m, 1H), 6.83 (d, 1H, J = 8.0 Hz), 6.89 (d, 1H, J = 8.0 Hz), 7.02 (t, 1H, J = 4.5 Hz), 7.42-7.50 (m, 3H), 7.53-7.59 (m, 2H).

化合物Ij-101

¹H-NMR (DMSO-d₆)δ: 0.92-1.05 (m, 2H), 1.08-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.36-1.43 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.09 (m, 2H), 2.77-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.56-3.68 (m, 1H), 6.62 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 6.98 (t, 1H, J = 4.5 Hz), 7.10-7.15 (m, 3H), 7.43 (d, 2H, J = 8.0 Hz).

化合物Ij-102

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.08-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.36-1.43 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.09 (m, 2H), 2.77-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.57-3.68 (m, 1H), 6.65 (d, 1H, J = 8.0 Hz), 6.94 (d, 1H, J = 8.0 Hz), 6.97 (t, 1H, J = 4.5 Hz), 7.06 (d, 1H, J = 8.0 Hz), 7.13 (d, 1H, J = 8.0 Hz), 7.18-7.26 (m, 2H), 7.41 (t, 1H, J = 8.0 Hz).

化合物Ij-103

¹H-NMR (DMSO-d₆) δ: 0.88-1.04 (m, 2H), 1.05-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.77-1.82 (m, 2H), 2.00-2.07 (m, 2H), 2.76-2.82 (m, 2H), 3.08-3.20 (m, 1H), 3.52-3.64 (m, 1H), 6.57 (d, 1H, J = 8.0 Hz), 6.92-7.00 (m, 2H), 7.17 (d, 1H, J = 8.0 Hz), 7.23-7.28 (m, 2H), 7.38 (t, 1H, J = 8.0 Hz), 7.56 (d, 1H, J = 8.0 Hz).

化合物Ij-104

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24 (m, 2H), 1.19 (t, 3H, J = 7.6 Hz), 1.35-1.46 (m, 1H), 1.78-1.86 (m, 2H), 2.04-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.6 Hz), 3.67-3.78 (m, 1H), 6.27 (s, 2H), 6.71 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 7.02 (brs, 1H), 7.52 (s, 2H), 7.67 (d, 1H, J = 8.0 Hz).

化合物Ij-105

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.13-1.25 (m, 2H), 1.19 (t, 3H, J = 7.6 Hz), 1.35-1.46 (m, 1H), 1.78-1.87 (m, 2H), 2.04-2.12 (m, 2H), 2.76-2.83 (m, 2H), 2.99 (q, 2H, J = 7.6 Hz), 3.72-3.82 (m, 1H), 6.82 (d, 1H, J = 8.0 Hz), 6.85 (d, 1H, J = 8.0 Hz), 7.03 (t, 1H, J = 4.5 Hz), 7.12 (t, 1H, J = 4.0 Hz), 7.51 (d, 1H, J = 4.0 Hz), 7.56 (d, 1H, J = 4.0 Hz), 7.76 (d, 1H, J = 8.0 Hz).

化合物Ij-106

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.45 (m, 1H), 1.76-1.85 (m, 2H), 2.02-2.08 (m, 2H), 2.76-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.57-3.67 (m, 1H), 6.63 (d, 1H, J = 8.0 Hz), 6.92-7.00 (m, 3H), 7.13 (d, 1H, J = 8.0 Hz), 7.29-7.36 (m, 1H), 7.42-7.50 (m, 1H).

化合物Ij-107

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.83 (m, 2H), 1.98-2.06 (m, 2H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.52-3.63 (m, 1H), 6.57 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 6.97 (t, 1H, J = 4.5 Hz), 7.12 (t, 1H, J = 4.0 Hz), 7.19 (d, 1H, J = 8.0 Hz), 7.33-7.47 (m, 2H).

化合物Ij-108

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.83 (m, 2H), 1.98-2.07 (m, 2H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.54-3.63 (m, 1H), 6.63 (d, 1H, J = 8.0 Hz), 6.93-7.00 (m, 2H), 7.14 (t, 1H, J = 8.0 Hz), 7.20-7.37 (m, 3H).

化合物Ij-109

¹H-NMR (DMSO-d₆) δ: 0.82-1.05 (m, 2H), 1.05-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.43 (m, 1H), 1.76-1.83 (m, 2H), 2.00-2.08 (m, 2H), 2.29 (s, 3H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.56-3.66 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.90 (d, 1H, J = 8.0 Hz), 6.93-7.00 (m, 3H), 7.05 (d, 1H, J = 8.0 Hz), 7.17 (d, 2H, J = 8.0 Hz).

化合物Ij-110

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.28 (s, 9H), 1.32-1.43 (m, 1H), 1.80 (d, 2H, J = 12.0 Hz), 2.07 (d, 2H, J = 12.0 Hz), 2.88 (t, 2H, J = 6.4 Hz), 3.16-3.27 (m, 1H), 5.47 (d, 1H, J = 7.6 Hz), 5.80 (s, 1H), 6.83 (d, 1H, J = 6.0 Hz), 7.15-7.40 (m, 3H), 7.75 (t, 1H, J = 8.4 Hz), 7.86 (s, 1H).

化合物Ij-111

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.32-1.43 (m, 1H), 1.76-1.82 (m, 2H), 2.02-2.12 (m, 2H), 2.77-2.83 (m, 2H), 3.08-3.27 (m, 2H), 5.48 (d, 1H, J = 8.1 Hz), 5.80 (d, 1H, J = 2.7 Hz), 6.95 (t, 1H, J = 6.0 Hz), 7.15-7.39 (m, 3H), 7.75 (td, 1H, J = 8.4, 1.8 Hz), 7.86 (t, 1H, J = 2.7 Hz).

化合物Ij-112

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.30-1.45 (m, 1H), 1.76-1.82 (m, 2H), 2.02-2.12 (m, 2H), 2.77-2.83 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz) 3.10-3.30 (m, 1H), 5.48 (d, 1H, J = 7.8 Hz), 5.80 (d, 1H, J = 2.7 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.15-7.40 (m, 3H), 7.75 (td, 1H, J = 8.4, 1.8 Hz), 7.86 (t, 1H, J = 2.7 Hz).

化合物Ij-113

化合物Ij-114

化合物Ij-115

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.30-1.45 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.74-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz) 3.15-3.30 (m, 1H), 5.53 (d, 1H, J = 8.1 Hz), 5.80 (d, 1H, J = 2.4 Hz), 6.92 (t, 1H, J = 8.4 Hz), 7.01 (t, 1H, J = 6.0 Hz), 7.37-7.43 (m, 3H), 8.21 (d, 1H, J = 2.4 Hz).

化合物Ij-116

化合物Ij-117

化合物Ij-118

¹H-NMR (DMSO-d₆)δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.75-1.86 (m, 2H), 2.02-2.12 (m, 2H), 2.74-2.83 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz) 3.13-3.30 (m, 1H), 5.38 (d, 1H, J = 8.4 Hz), 5.75 (d, 1H, J = 2.7 Hz), 6.99 (t, 1H, J = 6.3 Hz), 7.18-7.28 (m, 2H), 7.63-7.70 (m, 2H), 8.11 (d, 1H, J = 2.7 Hz).

化合物Ij-119

¹H-NMR (DMSO-d₆) δ: 0.88-1.19 (m, 4H), 1.18 (t, 3H, J = 7.5 Hz), 1.28-1.45 (m, 1H), 1.73-1.83 (m, 2H), 2.02-2.13 (m, 2H), 2.73-2.81 (m, 2H), 2.95 (q, 2H, J = 7.5 Hz) 3.12-3.30 (m, 1H), 5.36 (d, 1H, J = 7.5 Hz), 5.76 (d, 1H, J = 2.4 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.30 (td, 1H, J = 7.5, 1.8 Hz), 7.42 (td, 1H, J = 7.8, 1.5 Hz), 7.53-7.60 (m, 2H), 7.84 (d, 1H, J = 2.7 Hz).

化合物Ij-120

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.74-1.84 (m, 2H), 2.02-2.10 (m, 2H), 2.75-2.82 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz) 3.20-3.30 (m, 1H), 5.52 (d, 1H, J = 7.8 Hz), 5.80 (d, 1H, J = 2.4 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.13 (d, 1H, J = 8.1 Hz), 7.40 (t, 1H, J = 8.1 Hz), 7.62 (d, 1H, J = 8.4 Hz), 7.72 (s, 1H), 8.22 (d, 1H, J = 2.4 Hz).

化合物Ij-121

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.74-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.75-2.82 (m, 2H), 2.98 (q, 2H, J = 7.5 Hz) 3.15-3.30 (m, 1H), 5.47 (d, 1H, J = 8.1 Hz), 5.78 (d, 1H, J = 2.4 Hz), 7.00 (t, 1H, J = 6.0 Hz), 7.43 (d, 2H, J = 7.8 Hz), 7.67 (d, 2H, J = 9.0 Hz), 8.17 (d, 1H, J = 2.4 Hz).

化合物Ij-122

¹H-NMR (DMSO-d₆) δ: 0.94-1.07 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.81-1.84 (m, 2H), 1.99-2.07 (m, 2H), 2.77-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.77 (m, 1H), 7.01-7.05 (m, 1H), 7.22-7.40 (m, 4H), 7.81-7.87 (m, 1H), 8.02 (s, 1H), 8.36 (s, 1H).

化合物Ij-123

¹H-NMR (DMSO-d₆) δ: 0.95-1.12 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.77-1.81 (m, 2H), 1.96-1.99 (m, 2H), 2.74-2.78 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.54-3.70 (m, 1H), 4.81 (q, 2H, J = 9.0 Hz), 6.50-6.53 (m, 1H), 6.99-7.03 (m, 1H), 7.50 (d, 1H, J =0.9 Hz) 7.83 (d, 1H, J = 0.9 Hz).

化合物Ij-124

¹H-NMR (DMSO-d₆) δ: 0.95-1.23 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.77-1.81 (m, 2H), 2.03-2.07 (m, 2H), 2.74-2.80 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.61-3.73 (m, 1H), 7.00-7.04 (m, 1H), 7.09-7.12 (m, 1H), 7.29-7.37 (m, 2H), 7.45-7.52 (m, 1H), 7.88-7.94 (m, 2H), 8.04-8.05 (m, 1H).

化合物Ij-125

¹H-NMR (DMSO-d₆) δ: 0.94-1.14 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.79-1.83 (m, 2H), 1.97-2.03 (m, 2H), 2.76-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.50-3.63 (m, 1H), 4.43 (q, 2H, J = 9.0 Hz), 7.00-7.04 (m, 1H), 7.13-7.15 (m, 1H), 7.35 (s, 1H) 7.55 (s, 1H).

化合物Ij-126

¹H-NMR (DMSO-d₆) δ: 1.02-1.08 (m, 2H), 1.17-1.29 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.36-1.43 (m, 1H), 1.79-1.85 (m, 2H), 2.05-2.11 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.53-3.62 (m, 1H), 6.98 (t, 1H, J = 7.8 Hz), 7.03 (t, 1H, J = 6.3 Hz), 7.28 (dd, 1H, J = 7.5, 1.2 Hz), 7.63 (dd, 1H, J = 7.5, 1.2 Hz), 8.28 (d, 1H, J = 7.5 Hz).

化合物Ij-127

¹H-NMR (DMSO-d₆) δ: 0.97-1.05 (m, 2H), 1.18-1.24 (m, 2H), 1.16 (t, 3H, J = 7.5 Hz), 1.34-1.41 (m, 1H), 1.77-1.81 (m, 2H), 2.02-2.08 (m, 2H), 2.76 (t, 2H, J = 6.0 Hz), 2.96 (q, 2H, J = 7.5 Hz), 3.55-3.64 (m, 1H), 7.00 (t, 1H, J = 7.8 Hz), 7.18 (dd, 1H, J = 8.4, 1.8 Hz), 7.32 (dd, 1H, J = 8.4, 0.6 Hz), 7.74 (d, 1H, J = 1.8 Hz), 8.04 (d, 1H, J = 7.8 Hz).

化合物Ij-128

¹H-NMR (DMSO-d₆) δ: 0.98-1.07 (m, 2H), 1.15-1.26 (m, 8H), 1.32-1.43 (m, 1H), 1.78-1.84 (m, 2H), 1.98-2.09 (m, 2H), 2.60 (q, 2H, J = 7.5 Hz), 2.78 (t, 2H, J = 6.3 Hz), 2.96 (q, 2H, J = 7.5 Hz), 3.55-3.64 (m, 1H), 6.98-7.05 (m, 2H), 7.27 (dd, 1H, J = 7.8, 1.8 Hz), 7.47 (m, 1H), 7.84 (d, 1H, J =7.5 Hz).

化合物Ij-129

¹H-NMR (DMSO-d₆) δ: 0.92-1.15 (m, 2H), 1.15-1.35 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.48 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.78-2.84 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.62-3.80 (m, 1H), 7.02 (t, 1H, J = 6.0 Hz), 7.45 (d, 1H, J = 9.0 Hz), 8.09 (dd, 1H, J = 9.0, 2.4 Hz), 8.68 (d, 1H, J = 2.4 Hz), 8.70 (brs, 1H).

化合物Ij-130

¹H-NMR (DMSO-d₆) δ: 0.88-1.10 (m, 2H), 1.15-1.46 (m, 3H), 1.21 (d, 6H, J = 6.6 Hz), 1.78-1.88 (m, 2H), 1.98-2.08 (m, 2H), 2.76-2.86 (m, 2H), 3.10-3.20 (m, 1H), 3.46-3.62 (m, 1H), 6.91-6.96 (m, 1H), 7.01 (brs, 1H), 7.64 (d, 1H, J = 7.8 Hz), 8.07 (d, 1H, J = 5.1 Hz), 8.35 (d, 1H, J = 7.8 Hz).

化合物Ij-131

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.15-1.30 (m, 2H), 1.27 (s, 9H), 1.30-1.43 (m, 1H), 1.77-1.86 (m, 2H), 1.98-2.08 (m, 2H), 2.86-2.92 (m, 2H), 3.35-3.50 (m, 1H), 3.73 (s, 3H), 6.69 (dd, 1H, J = 8.4, 2.0 Hz), 6.86 (t, 1H, J = 6.0 Hz), 7.01 (d, 1H, J = 2.0 Hz), 7.10 (d, 1H, J = 8.4 Hz), 7.62 (d, 1H, J = 7.6 Hz).

化合物Ij-132

¹H-NMR (DMSO-d₆)δ: 0.92-1.08 (m, 2H), 1.15-1.33 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.42 (m, 1H), 1.76-1.86 (m, 2H), 1.98-2.08 (m, 2H), 2.76-2.82 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.40-3.58 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz), 7.13 (d, 1H, J = 8.4 Hz), 7.20 (d, 1H, J = 8.4 Hz), 7.49 (s, 1H), 8.01 (d, 1H, J = 7.6 Hz).

化合物Ij-133

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.16-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.46 (m, 1H), 1.78-1.85 (m, 2H), 2.04-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.55-3.70 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz), 7.12 (t, 1H, J = 9.6 Hz), 7.48 (d, 1H, J = 7.6 Hz), 8.13 (d, 1H, J = 7.6 Hz).

化合物Ij-134

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.26 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.33-1.42 (m, 1H), 1.39-1.84 (m, 2H), 2.05-2.09 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.61-3.75 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.45 (dd, 1H, J = 7.5, 0.6 Hz), 7.60 (dd, 1H, J = 8.4, 1.5 Hz), 8.17 (d, 1H, J = 1.5 Hz), 8.50 (d, 1H, J = 7.5 Hz).

化合物Ij-135

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.25 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.35-1.44 (m, 1H), 1.80-1.84 (m, 2H), 2.05-2.08 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.19 (m, 1H), 3.62-3.78 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.79 (d, 1H, J = 2.1 Hz), 8.10 (d, 1H, J = 2.1, 1.5 Hz), 8.52 (d, 1H, J = 6.9 Hz).

化合物Ij-136

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.17-1.24 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.33-1.41 (m, 1H), 1.78-1.83 (m, 2H), 2.04-2.08 (m, 2H), 2.78 (t, 2H, J = 6.3 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.56-3.67 (m, 1H), 7.00-7.04 (m, 2H), 7.39 (d, 1H, J = 2.1 Hz), 7.66 (dd, 1H, J = 8.4, 1.8 Hz), 8.14 (d, 1H, J = 7.5 Hz).

化合物Ij-137

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.12-1.28 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.31 (t, 3H, J = 6.9 Hz), 1.33-1.46 (m, 1H), 1.76-1.85 (m, 2H), 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.22 (m, 1H), 3.50-3.64 (m, 1H), 3.98 (q, 2H, J = 6.9 Hz), 6.78 (dd, 1H, J = 8.7, 2.7 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.23-7.27 (m, 2H), 7.68 (d, 1H, J = 7.2 Hz).

化合物Ij-138

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 2H), 1.14-1.26 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.45 (m, 1H), 1.77-1.86 (m, 2H), 2.03-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.52-3.68 (m, 1H), 6.97-7.06 (m, 2H), 7.34 (dd, 1H, J = 8.4, 4.8 Hz), 7.56 (dd, 1H, J = 8.4, 2.4 Hz), 7.91 (d, 1H, J = 7.6 Hz).

化合物Ij-139

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.16-1.32 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.78-1.86 (m, 2H), 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.21 (m, 1H), 3.58-3.76 (m, 1H), 7.00 (t, 1H, J = 6.0 Hz), 8.19-8.23 (m, 2H), 8.52 (d, 1H, J = 6.9 Hz).

化合物Ij-140

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.12-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.78-1.86 (m, 2H), 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.58-3.78 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz), 8.08 (dd, 1H, J = 8.4, 2.7 Hz), 8.19 (d, 1H, J = 2.7 Hz), 8.38 (d, 1H, J = 7.2 Hz).

化合物Ij-141

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.15-1.22 (m, 5H), 1.34-1.42 (m, 1H), 1.78-1.83 (m, 2H), 2.04-2.08 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.53-3.62 (m, 1H), 3.81 (s, 1H), 7.02 (t, 1H, J = 6.3 Hz), 7.41 (s, 1H), 7.53 (s, 1H), 7.88 (d, 1H, J = 7.5 Hz).

化合物Ij-142

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.17-1.30 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.32-1.41 (m, 1H), 1.79-1.84 (m, 2H), 2.01-2.05 (m, 2H), 2.77 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.41-3.58 (m, 1H), 6.97 (dd, 1H, J = 8.4, 2.4 Hz), 6.99-7.03 (m, 1H), 7.27 (d, 1H, J = 2.4 Hz), 7.34 (dd, 1H, J = 8.4, 0.3 Hz), 8.07-8.14 (m, 1H).

化合物Ij-143

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 2H), 1.16-1.33 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.45 (m, 1H), 1.77-1.86 (m, 2H), 2.00-2.08 (m, 2H), 2.74-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.38-3.54 (m, 1H), 6.90-7.00 (m, 1H), 7.02 (t, 1H, J = 4.5 Hz), 7.19 (dd, 1H, J = 8.4, 5.1 Hz), 7.33 (dd, 1H, J = 8.4, 2.7 Hz), 7.88 (d, 1H, J = 7.8 Hz).

化合物Ij-144

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.19-1.29 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.31-1.41 (m, 1H), 1.79-1.84 (m, 2H), 2.01-2.05 (m, 2H), 2.77 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 6.9 Hz), 3.41-3.57 (m, 1H), 6.71-6.79 (m, 1H), 7.06-7.08 (m, 2H), 7.31 (dd, 1H, J = 8.7, 4.8 Hz), 8.03 (d, 1H, J = 7.8 Hz).

化合物Ij-145

¹H-NMR (DMSO-d₆) δ: 0.95-1.16 (m, 2H), 1.18-1.44 (m, 3H), 1.21 (d, 6H, J = 6.6 Hz), 1.78-1.86 (m, 2H), 2.02-2.12 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.40-3.58 (m, 1H), 6.95 (t, 1H, J = 7.8 Hz), 7.01 (brs, 1H), 7.09 (t, 1H, J = 6.9 Hz), 7.22 (d, 1H, J = 6.6 Hz), 7.31 (d, 1H, J = 7.8 Hz), 7.83 (d, 1H, J = 7.8 Hz).

化合物Ij-146

化合物Ij-147

化合物Ij-148

化合物Ij-149

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.13-1.30 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 2.02-2.14 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.56-3.70 (m, 1H), 6.95-7.05 (m, 2H), 7.20 (t, 1H, J = 7.8 Hz ), 7.37 (d, 1H, J = 7.8 Hz), 7.64 (d, 1H, J = 7.5 Hz), 7.92 (d, 1H, J = 7.5 Hz). 融点：168-169℃ Anal. Calcd for C₁₆H₂₃N₃O₂S₂: C,54.36; H,6.56; N,11.89; S,18.14. Found: C,54.33; H,6.55; N,11.89; S,18.05.

化合物Ij-150

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.77-1.87 (m, 2H), 1.99-2.12 (m, 2H), 2.78 (t, 2H, J = 6.6 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.40-3.58 (m, 1H), 6.95 (t, 1H, J = 7.8 Hz), 7.02 (t, 1H, J = 6.0 Hz), 7.09 (t, 1H, J = 7.8 Hz), 7.22 (d, 1H, J = 7.5 Hz), 7.31 (d, 1H, J = 8.1 Hz), 7.83 (d, 1H, J = 7.8 Hz). 融点：170-171℃ Anal. Calcd for C₁₆H₂₃N₃O₃S: C,56.95; H,6.87; N,12.45; S,9.50. Found: C,56.91; H,6.91; N,12.43; S,9.51.

化合物Ij-151

¹H-NMR (DMSO-d₆) δ: 0.92-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.76-1.87 (m, 2H), 2.02-2.14 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.22 (m, 1H), 3.54-3.70 (m, 1H), 6.83 (t, 1H, J = 10.5 Hz), 6.99 (t, 1H, J = 5.4 Hz), 7.17 (dd, 1H, J = 10.5, 2.1 Hz), 7.63 (dd, 1H, J = 8.4, 5.7 Hz), 8.10 (d, 1H, J = 7.5 Hz). 融点：165-166℃ Anal. Calcd for C₁₇H₂₄FN₃O₂S₂: C,52.96; H,6.27; F,4.93; N,10.90; S,16.63. Found: C,52.99; H,6.31; F,5.00; N,10.91; S,16.84.

化合物Ij-152

¹H-NMR (DMSO-d₆) δ: 0.92-1.09 (m, 2H), 1.11-1.28 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.75-1.82 (m, 2H), 2.02-2.12 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.52-3.67 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.03 (td, 1H, J = 9.6, 2.7 Hz), 7.34 (dd, 1H, J = 9.0, 5.1 Hz), 7.57 (dd, 1H, J = 9.0, 2.7 Hz), 7.91 (d, 1H, J = 7.2 Hz). 融点：151-152℃ Anal. Calcd for C₁₇H₂₄FN₃O₂S₂: C,52.96; H,6.27; F,4.93; N,10.90; S,16.63. Found: C,52.97; H,6.28; F,4.90; N,10.87; S,16.71.

化合物Ij-153

¹H-NMR (DMSO-d₆) δ: 0.94-1.12 (m, 2H), 1.14-1.31 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 2.02-2.15 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.55-3.70 (m, 1H), 6.84-6.94 (m, 1H), 6.99 (t, 1H, J = 6.0 Hz), 7.18-7.28 (m, 2H), 8.21 (d, 1H, J = 7.2 Hz).

化合物Ij-154

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.13-1.30 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.76-1.87 (m, 2H), 2.02-2.14 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.22 (m, 1H), 3.54-3.70 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.02 (dd, 1H, J = 8.1, 2.1 Hz), 7.39 (d, 1H, J = 2.1 Hz), 7.66 (d, 1H, J = 8.1 Hz), 8.15 (d, 1H, J = 7.5 Hz). 融点：166-167℃ Anal. Calcd for C₁₇H₂₄ClN₃O₂S₂: C,50.79; H,6.02; Cl,8.82; N,10.45; S,15.95. Found: C,50.84; H,6.04; Cl,8.80; N,10.44; S,16.00.

化合物Ij-155

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.20-1.34 (m, 2H), 1.22 (d, 6H, J = 6.8 Hz), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 1.99-2.14 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.42-3.54 (m, 1H), 6.74 (td, 1H, J = 8.8, 2.8 Hz), 6.98 (t, 1H, J = 5.6 Hz), 7.06 (dd, 1H, J = 9.6, 2.8 Hz), 7.30 (dd, 1H, J = 8.0, 4.4 Hz), 8.02 (d, 1H, J = 8.0 Hz). Anal. Calcd for C₁₇H₂₄FN₃O₃S: C,55.27; H,6.55; F,5.14; N,11.37; S,8.68. Found: C,55.16; H,6.50; F,5.16; N,11.30; S,8.42.

化合物Ij-156

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.20-1.34 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 2.00-2.14 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.21 (m, 1H), 3.38-3.54 (m, 1H), 6.90-7.00 (m, 2H), 7.19 (dd, 1H, J = 8.4, 4.8 Hz), 7.33 (dd, 1H, J = 8.4, 2.4 Hz), 7.86 (d, 1H, J = 7.8 Hz). 融点：170-171℃ Anal. Calcd for C₁₇H₂₄FN₃O₃S: C,55.27; H,6.55; F,5.14; N,11.37; S,8.68. Found: C,55.31; H,6.59; F,5.13; N,11.46; S,8.59.

化合物Ij-157

¹H-NMR (DMSO-d₆) δ: 0.88-1.20 (m, 4H), 1.20 (d, 6H, J = 6.9 Hz), 1.36 (m, 1H), 1.75-1.83 (m, 2H), 2.02-2.13 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 3.05-3.25 (m, 2H), 5.36 (d, 1H, J = 7.8 Hz), 5.76 (d, 1H, J = 2.4 Hz), 6.95(t, 1H, J = 6.9 Hz), 7.30 (td, 1H, J = 7.5, 1.8 Hz), 7.42 (td, 1H, J = 7.8, 1.5 Hz), 7.53-7.60 (m, 2H), 7.84 (d, 1H, J = 2.7 Hz). 融点：142-143℃

化合物Ij-158

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.19-1.34 (m, 2H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 1.99-2.14 (m, 2H), 2.88 (t, 2H, J = 6.3 Hz), 3.40-3.56 (m, 1H), 6.75 (td, 1H, J = 8.7, 2.7 Hz), 6.87 (t, 1H, J = 6.0 Hz), 7.06 (dd, 1H, J = 9.3, 2.7 Hz), 7.31 (dd, 1H, J = 8.7, 4.5 Hz), 8.02 (d, 1H, J = 7.8 Hz). 融点：220-221℃ Anal. Calcd for C₁₈H₂₆FN₃O₃S: C,56.38; H,6.83; F,4.95; N,10.96; S,8.36. Found: C,56.41; H,6.90; F,4.96; N,11.07; S,8.36.

化合物Ij-159

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2H), 1.16-1.46 (m, 3H), 1.27 (s, 9H), 1.77-1.87 (m, 2H), 1.98-2.10 (m, 2H), 2.89 (t, 2H, J = 6.0 Hz), 3.38-3.54 (m, 1H), 6.88 (t, 1H, J = 5.7 Hz), 6.90-7.00 (m, 1H), 7.19 (dd, 1H, J = 8.7, 5.1 Hz), 7.34 (dd, 1H, J = 8.7, 2.7 Hz), 7.88 (d, 1H, J = 7.5 Hz). Anal. Calcd for C₁₈H₂₆FN₃O₃S: C,56.38; H,6.83; F,4.95; N,10.96; S,8.36. Found: C,56.39; H,6.93; F,4.98; N,11.09; S,8.29.

化合物Ij-160

¹H-NMR (DMSO-d₆) δ: 0.95 (t, 3H, J = 7.8 Hz), 0.92-1.07 (m, 2H), 1.21 (d, 3H, J = 6.9 Hz), 1.20-1.47 (m, 4H), 1.77-1.96 (m, 3H), 1.98-2.08 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.85-2.98 (m, 1H), 3.42-3.57 (m, 1H), 6.71-6.80 (m, 1H), 7.00 (t, 1H, J = 5.7 Hz), 7.06 (dd, 1H, J = 9.3, 2.7 Hz), 7.31 (dd, 1H, J = 8.7, 4.5 Hz), 8.02 (d, 1H, J = 7.8 Hz). 融点：172-173℃ Anal. Calcd for C₁₈H₂₆FN₃O₃S: C,56.38; H,6.83; F,4.95; N,10.96; S,8.36. Found: C,56.37; H,6.84; F,5.04; N,11.12; S,8.14.

化合物Ij-161

¹H-NMR (DMSO-d₆) δ: 0.95 (t, 3H, J = 7.5 Hz), 0.92-1.08 (m, 2H), 1.21 (d, 3H, J = 6.9 Hz), 1.20-1.47 (m, 4H), 1.77-1.96 (m, 3H), 1.98-2.08 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.85-2.98 (m, 1H), 3.38-3.56 (m, 1H), 6.90-6.98 (m, 1H), 7.00 (t, 1H, J = 6.0 Hz), 7.19 (dd, 1H, J = 8.7, 5.1 Hz), 7.33 (dd, 1H, J = 8.7, 2.7 Hz), 7.88 (d, 1H, J = 7.8 Hz). 融点：173-174℃ Anal. Calcd for C₁₈H₂₆FN₃O₃S: C,56.38; H,6.83; F,4.95; N,10.96; S,8.36. Found: C,56.45; H,6.80; F,4.93; N,11.02; S,8.54.
Compound Ij-2

¹H-NMR (DMSO-d₆) δ: 0.98-1.24 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.02-2.14 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.86 (q, 2H, J = 7.2 Hz), 3.64-3.82 (m, 1H), 6.40 (d, 2H, J = 8.1 Hz), 7.01 (d, 2H, J = 7.2 Hz), 7.32-7.50 (m, 4H), 7.99 (d, 2H, J = 6.9 Hz)

Compound Ij-3

¹H-NMR (DMSO-d₆) δ: 0.96-1.26 (m, 4H), 1.18 (t, 3H, J = 7.5 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.02-2.14 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.40-6.50 (m, 2H), 6.85-6.92 (m, 1H), 6.97-7.03 (m, 1H), 7.22-7.35 (m, 2H), 7.36-7.46 (m, 2H), 7.88-7.96 (m, 1H)

Compound Ij-4

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.50 (t, 1H, J = 3.9 Hz), 6.53 (s, 1H) , 7.00 (t, 1H, J = 5.7 Hz), 7.25 (t, 1H, J = 7.2 Hz), 7.34-7.45 (m, 2H), 7.55 (d, 2H, J = 7.2 Hz), 7.67 (dd, 1H, J = 8.7, 2.7 Hz), 8.29 (d, 1H, J = 2.7 Hz)

Compound Ij-5

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.52 (d, 1H, J = 8.4 Hz), 6.60 (d, 1H, J = 7.8 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.20-7.36 (m, 3H), 7.46 (t, 1H, J = 8.1 Hz), 7.55 (d, 1H, J = 8.7 Hz) , 8.15 (s, 1H)

Compound Ij-6

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.51 (d, 1H, J = 8.7 Hz), 6.60 (d, 1H, J = 7.5 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.02-7.12 (m, 1H), 7.36-7.48 (m, 3H), 7.71 (dd, 1H, J = 8.7, 2.1 Hz), 8.33 (d, 1H, J = 2.1 Hz)

Compound Ij-7

¹H-NMR (DMSO-d₆) δ: 0.92-1.24 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.60-3.78 (m, 1H), 6.50 (d, 2H, J = 8.7 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.16-7.26 (m, 2H), 7.52-7.68 (m, 3H), 8.25 (s, 1H)

Compound Ij-8

¹H-NMR (CDCl_Three) δ: 1.15-1.26 (m, 4H), 1.40 (t, 3H, J = 7.5 Hz), 1.55-1.58 (m, 1H), 1.93 (d, 2H, J = 9.7 Hz), 2.23 (d, 2H , J = 9.7 Hz), 3.01-3.11 (m, 4H), 3.56-3.61 (m, 1H), 3.84 (s, 3H), 4.34 (t, 1H, J = 6.1 Hz), 4.83-4.86 (m, 1H), 6.46 (d, 1H, J = 8.6 Hz), 6.99 (d, 1H, J = 8.5 Hz), 7.05 (d, 1H, J = 8.5 Hz), 7.29 (s, 1H), 7.30-7.34 ( m, 1H), 7.69 (dd, 1H, J = 8.7, 2.4 Hz), 8.25 (s, 1H).

Compound Ij-9

¹H-NMR (CDCl_Three) δ: 1.16-1.24 (m, 4H), 1.40 (t, 3H, J = 6.2 Hz), 1.55-1.59 (m, 1H), 1.94 (d, 2H, J = 11.8 Hz), 2.23 (d, 2H , J = 11.8 Hz), 3.03-3.09 (m, 4H), 3.58-3.62 (m, 1H), 3.88 (s, 3H), 4.29 (t, 1H, J = 6.4 Hz), 4.85-4.89 (m, 1H), 6.49 (d, 1H, J = 8.7 Hz), 6.88 (dd, 1H, J = 8.7, 2.2 Hz), 7.04-7.06 (m, 1H), 7.10 (d, 1H, J = 8.7 Hz), 7.36 (t, 1H, J = 7.9 Hz), 7.70 (dd, 1H, J = 8.7, 2.2 Hz), 8.32 (s, 1H).

Compound Ij-10

¹H-NMR (CDCl_Three) δ: 1.19-1.30 (m, 4H), 1.41 (t, 3H, J = 6.3 Hz), 1.56-1.59 (m, 1H), 1.94 (d, 2H, J = 11.1 Hz), 2.23 (d, 2H , J = 11.1 Hz), 3.01-3.11 (m, 4H), 3.57-3.61 (m, 1H), 3.87 (s, 3H), 4.27 (t, 1H, J = 6.4 Hz), 4.98 (s, 1H) , 6.50 (dd, 1H, J = 8.7, 2.2 Hz), 6.99 (d, 2H, J = 8.9 Hz), 7.43 (d, 2H, J = 8.7 Hz), 7.68 (dd, 1H, J = 8.7, 2.2 Hz), 8.25 (s, 1H).

Compound Ij-11

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2H), 1.09-1.25 (m, 5H), 1.39 (m, 1H), 1.75-1.86 (m, 2H), 1.95-2.07 (m, 2H), 2.34 (s, 3H), 2.78 (t, 2H, J = 6.2 Hz), 2.98 (q, 2H, J = 7.3 Hz), 3.65 (m, 1H), 6.45-6.53 (m, 2H), 7.01 (t, 1H, J = 5.6 Hz), 7.07 (d, 1H, J = 7.1 Hz), 7.23-7.38 (m, 3H), 7.64 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.26 (d, 1H, J = 2.5 Hz).

Compound Ij-12

¹H-NMR (DMSO-d₆) δ: 0.93-1.08 (m, 2H), 1.09-1.27 (m, 11H), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.2 Hz), 2.84-3.03 (m, 3H), 3.66 (m, 1H), 6.45-6.54 (m, 2H), 7.01 (t, 1H, J = 5.8 Hz), 7.13 (d, 1H , J = 6.9 Hz), 7.27-7.41 (m, 3H), 7.66 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.27 (d, 1H, J = 2.2 Hz).

Compound Ij-13

¹H-NMR (DMSO-d₆) δ: 0.92-1.09 (m, 2H), 1.09-1.25 (m, 5H), 1.39 (m, 1H), 1.76-1.85 (m, 2H), 1.95-2.06 (m, 2H), 2.78 (t, 2H, J = 6.2 Hz), 2.98 (q, 2H, J = 7.3 Hz), 3.68 (m, 1H), 6.52 (d, 1H, J = 8.8 Hz), 6.66 (d, 1H, J = 8.0 Hz) , 7.02 (t, 1H, J = 5.5 Hz), 7.23 (d, 1H, J = 8.1 Hz), 7.49-7.55 (m, 2H), 7.62 (d, 1H, J1 = 8.5 Hz), 7.72 (dd, 1H, J1 = 8.8 Hz, J2 = 2.5 Hz), 8.35 (d, 1H, J = 2.5 Hz).

Compound Ij-14

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.22 (d, 6H, J = 6.4 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.95-2.03 (m, 2H), 2.81 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.60-3.75 (m, 1H), 6.65 (d, 1H, J = 4.8 Hz), 6.70 (s, 1H), 6.88- 6.98 (m, 2H), 8.16 (d, 1H, J = 5.2 Hz).

Compound Ij-15

¹H-NMR (CDCl_Three) δ: 1.02-1.28 (m, 4H), 1.38 (d, 6H, J = 6.9 Hz), 1.52 (m, 1H), 1.85-1.94 (m, 2H), 2.11-2.21 (m, 2H), 3.01 (t, 2H, J = 6.6 Hz), 3.10-3.25 (m, 1H), 3.38-3.54 (m, 1H), 4.22 (t, 1H, J = 6.3 Hz), 4.58 (d, 1H, J = 7.8 Hz), 6.34 (d, 1H, J = 1.8 Hz), 6.53 (dd, 1H, J = 5.4, 1.8 Hz), 7.93 (d, 1H, J = 5.4 Hz).

Compound Ij-16

¹H-NMR (CDCl_Three) δ: 1.03-1.28 (m, 4H), 1.37 (d, 6H, J = 6.9 Hz), 1.52 (m, 1H), 1.84-1.93 (m, 2H), 2.11-2.21 (m, 2H), 3.01 (t, 2H, J = 6.6 Hz), 3.09-3.24 (m, 1H), 3.40-3.54 (m, 1H), 4.26 (t, 1H, J = 6.6 Hz), 4.44 (d, 1H, J = 8.1 Hz), 6.29 (d, 1H, J = 8.7 Hz), 7.33 (dd, 1H, J = 8.7, 2.7 Hz), 7.99 (d, 1H, J = 2.7 Hz).

Compound Ij-17

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.21 (d, 6H, J = 6.8 Hz), 1.36 (m, 1H), 1.76-1.84 (m, 2H), 1.92-2.00 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.08-3.18 (m, 1H), 3.45-3.56 (m, 1H), 6.36 (d, 1H, J = 8.4 Hz), 6.43 (d, 1H, J = 7.2 Hz), 6.75 (d, 1H, J = 7.6 Hz), 6.94 (t, 1H, J = 6.0 Hz), 7.33 (t, 1H, J = 7.6 Hz).

Compound Ij-18

¹H-NMR (DMSO-d₆) δ: 0.98-1.24 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.14 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.64-3.82 (m, 1H), 6.40 (d, 2H, J = 8.4 Hz), 6.95-7.05 (m, 2H), 7.35-7.50 (m, 4H), 7.99 (d, 2H, J = 7.2 Hz)

Compound Ij-19

¹H-NMR (CDCl_Three) δ: 1.22-1.38 (m, 4H), 1.38 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.12-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.16 (t, 1H, J = 6.4 Hz), 4.82-4.92 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 7.10-7.20 (m, 2H), 7.23-7.33 (m, 1H), 7.37 (t, 1H, J = 8.0 Hz), 7.65 (d, 1H, J = 8.7 Hz), 8.24 (s, 1H).

Compound Ij-20

¹H-NMR (CDCl_Three) δ: 1.22-1.38 (m, 4H), 1.39 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.12-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.16 (t, 1H, J = 6.4 Hz), 4.78-4.88 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 6.98 (t, 1H, J = 5.7 Hz), 7.18 (d, 1H, J = 8.0 Hz), 7.23-7.29 (m, 1H), 7.33-7.40 (m , 1H), 7.65 (d, 1H, J = 8.7 Hz), 8.29 (s, 1H).

Compound Ij-21

¹H-NMR (CDCl_Three) δ: 1.10-1.30 (m, 4H), 1.38 (d, 6H, J = 8.0 Hz), 1.54 (m, 1H), 1.86-1.95 (m, 2H), 2.18-2.26 (m, 2H), 3.03 (t, 2H, J = 6.0 Hz), 3.13-3.22 (m, 1H), 3.52-3.64 (m, 1H), 4.15 (t, 1H, J = 6.4 Hz), 4.78-4.88 (m, 1H), 6.46 (d, 1H, J = 8.0 Hz), 7.07-7.14 (m, 2H), 7.40-7.46 (m, 2H), 7.62 (d, 1H, J = 8.7 Hz), 8.23 (s, 1H).

Compound Ij-22

¹H-NMR (DMSO-d₆) δ: 0.95-1.25 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.25-1.50 (br, 1H), 1.81 (d, 2H, J = 11.4 Hz), 2.00 (d, 2H , J = 10.5 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.05-3.22 (m, 1H), 3.58-3.80 (m, 1H), 3.76 (s, 3H), 6.49 (d, 2H, J = 8.7 Hz), 6.50-6.70 (br, 1H), 6.95-7.10 (m, 3H), 7.20-7.32 (m, 2H), 7.51 (d, 1H, J = 7.2Hz), 8.05 (br, 1H ). ESI (positive) 418.3 [M + H] +

Compound Ij-23

¹H-NMR (DMSO-d₆) δ: 0.95-1.32 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.25-1.55 (br, 1H), 1.82 (d, 2H, J = 11.4 Hz), 2.01 (d, 2H , J = 10.2 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.05-3.22 (m, 1H), 3.58-3.78 (m, 1H), 3.80 (s, 3H), 6.59 (d, 2H, J = 9.6 Hz), 6.85 (dd, 1H, J = 8.4 Hz, 2.4 Hz), 6.99 (t, 3H, J = 5.7 Hz), 7.05-7.18 (m, 2H), 7.32 (d, 1H, J = 7.8Hz), 7.76 (d, 1H, J = 8.4Hz), 8.27 (d, 1H, J = 2.1 Hz). ESI (positive) 418.3 [M + H] +

Compound Ij-24

¹H-NMR (DMSO-d₆) δ: 0.92-1.25 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.28-1.48 (m, 1H), 1.81 (d, 2H, J = 10.8 Hz), 2.00 (d, 2H , J = 9.6 Hz), 2.81 (t, 2H, J = 6.6 Hz), 3.08-3.22 (m, 1H), 3.58-3.74 (m, 1H), 3.77 (s, 3H), 6.51 (d, 2H, J = 8.7 Hz), 6.97 (d, 2H, J = 8.7 Hz), 6.98 (brs, 1H), 7.48 (d, 2H, J = 8.7 Hz), 7.63 (dd, 1H, J = 11.4Hz, 2.4Hz ), 8.21 (d, 1H, J = 2.4 Hz). ESI (positive) 418.3 [M + H] +

Compound Ij-25

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.95-2.05 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.80 (m, 1H), 6.65 (d, 1H, J = 5.4 Hz), 6.70 (s, 1H), 6.87 (t, 1H, J = 6.0 Hz), 6.94 (d, 1H, J = 7.8 Hz), 8.16 (d, 1H, J = 5.4 Hz)

Compound Ij-26

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.94-2.04 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.80 (m, 1H), 6.53 (d, 1H, J = 8.7 Hz), 6.87 (t, 1H, J = 5.7 Hz), 7.19 (d, 1H, J = 7.5 Hz) , 7.59 (dd, 1H, J = 9.0, 2.4 Hz), 8.26 (d, 1H, J = 2.4 Hz)

Compound Ij-27

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.26 (s, 9H), 1.38 (m, 1H), 1.76-1.86 (m, 2H), 1.92-2.02 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.40-3.60 (m, 1H), 6.36 (d, 1H, J = 8.1 Hz), 6.43 (d, 1H, J = 6.9 Hz), 6.80 (d, 1H, J = 7.5 Hz) , 6.86 (t, 1H, J = 5.4 Hz), 7.34 (t, 1H, J = 8.4 Hz)

Compound Ij-28

¹H-NMR ((DMSO-d₆) δ: 0.93-1.18 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.75-1.86 (m, 2H), 1.94-2.05 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 3.09-3.27 (m, 2H), 6.19 (d, 1H, J = 8.1 Hz), 6.64 (d, 2H, J = 8.7 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.33 (d, 2H, J = 8.7 Hz) Mass: 379 [M + H]⁺

Compound Ij-29

¹H-NMR (DMSO-d₆) δ: 0.93-1.18 (m, 4H), 1.22 (s, 3H), 1.24 (s, 3H), 1.32-1.49 (m, 2H), 1.82 (d, 2H, J = 11.2 Hz), 2.04 (d , 2H, J = 11.2 Hz), 2.75-2.87 (m, 2H), 3.07-3.28 (m, 2H), 6.64 (s, 1H), 6.96 (s, 1H), 7.10-7.22 (m, 2H), 7.25-7.39 (m, 2H), 7.77-7.90 (m, 2H), 8.63 (s, 1H). Melting point: 161-162 ° C

Compound Ij-30

¹H-NMR (DMSO-d₆) δ: 0.92-1.22 (m, 4H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.86 (m, 2H), 1.94-2.05 (m, 2H), 2.88 (t, 2H, J = 6.3 Hz), 3.19 (m, 1H), 6.19 (d, 1H, J = 7.5 Hz), 6.64 (d, 2H, J = 8.7 Hz), 6.88 (d, 1H, J = 6.0 Hz), 7.33 (d, 2H, J = 8.7 Hz) Mass: 392M +

Compound Ij-31

¹H-NMR (DMSO-d₆) δ: 0.92-1.16 (m, 4H), 1.26 (s, 9H), 1,36 (m, 1H), 1.72-1.83 (m, 2H), 1.92-2.02 (m, 2H), 2.87 (t, 2H, J = 6.3 Hz), 3.12 (m, 1H), 6.09-6.23 (m, 4H), 6.87 (t, 1H, J = 6.0 Hz) Mass: 361 [M + H]⁺

Compound Ij-32

¹H-NMR (CDCl_Three) δ: 1.00-1.20 (m, 4H), 1.40 (s, 9H), 1.42-1.64 (m, 2H), 1.84-1.95 (m, 2H), 2.09-2.20 (m, 2H), 3.07 (m, 1H), 3.07 (t, 2H, J = 6.3 Hz), 3.90 (m, 1H), 6.10 (dd, 2H, J = 9.6, 5.4 Hz).

Compound Ij-33

¹H-NMR (DMSO-d₆) δ: 0.93-1.21 (m, 5H), 1.28 (s, 9H), 1.33-1.46 (m, 1H), 1.82 (d, 2H, J = 11.6 Hz), 2.04 (d, 2H, J = 11.6 Hz) ), 2.86-2.95 (m, 2H), 3.03-3.29 (m, 1H), 6.59-6.71 (m, 1H), 6.80-6.92 (m, 1H), 7.09-7.21 (m, 2H), 7.27-7.37 (m, 2H), 7.77-7.88 (m, 2H), 8.58-8.67 (s, 1H). Melting point: 172-273 ° C

Compound Ij-34

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24 (m, 2H), 1.21 (d, 6H, J = 6.4 Hz), 1.38 (m, 1H), 1.76-1.86 (m, 2H), 1.92 -2.00 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.48-3.60 (m, 1H), 6.95 (t, 1H, J = 5.6 Hz), 7.41 (d, 1H, J = 7.6 Hz), 7.63 (s, 1H), 7.82 (s, 1H).

Compound Ij-35

¹H-NMR (DMSO-d₆) δ: 0.96-1.26 (m, 4H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.88 (m, 2H), 1.92-2.02 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.48-3.62 (m, 1H), 6.87 (t, 1H, J = 6.0 Hz), 7.45 (d, 1H, J = 7.5 Hz), 7.63 (s, 1H), 7.82 (s, 1H)

Compound Ij-36

¹H-NMR (DMSO-d₆) δ: 0.96-1.06 (m, 2H), 1.12-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.39 (m, 1H), 1.78-1.84 (m, 2H), 1.95 -1.99 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.10-3.20 (m, 1H), 3.74-3.88 (m, 1H), 6.80 (s, 1H), 6.98 (t, 1H , J = 6.0 Hz), 7.93 (d, 2H, J = 7.2 Hz), 8.53 (s, 1H).

Compound Ij-37

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.93 (d, 1H, J = 7.5 Hz), 7.04 (t, 1H, J = 5.7 Hz), 7.26-7.38 (m, 2H), 7.40-7.52 (m, 1H), 7.57 (d, 1H, J = 9.0 Hz), 7.85 ( (t, 1H, J = 7.8 Hz)

Compound Ij-38

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 3.80 (s, 3H), 6.72 (d, 1H, J = 7.8 Hz) , 6.77 (d, 1H, J = 9.0 Hz), 6.98-7.10 (m, 2H), 7.12 (d, 1H, J = 8.4 Hz), 7.38 (t, 1H, J = 8.1 Hz), 7.56 (d, 1H, J = 9.3 Hz), 7.61 (d, 1H, J = 7.8 Hz)

Compound Ij-39

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.72-3.90 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.92 (d, 1H, J = 7.5 Hz), 7.04 (t, 1H, J = 5.7 Hz), 7.21 (t, 1H, J = 8.7 Hz), 7.46-7.56 (m, 1H), 7.75-7.88 (m, 3H)

Compound Ij-40

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.15-1.26 (m, 2H), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04 -2.14 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.76-3.87 (m, 1H), 6.85 (d, 1H, J = 9.6 Hz), 6.91 (d, 1H, J = 7.5 Hz), 7.01 (t, 1H, J = 5.7 Hz), 7.42-7.52 (m, 2H), 7.83 (d, 1H, J = 8.0 Hz), 7.93 ( d, 1H, J = 8.0 Hz), 8.02 (s, 1H).

Compound Ij-41

¹H-NMR (DMSO-d₆) δ: 0.96-1.30 (m, 4H), 1.20 (t, 3H, J = 7.5 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.76-3.90 (m, 1H), 6.88 (d, 1H, J = 9.3 Hz), 6.97 (d, 1H, J = 7.5 Hz), 7.03 (t, 1H, J = 5.7 Hz), 7.67-7.77 (m, 2H), 7.92 (d, 1H, J = 9.6 Hz), 8.26 (d, 1H, J = 6.9 Hz) , 8.33 (s, 1H)

Compound Ij-42

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.20 (t, 3H, J = 7.2 Hz), 1.22-1.28 (m, 1H), 1.35-1.50 (m, 2H), 1.84 (d, 2H, J = 12.0 Hz), 2.08 (d, 2H, J = 12.0 Hz), 2.63-2.76 (m, 2H), 2.91-3.03 (m, 2H), 3.75-3.90 (m, 1H), 6.86 (d, 1H, J = 9.2 Hz), 6.93 (d, 1H, J = 7.2 Hz), 6.98-7.07 (m, 1H), 7.36 (d, 1H, J = 7.2 Hz), 7.59 (t, 1H, J = 8.0 Hz), 7.85 (d, 1H, J = 9.2 Hz), 7.91-8.02 (m, 2H). Melting point: 144-145 ° C

Compound Ij-43

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.10-1.24 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.98 -2.06 (m, 2H), 2.81 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.62-3.74 (m, 1H), 6.84 (d, 1H, J = 9.2 Hz), 6.88-6.98 (m, 2H), 7.31 (d, 1H, J = 9.6 Hz).

Compound Ij-44

¹H-NMR (DMSO-d₆) δ: 0.94-1.26 (m, 4H), 1.20 (d, 6H, J = 6.6 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.06-3.20 (m, 1H), 3.72-3.90 (m, 1H), 6.75-6.88 (m, 2H), 6.97 (t, 1H, J = 6.0 Hz), 7.30-7.48 (m, 3H), 7.76 (d, 1H, J = 9.3 Hz), 7.94 (d, 2H, J = 8.4 Hz)

Compound Ij-45

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.85 (d, 1H, J = 9.0 Hz), 6.91 (d, 1H, J = 7.5 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.25-7.36 (m, 2H), 7.40-7.50 (m, 1H), 7.57 (d, 1H, J = 6.9 Hz), 7.85 (t, 1H , J = 8.1 Hz)

Compound Ij-46

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.85 (d, 1H, J = 9.3 Hz), 6.90 (d, 1H, J = 7.5 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.21 (t, 1H, J = 7.8 Hz), 7.46-7.56 (m, 1H), 7.75-7.86 (m, 3H)

Compound Ij-47

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 6.81 (d, 1H, J = 7.5 Hz), 6.84 (d, 1H, J = 9.3 Hz), 6.98 (t, 1H, J = 6.3 Hz), 7.25-7.35 (m, 2H), 7.77 (d, 1H, J = 9.3 Hz), 7.96-8.06 (m, 2H)

Compound Ij-48

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.80 (s, 3H), 6.71 (d, 1H, J = 7.8 Hz), 6.76 ( d, 1H, J = 9.3 Hz), 6.98 (t, 1H, J = 5.7 Hz), 7.05 (d, 1H, J = 7.2 Hz), 7.12 (d, 1H, J = 7.8 Hz), 7.38 (t, 1H, J = 8.4 Hz), 7.56 (d, 1H, J = 9.3 Hz), 7.62 (d, 1H, J = 6.9 Hz)

Compound Ij-49

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.6 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.82 (s, 3H), 6.78-6.88 (m, 2H), 6.92-7.04 (m , 2H), 7.37 (t, 1H, J = 7.5 Hz), 7.46-7.58 (m, 2H), 7.79 (d, 1H, J = 9.3 Hz)

Compound Ij-50

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.22 (d, 6H, J = 6.9 Hz), 1.42 (m, 1H), 1.78-1.88 (m, 2H), 2.04-2.16 (m, 2H), 2.83 (t, 2H, J = 6.0 Hz), 3.10-3.22 (m, 1H), 3.74-3.92 (m, 1H), 3.80 (s, 3H), 6.70 (d, 1H, J = 7.8 Hz), 6.82 ( d, 1H, J = 9.3 Hz), 6.95-7.05 (m, 3H), 7.72 (d, 1H, J = 9.3 Hz), 7.90 (d, 2H, J = 9.0 Hz).

Compound Ij-51

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.07-1.20 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.76-1.85 (m, 2H), 2.02 -2.10 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.57-3.68 (m, 1H), 4.89-4.98 (m, 2H), 6.47 (d , 1H, J = 8.0 Hz), 6.88 (d, 1H, J = 7.5 Hz), 6.96 (t, 1H, J = 6.0 Hz), 7.02 (d, 1H, J = 7.5 Hz).

Compound Ij-52

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.07-1.20 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.52-1.74 (m, 6H), 1.77 -1.85 (m, 2H), 1.87-1.97 (m, 2H), 2.02-2.09 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.55-3.65 (m, 1H), 5.25-5.32 (m, 1H), 6.19 (d, 1H, J = 8.0 Hz), 6.77 (s, 2H), 6.95 (t, 1H, J = 6.0 Hz).

Compound Ij-53

¹H-NMR (DMSO-d₆) δ: 0.92-1.15 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 1.88-1.95 (m, 4H), 2.02 -2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.25-3.35 (m, 4H), 3.55-3.65 (m, 1H), 5.80-5.85 (m, 1H), 6.72 (d, 1H, J = 8.0 Hz), 6.80 (d, 1H, J = 8.0 Hz), 6.96 (t, 1H, J = 6.0 Hz).

Compound Ij-54

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 6.56 (d, 1H, J = 8.0 Hz), 6.90-6.98 (m, 2H), 7.03-7.10 (m, 3H), 7.15 (t, 1H, J = 8.0 Hz), 6.38 (t, 2H, J = 8.0 Hz).

Compound Ij-55

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.90-6.98 (m, 2H), 7.05-7.15 (m, 3H), 7.21 (t, 2H, J = 8.0 Hz).

Compound Ij-56

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 2.02-2.09 (m, 2H), 2.80 (t, 2H, J = 6.3 Hz), 3.09-3.20 (m, 1H), 3.58-3.65 (m, 1H), 3.75 (s, 3H), 6.49 (d, 1H, J = 8.0 Hz), 6.87- 6.98 (m, 4H), 7.00-7.07 (m, 3H).

Compound Ij-57

¹H-NMR (DMSO-d₆) δ: 0.96-1.28 (m, 4H), 1.27 (s, 9H), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.00-2.10 (m, 2H), 2.88 (t, 2H, J = 6.0 Hz), 3.60-3.76 (m, 1H), 6.82-6.92 (m, 2H), 6.96 (d, 1H, J = 7.8 Hz), 7.32 (d, 1H, J = 9.6 Hz).

Compound Ij-58

¹H-NMR (DMSO-d₆) δ: 0.99-1.28 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.39 (m, 1H), 1.78-1.86 (m, 2H), 2.04-2.10 (m, 2H), 2.82 (t, 2H, J = 6.1 Hz), 3.06-3.20 (m, 1H), 3.80-3.96 (m, 1H), 6.71 (d, 1H, J = 9.0 Hz), 6.76-6.86 (m, 1H), 6.90-6.98 (m, 1H), 7.10 (t, 1H, J = 8.1 Hz), 7.39-7.50 (m, 2H), 7.56 (d, 1H, J = 7.5 Hz), 7.78 (d, 1H, J = 7.5 Hz).

Compound Ij-59

¹H-NMR (DMSO-d₆) δ: 0.99-1.28 (m, 4H), 1.27 (s, 9H), 1.40 (m, 1H), 1.80-1.85 (m, 2H), 2.04-2.09 (m, 2H), 2.91 (t, 2H, J = 6.1 Hz), 3.80-3.96 (m, 1H), 6.70 (d, 1H, J = 9.0 Hz), 6.81-6.87 (m, 2H), 7.10 (t, 1H, J = 8.1 Hz), 7.39- 7.44 (m, 2H), 7.56 (d, 1H, J = 7.5 Hz), 7.79 (d, 1H, J = 7.5 Hz).

Compound Ij-60

¹H-NMR (DMSO-d₆) δ: 0.97-1.09 (m, 2H), 1.23 (d, 6H, J = 6.9 Hz), 1.31-1.50 (m, 2H), 1.82-1.87 (m, 2H), 2.01-2.05 (m, 2H) , 2.83 (t, 2H, J = 6.0 Hz), 3.11-3.20 (m, 1H), 4.00-4.18 (m, 1H), 6.83 (d, 1H, J = 5.7 Hz), 6.90-7.06 (m, 2H ), 7.45 (t, 1H, J = 6.9 Hz), 7.59 (t, 1H, J = 8.1 Hz), 7.67 (d, 1H, J = 8.4 Hz), 7.83 (d, 1H, J = 5.7 Hz), 8.27 (d, 1H, J = 7.5 Hz).

Compound Ij-61

¹H-NMR (DMSO-d₆) δ: 0.96-1.09 (m, 2H), 1.28 (s, 9H), 1.29-1.50 (m, 2H), 1.82-1.87 (m, 2H), 2.01-2.05 (m, 2H), 2.91 (t, 2H, J = 7.8 Hz), 4.00-4.18 (m, 1H), 6.82-6.89 (m, 2H), 6.97 (d, 1H, J = 7.5 Hz), 7.45 (t, 1H, J = 7.2 Hz), 7.59 (t, 1H, J = 8.1 Hz), 7.67 (d, 1H, J = 7.8 Hz), 7.84 (d, 1H, J = 6.0 Hz), 8.27 (d, 1H, J = 8.4 Hz).

Compound Ij-62

¹H-NMR (DMSO-d₆) δ: 0.96-1.14 (m, 2H), 1.18-1.30 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.40 (m, 1H), 1.78-1.88 (m, 2H), 2.04 -2.14 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.58-3.70 (m, 1H), 6.95-7.03 (m, 2H), 7.20 (t , 1H, J = 7.5 Hz), 7.37 (d, 1H, J = 8.1 Hz), 7.64 (d, 1H, J = 7.5 Hz), 7.92 (d, 1H, J = 7.8 Hz).

Compound Ij-63

¹H-NMR (DMSO-d₆) δ: 1.00 (dd, 2H, J = 24.8, 10.6 Hz), 1.15-1.22 (m, 2H), 1.18 (t, 3H, J = 7.6 Hz), 1.27 (s, 9H), 1.34-1.40 (m , 1H), 1.81 (d, 2H, J = 11.6 Hz), 2.07 (d, 2H, J = 11.6 Hz), 2.60 (q, 2H, J = 7.6 Hz), 2.89 (t, 2H, J = 6.3 Hz ), 3.52-3.63 (m, 1H), 6.87 (t, 1H, J = 5.8 Hz), 7.04 (d, 1H, J = 7.9 Hz), 7.27 (d, 1H, J = 8.2 Hz), 7.47 (s , 1H), 7.80 (d, 1H, J = 7.6 Hz).

Compound Ij-64

¹H-NMR (DMSO-d₆) δ: 0.92-1.10 (m, 2H), 1.12-1.25 (m, 2H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.89 (t, 2H, J = 6.0 Hz), 3.50-3.66 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.03 (dd, 1H, J = 8.7, 2.7 Hz), 7.32-7.37 (m, 1H), 7.58 (dd, 1H, J = 8.7, 2.7 Hz), 7.92 (d, 1H, J = 7.2 Hz).

Compound Ij-65

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 24.6, 10.2 Hz), 1.21 (dd, 2H, J = 24.6, 10.2 Hz), 1.27 (s, 9H), 1.34-1.40 (m, 1H), 1.82 (d , 2H, J = 11.2 Hz), 2.08 (d, 2H, J = 11.2 Hz), 2.89 (t, 2H, J = 6.2 Hz), 3.59-3.65 (m, 1H), 6.87 (t, 1H, J = 5.8 Hz), 7.21 (dd, 1H, J = 8.6, 2.4 Hz), 7.34 (d, 1H, J = 8.6 Hz), 7.77 (d, 1H, J = 1.8 Hz), 8.06 (d, 1H, J = (7.6 Hz).

Compound Ij-66

¹H-NMR (CDCl_Three) δ: 1.09-1.46 (m, 4H), 1.41 (s, 9H), 1.54 (m, 1H), 1.90-2.00 (m, 2H), 2.24-2.34 (m, 2H), 3.09 (t, 2H, J = 6.6 Hz), 3.46-3.60 (m, 1H), 3.99 (t, 1H, J = 6.6 Hz), 6.58 (brs, 1H), 7.58 (s, 2H), 7.85 (s, 1H).

Compound Ij-67

¹H-NMR (DMSO-d₆) δ: 0.90-1.30 (m, 4H), 1.27 (s, 9H), 1.30-1.48 (m, 1H), 1.82 (d, 2H, J = 11.1 Hz), 2.08 (d, 2H, J = 9.6 Hz) ), 2.89 (t, 2H, J = 6.3 Hz), 3.55-3.70 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.17 (m, 1H), 7.41 (d, 1H, J = 8.7 Hz), 7.77 (d, 1H, J = 1.5 Hz), 8.10 (d, 1H, J = 7.5 Hz). ESI (positive) m / z 466.2 [M + H] +

Compound Ij-68

¹H-NMR (DMSO-d₆) δ: 0.90-1.28 (m, 4H), 1.25 (s, 9H), 1.32 (m, 1H), 1.76-1.82 (m, 2H), 2.00-2.10 (m, 2H), 2.87 (t, 2H, J = 6.6 Hz), 3.50-3.62 (m, 1H), 3.71 (s, 3H), 6.77 (dd, 1H, J = 8.7, 2.7 Hz), 6.84 (t, 1H, J = 5.7 Hz), 7.22- 7.28 (m, 2H), 7.66 (d, 1H, J = 7.2 Hz).

Compound Ij-69

¹H-NMR (DMSO-d₆) δ: 0.94-1.10 (m, 2H), 1.12-1.25 (m, 2H), 1.27 (s, 9H), 1.37 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H), 2.90 (t, 2H, J = 6.0 Hz), 3.52-3.68 (m, 1H), 3.84 (s, 3H), 6.82 (d, 1H, J = 8.1 Hz), 6.88 (t, 1H, J = 5.4 Hz), 6.95 (t, 1H, J = 7.8 Hz), 7.23 (d, 1H, J = 7.8 Hz), 7.83 (d, 1H, J = 7.8 Hz).

Compound Ij-70

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.17-1.32 (m, 2H), 1.40 (m, 1H), 1.76-1.88 (m, 2H), 2.04 -2.14 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.78 (m, 1H), 7.03 (t, 1H, J = 6.3 Hz), 7.45-7.54 (m, 2H), 8.10 (s, 1H), 8.34 (d, 1H, J = 7.2 Hz).

Compound Ij-71

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 26.1, 12.3 Hz), 1.16-1.22 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.35-1.41 (m, 1H), 1.70-1.77 (m, 1H), 1.82 (d, 2H, J = 11.6 Hz), 2.08 (d, 2H, J = 11.6 Hz), 2.81 (t, 2H, J = 6.3 Hz), 3.66-3.72 (m, 1H) , 6.99 (t, 1H, J = 6.3 Hz), 7.23 (dd, 1H, J = 8.1, 4.7 Hz), 7.66 (d, 1H, J = 8.1 Hz), 8.07 (d, 1H, J = 4.7 Hz) , 8.26 (d, 1H, J = 6.3 Hz).

Compound Ij-72

¹H-NMR (DMSO-d₆) δ: 1.01 (dd, 2H, J = 24.8, 11.3 Hz), 1.18-1.23 (m, 2H), 1.27 (s, 9H), 1.36-1.39 (m, 1H), 1.82 (d, 2H, J = 11.5 Hz), 2.08 (d, 2H, J = 11.5 Hz), 2.89 (t, 2H, J = 6.1 Hz), 3.65-3.73 (m, 1H), 6.87 (t, 1H, J = 5.7 Hz), 7.23 (dd, 1H, J = 8.1, 4.8 Hz), 7.66 (d, 1H, J = 7.9 Hz), 8.07 (d, 1H, J = 4.7 Hz), 8.26 (d, 1H, J = 7.6 Hz).

Compound Ij-73

¹H-NMR (CDCl_Three) δ: 1.09-1.46 (m, 4H), 1.41 (s, 9H), 1.55 (m, 1H), 1.92-2.02 (m, 2H), 2.24-2.34 (m, 2H), 3.09 (t, 2H, J = 6.3 Hz), 3.58-3.72 (m, 1H), 3.98 (t, 1H, J = 6.0 Hz), 6.30 (brs, 1H), 7.62 (d, 1H, J = 8.1 Hz), 7.77 (d, 1H, J = 8.4 Hz).

Compound Ij-74

¹H-NMR (DMSO-d₆) δ: 0.90-1.08 (m, 2H), 1.12-1.40 (m, 3H), 1.25 (s, 9H), 1.76-1.86 (m, 2H), 1.98-2.10 (m, 2H), 2.87 (d, 2H, J = 6.3 Hz), 3.40-3.56 (m, 1H), 6.85 (brs, 1H), 6.93 (t, 1H, J = 7.5 Hz), 7.07 (t, 1H, J = 7.5 Hz), 7.20 ( d, 1H, J = 7.5 Hz), 7.29 (d, 1H, J = 7.8 Hz), 7.79 (brs, 1H).

Compound Ij-75

¹H-NMR (CDCl_Three) δ: 1.08-1.26 (m, 2H), 1.36-1.60 (m, 3H), 1.40 (s, 9H), 1.92-2.02 (m, 2H), 2.22-2.32 (m, 2H), 3.08 (t, 2H, J = 6.6 Hz), 3.68-3.80 (m, 1H), 4.03 (t, 1H, J = 6.0 Hz), 7.06 (brs, 1H), 7.20-7.36 (m, 3H).

Compound Ij-76

¹H-NMR (DMSO-d₆) δ: 1.02 (dd, 2H, J = 25.2, 12.4 Hz), 1.17 (t, 3H, J = 7.1 Hz), 1.20 (t, 3H, J = 7.3 Hz), 1.26-1.35 (m, 2H), 1.37-1.42 (m, 1H), 1.83 (d, 2H, J = 11.6 Hz), 2.05 (d, 2H, J = 11.6 Hz), 2.80 (t, 2H, J = 6.4 Hz), 2.99 (q, 2H , J = 7.3 Hz), 3.65-3.72 (m, 1H), 4.01 (q, 2H, J = 7.1 Hz), 6.32 (d, 1H, J = 7.9 Hz), 6.86-6.94 (m, 2H), 7.01 (t, 1H, J = 6.0 Hz), 7.12 (d, 1H, J = 6.9 Hz), 7.17 (d, 1H, J = 6.8 Hz).

Compound Ij-77

¹H-NMR (DMSO-d₆) δ: 1.02 (dd, 2H, J = 24.8, 10.8 Hz), 1.19-1.21 (m, 2H), 1.30 (s, 9H), 1.37-1.41 (m, 1H), 1.84 (d, 2H, J = 10.6 Hz), 2.06 (d, 2H, J = 10.6 Hz), 2.92 (t, 2H, J = 6.3 Hz), 3.50-3.52 (m, 1H), 6.42 (d, 1H, J = 8.1 Hz), 6.83 (d, 1H, J = 7.9 Hz), 6.88-6.92 (m, 2H), 7.11-7.14 (m, 2H), 10.58 (s, 1H).

Compound Ij-78

¹H-NMR (DMSO-d₆) δ: 0.97-1.05 (m, 2H), 1.20-1.26 (m, 2H), 1.28 (s, 9H), 1.34-1.38 (m, 1H), 1.84 (d, 2H, J = 11.5 Hz), 2.07 (d, 2H, J = 11.5 Hz), 2.90 (t, 2H, J = 6.1 Hz), 3.47 (s, 3H), 3.63-3.69 (m, 1H), 6.34 (d, 1H, J = 7.6 Hz) , 6.87-6.93 (m, 3H), 7.11 (d, 1H, J = 8.4 Hz), 7.17 (d, 1H, J = 8.4 Hz).

Compound Ij-79

¹H-NMR (DMSO-d₆) δ: 1.03 (dd, 2H, J = 23.6, 10.8 Hz), 1.18 (t, 3H, J = 7.5 Hz), 1.25-1.34 (m, 2H), 1.29 (s, 9H), 1.37-1.40 (m , 1H), 1.86 (d, 2H, J = 11.7 Hz), 2.07 (d, 2H, J = 11.7 Hz), 2.92 (t, 2H, J = 6.2 Hz), 3.67-3.73 (m, 1H), 4.03 (q, 2H, J = 7.1 Hz), 6.34 (d, 1H, J = 7.9 Hz), 6.87-6.96 (m, 3H), 7.14 (dd, 1H, J = 8.1, 1.2 Hz), 7.19 (dd, 1H, J = 8.1, 1.2 Hz).

Compound Ij-80

¹H-NMR (DMSO-d₆) δ: 1.00 (dd, 2H, J = 23.2, 11.9 Hz), 1.19-1.25 (m, 2H), 1.28 (s, 9H), 1.33-1.38 (m, 1H), 1.45 (s, 3H), 1.47 (s, 3H), 1.83 (d, 2H, J = 11.1 Hz), 2.07 (d, 2H, J = 11.1 Hz), 2.90 (t, 2H, J = 6.1 Hz), 3.62-3.70 (m, 1H) , 4.57-4.66 (m, 1H), 6.21 (d, 1H, J = 7.9 Hz), 6.82-6.94 (m, 3H), 7.18 (d, 1H, J = 7.6 Hz), 7.31 (d, 1H, J = 7.6 Hz).

Compound Ij-81

Compound Ij-82

¹H-NMR (DMSO-d₆) δ: 0.90-1.19 (m, 4H), 1.28 (s, 9H), 1.32-1.45 (m, 1H), 1.80 (d, 2H, J = 11.2 Hz), 1.98 (d, 2H, J = 11.2 Hz) ), 2.84-2.93 (m, 2H), 3.26 (s, 3H), 3.40-3.53 (m, 1H), 6.29 (d, 1H, J = 8.0 Hz), 6.38 (d, 1H, J = 7.2 Hz) , 6.86 (s, 1H), 7.33 (d, 1H, J = 8.4 Hz).

Compound Ij-83

Compound Ij-84

¹H-NMR (DMSO-d₆) δ: 0.92-1.20 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.75-1.85 (m, 2H), 1.96-2.06 (m, 2H), 2.78 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.78 (m, 1H), 6.38 (d, 1H, J = 8.1 Hz), 6.67 (s, 1H) , 6.72 (d, 1H, J = 5.4 Hz), 7.00 (t, 1H, J = 6.0 Hz), 7.36-7.54 (m, 3H), 7.62 (d, 2H, J = 6.9 Hz), 8.00 (d, (1H, J = 5.4 Hz)

Compound Ij-85

¹H-NMR (DMSO-d₆) δ: 1.00-1.20 (m, 4H), 1.20 (t, 3H, J = 7.2 Hz), 1.43 (m, 1H), 1.80-1.88 (m, 2H), 2.03-2.13 (m, 2H), 2.81 (t, 3H, J = 6.0 Hz), 3.00 (q, 2H, J = 7.2 Hz), 3.26 (m, 1H), 6.17 (d, 1H, J = 7.6 Hz), 6.57 (s, 1H), 6.96 -7.07 (m, 2H), 7.35 (dd, 1H, J = 8.4, 4.0 Hz), 8.02 (d, 1H, J = 8.4 Hz), 8.47 (d, 1H, J = 4.0 Hz).

Compound Ij-86

¹H-NMR (DMSO-d₆) δ: 1.00-1.24 (m, 4H), 1.23 (d, 6H, J = 6.4 Hz), 1.42 (m, 1H), 1.80-1.88 (m, 2H), 2.03-2.12 (m, 2H), 2.79 -2.87 (m, 2H), 3.16 (m, 1H), 3.27 (m, 1H), 6.17 (d, 1H, J = 8.0 Hz), 6.57 (s, 1H), 6.99 (d, 1H, J = 8.0 Hz), 7.01 (s, 1H), 7.35 (dd, 1H, J = 8.0, 4.0 Hz), 8.02 (d, 1H, J = 8.0 Hz), 8.47 (d, 1H, J = 2.8 Hz).

Compound Ij-87

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.11-1.25 (m, 2H), 1.20 (t, 3H, J = 7.2 Hz), 1.40 (m, 1H), 1.76-1.86 (m, 2H), 1.97 -2.04 (m, 2H), 2.73-2.82 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.70 (m, 1H), 6.53 (d, 1H, J = 8.8 Hz), 6.53 ( d, 1H, J = 8.8 Hz), 7.01 (t, 1H, J = 6.0 Hz), 7.58 (d, 1H, J = 3.2 Hz), 7.79 (d, 1H, J = 3.2 Hz), 7.86 (d, 1H, J = 8.8 Hz), 8.55 (s, 1H).

Compound Ij-88

¹H-NMR (DMSO-d₆) δ: 0.92-1.07 (m, 2H), 1.09-1.20 (m, 2H), 1.19 (t, 6H, J = 7.2 Hz), 1.39 (m, 1H), 1.75-1.83 (m, 2H), 1.95 -2.03 (m, 2H), 2.74-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.66 (m, 1H), 6.48 (d, 1H, J = 8.4 Hz), 6.60 ( d, 1H, J = 7.6 Hz), 7.00 (t, 1H, J = 5.6 Hz), 7.06 (dd, 1H, J = 4.8, 2.4 Hz), 7.25 (d, 1H, J = 2.4 Hz), 7.37 ( d, 1H, J = 4.8 Hz), 7.60 (dd, 1H, J = 8.4, 2.0 Hz), 8.26 (s, 1H).

Compound Ij-89

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.10-1.20 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.76-1.84 (m, 2H), 1.96 -2.04 (m, 2H), 2.73-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.65 (m, 1H), 6.41-6.50 (m, 2H), 7.01 (t, 1H , J = 6.0 Hz), 7.44 (d, 1H, J = 4.0 Hz), 7.58 (m, 1H), 7.59 (s, 1H), 7.68 (d, 1H, J = 8.0 Hz), 8.34 (s, 1H ).

Compound Ij-90

¹H-NMR (DMSO-d₆) δ: 0.95-1.08 (m, 2H), 1.12-1.25 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.76-1.86 (m, 2H), 1.94 -2.03 (m, 2H), 2.75-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.71 (m, 1H), 6.54 (d, 1H, J = 8.8 Hz), 6.98- 7.07 (m, 2H), 7.25 (s, 1H), 7.85 (dd, 1H, J = 8.8, 2.0 Hz), 8.07 (s, 1H), 8.56 (d, 1H, J = 2.0 Hz).

Compound Ij-91

¹H-NMR (DMSO-d₆) δ: 0.93-1.07 (m, 2H), 1.11-1.22 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.38 (m, 1H), 1.77-1.85 (m, 2H), 1.95 -2.03 (m, 2H), 2.77-2.83 (m, 2H), 3.14 (m, 1H), 3.72 (m, 1H), 6.53 (d, 1H, J = 8.8 Hz), 6.97 (t, 1H, J = 6.0 Hz), 7.02 (d, 1H, J = 7.6 Hz), 7.25 (s, 1H), 7.84 (dd, 1H, J = 8.8, 2.0 Hz), 8.06 (s, 1H), 8.56 (d, 1H , J = 2.0 Hz).

Compound Ij-92

¹H-NMR (DMSO-d₆) δ: 0.92-1.03 (m, 2H), 1.11-1.23 (m, 2H), 1.21 (d, 6H, J = 6.8 Hz), 1.37 (m, 1H), 1.75-1.83 (m, 2H), 1.91 -1.99 (m, 2H), 2.36-2.42 (m, 2H), 3.12 (m, 1H), 3.70 (m, 1H), 6.49 (d, 1H, J = 9.2 Hz), 6.97 (t, 1H, J = 6.0 Hz), 7.47 (d, 1H, J = 8.0 Hz), 7.62 (d, 1H, J = 8.0 Hz), 8.36 (s, 1H).

Compound Ij-93

¹H-NMR (DMSO-d₆) δ: 0.95-1.13 (m, 4H), 1.23 (d, 6H, J = 6.9 Hz), 1.31-1.44 (m, 1H), 1.78-1.82 (m, 2H), 2.03-2.06 (m, 2H) , 2.76-2.82 (m, 2H), 3.10-3.19 (m, 1H), 3.20-3.25 (m, 4H), 3.58-3.65 (m, 1H), 3.69-3.74 (m, 4H), 6.04 (d, 1H, J = 7.5 Hz), 6.72 (d, 1H, J = 9.6 Hz), 6.95-6.99 (m, 1H), 7.10 (d, 1H, J = 9.6 Hz).

Compound Ij-94

¹H-NMR (DMSO-d₆) δ: 0.96-1.42 (m, 5H), 1.22 (d, 6H, J = 6.9 Hz), 1.79-1.83 (m, 2H), 2.03-2.07 (m, 2H), 2.80 (d, 2H, J = 6.3 Hz), 3.10-3.19 (m, 1H), 3.54-3.70 (m, 1H), 3.74 (s, 3H), 6.57-6.64 (m, 3H), 6.72-6.75 (m, 1H), 6.90-7.09 (m, 3H), 7.24-7.30 (m, 1H).

Compound Ij-95

¹H-NMR (DMSO-d₆) δ: 0.93-1.04 (m, 2H), 1.10-1.18 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.34-1.44 (m, 1H), 1.78-1.87 (m, 2H) , 2.02-2.12 (m, 2H), 2.77-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.52-3.70 (m, 1H), 6.64 (d, 1H, J = 8.0 Hz), 6.88 -7.06 (m, 5H), 7.12 (d, 1H, J = 8.0 Hz), 7.37-7.46 (m, 1H).

Compound Ij-96

¹H-NMR (DMSO-d₆) δ: 0.90-1.04 (m, 2H), 1.05-1.18 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.84 (m, 2H) , 1.98-2.08 (m, 2H), 2.76-2.84 (m, 2H), 3.08-3.18 (m, 1H), 3.52-3.64 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.91 -7.00 (m, 2H), 7.15-7.38 (m, 5H).

Compound Ij-97

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.25 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.35-1.47 (m, 1H), 1.78-1.87 (m, 2H) , 2.02-2.10 (m, 2H), 2.78-2.83 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.70-3.82 (m, 1H), 6.82 (d, 1H, J = 8.0 Hz ), 6.93 (d, 1H, J = 8.0 Hz), 7.01 (t, 1H, J = 4.5 Hz), 7.13 (d, 1H, J = 4.0 Hz), 7.43 (d, 1H, J = 4.0 Hz), 7.76 (d, 1H, J = 8.0 Hz).

Compound Ij-98

¹H-NMR (DMSO-d₆) δ: 0.97-1.10 (m, 2H), 1.17-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.49 (m, 1H), 1.80-1.88 (m, 2H) , 2.04-2.12 (m, 2H), 2.77-2.83 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.88 (m, 1H), 6.85 (d, 1H, J = 8.0 Hz ), 6.99-7.05 (m, 2H), 7.61 (s, 1H), 7.90 (d, 1H, J = 8.0 Hz), 8.02 (s, 2H).

Compound Ij-99

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.14-1.26 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.48 (m, 1H), 1.80-1.88 (m, 2H) , 2.04-2.13 (m, 2H), 2.77-2.83 (m, 2H), 2.96 (s, 6H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.86 (m, 1H), 6.72-6.78 (m, 2H), 6.82 (d, 1H, J = 8.0 Hz), 7.02 (t, 1H, J = 4.5 Hz), 7.18 (d, 1H, J = 8.0 Hz), 7.26 (t, 1H, J = 8.0 Hz), 7.34 (s, 1H), 7.74 (d, 1H, J = 8.0 Hz).

Compound Ij-100

¹H-NMR (DMSO-d₆) δ: 0.98-1.10 (m, 2H), 1.16-1.27 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.37-1.48 (m, 1H), 1.80-1.88 (m, 2H) , 2.04-2.13 (m, 2H), 2.77-2.83 (m, 2H), 2.99 (q, 2H, J = 7.2 Hz), 3.76-3.86 (m, 1H), 6.83 (d, 1H, J = 8.0 Hz ), 6.89 (d, 1H, J = 8.0 Hz), 7.02 (t, 1H, J = 4.5 Hz), 7.42-7.50 (m, 3H), 7.53-7.59 (m, 2H).

Compound Ij-101

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.08-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.36-1.43 (m, 1H), 1.76-1.84 (m, 2H) , 2.02-2.09 (m, 2H), 2.77-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.56-3.68 (m, 1H), 6.62 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 6.98 (t, 1H, J = 4.5 Hz), 7.10-7.15 (m, 3H), 7.43 (d, 2H, J = 8.0 Hz).

Compound Ij-102

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.08-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.36-1.43 (m, 1H), 1.76-1.84 (m, 2H) , 2.02-2.09 (m, 2H), 2.77-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.57-3.68 (m, 1H), 6.65 (d, 1H, J = 8.0 Hz), 6.94 (d, 1H, J = 8.0 Hz), 6.97 (t, 1H, J = 4.5 Hz), 7.06 (d, 1H, J = 8.0 Hz), 7.13 (d, 1H, J = 8.0 Hz), 7.18-7.26 (m, 2H), 7.41 (t, 1H, J = 8.0 Hz).

Compound Ij-103

¹H-NMR (DMSO-d₆) δ: 0.88-1.04 (m, 2H), 1.05-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.77-1.82 (m, 2H) , 2.00-2.07 (m, 2H), 2.76-2.82 (m, 2H), 3.08-3.20 (m, 1H), 3.52-3.64 (m, 1H), 6.57 (d, 1H, J = 8.0 Hz), 6.92 -7.00 (m, 2H), 7.17 (d, 1H, J = 8.0 Hz), 7.23-7.28 (m, 2H), 7.38 (t, 1H, J = 8.0 Hz), 7.56 (d, 1H, J = 8.0 Hz).

Compound Ij-104

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.12-1.24 (m, 2H), 1.19 (t, 3H, J = 7.6 Hz), 1.35-1.46 (m, 1H), 1.78-1.86 (m, 2H) , 2.04-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.6 Hz), 3.67-3.78 (m, 1H), 6.27 (s, 2H), 6.71 (d , 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 7.02 (brs, 1H), 7.52 (s, 2H), 7.67 (d, 1H, J = 8.0 Hz).

Compound Ij-105

¹H-NMR (DMSO-d₆) δ: 0.96-1.08 (m, 2H), 1.13-1.25 (m, 2H), 1.19 (t, 3H, J = 7.6 Hz), 1.35-1.46 (m, 1H), 1.78-1.87 (m, 2H) , 2.04-2.12 (m, 2H), 2.76-2.83 (m, 2H), 2.99 (q, 2H, J = 7.6 Hz), 3.72-3.82 (m, 1H), 6.82 (d, 1H, J = 8.0 Hz ), 6.85 (d, 1H, J = 8.0 Hz), 7.03 (t, 1H, J = 4.5 Hz), 7.12 (t, 1H, J = 4.0 Hz), 7.51 (d, 1H, J = 4.0 Hz), 7.56 (d, 1H, J = 4.0 Hz), 7.76 (d, 1H, J = 8.0 Hz).

Compound Ij-106

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.45 (m, 1H), 1.76-1.85 (m, 2H) , 2.02-2.08 (m, 2H), 2.76-2.83 (m, 2H), 3.10-3.20 (m, 1H), 3.57-3.67 (m, 1H), 6.63 (d, 1H, J = 8.0 Hz), 6.92 -7.00 (m, 3H), 7.13 (d, 1H, J = 8.0 Hz), 7.29-7.36 (m, 1H), 7.42-7.50 (m, 1H).

Compound Ij-107

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.83 (m, 2H) , 1.98-2.06 (m, 2H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.52-3.63 (m, 1H), 6.57 (d, 1H, J = 8.0 Hz), 6.93 (d, 1H, J = 8.0 Hz), 6.97 (t, 1H, J = 4.5 Hz), 7.12 (t, 1H, J = 4.0 Hz), 7.19 (d, 1H, J = 8.0 Hz), 7.33-7.47 (m, 2H).

Compound Ij-108

¹H-NMR (DMSO-d₆) δ: 0.88-1.02 (m, 2H), 1.07-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.33-1.43 (m, 1H), 1.75-1.83 (m, 2H) , 1.98-2.07 (m, 2H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.54-3.63 (m, 1H), 6.63 (d, 1H, J = 8.0 Hz), 6.93 -7.00 (m, 2H), 7.14 (t, 1H, J = 8.0 Hz), 7.20-7.37 (m, 3H).

Compound Ij-109

¹H-NMR (DMSO-d₆) δ: 0.82-1.05 (m, 2H), 1.05-1.20 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.43 (m, 1H), 1.76-1.83 (m, 2H) , 2.00-2.08 (m, 2H), 2.29 (s, 3H), 2.76-2.83 (m, 2H), 3.08-3.18 (m, 1H), 3.56-3.66 (m, 1H), 6.55 (d, 1H, J = 8.0 Hz), 6.90 (d, 1H, J = 8.0 Hz), 6.93-7.00 (m, 3H), 7.05 (d, 1H, J = 8.0 Hz), 7.17 (d, 2H, J = 8.0 Hz) .

Compound Ij-110

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.28 (s, 9H), 1.32-1.43 (m, 1H), 1.80 (d, 2H, J = 12.0 Hz), 2.07 (d, 2H, J = 12.0 Hz) ), 2.88 (t, 2H, J = 6.4 Hz), 3.16-3.27 (m, 1H), 5.47 (d, 1H, J = 7.6 Hz), 5.80 (s, 1H), 6.83 (d, 1H, J = 6.0 Hz), 7.15-7.40 (m, 3H), 7.75 (t, 1H, J = 8.4 Hz), 7.86 (s, 1H).

Compound Ij-111

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.21 (d, 6H, J = 6.9 Hz), 1.32-1.43 (m, 1H), 1.76-1.82 (m, 2H), 2.02-2.12 (m, 2H) , 2.77-2.83 (m, 2H), 3.08-3.27 (m, 2H), 5.48 (d, 1H, J = 8.1 Hz), 5.80 (d, 1H, J = 2.7 Hz), 6.95 (t, 1H, J = 6.0 Hz), 7.15-7.39 (m, 3H), 7.75 (td, 1H, J = 8.4, 1.8 Hz), 7.86 (t, 1H, J = 2.7 Hz).

Compound Ij-112

¹H-NMR (DMSO-d₆) δ: 0.91-1.19 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.30-1.45 (m, 1H), 1.76-1.82 (m, 2H), 2.02-2.12 (m, 2H) , 2.77-2.83 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz) 3.10-3.30 (m, 1H), 5.48 (d, 1H, J = 7.8 Hz), 5.80 (d, 1H, J = 2.7 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.15-7.40 (m, 3H), 7.75 (td, 1H, J = 8.4, 1.8 Hz), 7.86 (t, 1H, J = 2.7 Hz) .

Compound Ij-113

Compound Ij-114

Compound Ij-115

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.30-1.45 (m, 1H), 1.76-1.84 (m, 2H), 2.02-2.12 (m, 2H) , 2.74-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz) 3.15-3.30 (m, 1H), 5.53 (d, 1H, J = 8.1 Hz), 5.80 (d, 1H, J = 2.4 Hz), 6.92 (t, 1H, J = 8.4 Hz), 7.01 (t, 1H, J = 6.0 Hz), 7.37-7.43 (m, 3H), 8.21 (d, 1H, J = 2.4 Hz).

Compound Ij-116

Compound Ij-117

Compound Ij-118

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.75-1.86 (m, 2H), 2.02-2.12 (m, 2H) , 2.74-2.83 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz) 3.13-3.30 (m, 1H), 5.38 (d, 1H, J = 8.4 Hz), 5.75 (d, 1H, J = 2.7 Hz), 6.99 (t, 1H, J = 6.3 Hz), 7.18-7.28 (m, 2H), 7.63-7.70 (m, 2H), 8.11 (d, 1H, J = 2.7 Hz).

Compound Ij-119

¹H-NMR (DMSO-d₆) δ: 0.88-1.19 (m, 4H), 1.18 (t, 3H, J = 7.5 Hz), 1.28-1.45 (m, 1H), 1.73-1.83 (m, 2H), 2.02-2.13 (m, 2H) , 2.73-2.81 (m, 2H), 2.95 (q, 2H, J = 7.5 Hz) 3.12-3.30 (m, 1H), 5.36 (d, 1H, J = 7.5 Hz), 5.76 (d, 1H, J = 2.4 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.30 (td, 1H, J = 7.5, 1.8 Hz), 7.42 (td, 1H, J = 7.8, 1.5 Hz), 7.53-7.60 (m, 2H), 7.84 (d, 1H, J = 2.7 Hz).

Compound Ij-120

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.74-1.84 (m, 2H), 2.02-2.10 (m, 2H) , 2.75-2.82 (m, 2H), 2.97 (q, 2H, J = 7.5 Hz) 3.20-3.30 (m, 1H), 5.52 (d, 1H, J = 7.8 Hz), 5.80 (d, 1H, J = 2.4 Hz), 6.99 (t, 1H, J = 6.0 Hz), 7.13 (d, 1H, J = 8.1 Hz), 7.40 (t, 1H, J = 8.1 Hz), 7.62 (d, 1H, J = 8.4 Hz) ), 7.72 (s, 1H), 8.22 (d, 1H, J = 2.4 Hz).

Compound Ij-121

¹H-NMR (DMSO-d₆) δ: 0.92-1.19 (m, 4H), 1.19 (t, 3H, J = 7.5 Hz), 1.30-1.45 (m, 1H), 1.74-1.84 (m, 2H), 2.02-2.12 (m, 2H) , 2.75-2.82 (m, 2H), 2.98 (q, 2H, J = 7.5 Hz) 3.15-3.30 (m, 1H), 5.47 (d, 1H, J = 8.1 Hz), 5.78 (d, 1H, J = 2.4 Hz), 7.00 (t, 1H, J = 6.0 Hz), 7.43 (d, 2H, J = 7.8 Hz), 7.67 (d, 2H, J = 9.0 Hz), 8.17 (d, 1H, J = 2.4 Hz ).

Compound Ij-122

¹H-NMR (DMSO-d₆) δ: 0.94-1.07 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.81-1.84 (m, 2H), 1.99-2.07 (m, 2H) , 2.77-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.60-3.77 (m, 1H), 7.01-7.05 (m, 1H), 7.22-7.40 (m, 4H), 7.81 -7.87 (m, 1H), 8.02 (s, 1H), 8.36 (s, 1H).

Compound Ij-123

¹H-NMR (DMSO-d₆) δ: 0.95-1.12 (m, 4H), 1.18 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.77-1.81 (m, 2H), 1.96-1.99 (m, 2H) , 2.74-2.78 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.54-3.70 (m, 1H), 4.81 (q, 2H, J = 9.0 Hz), 6.50-6.53 (m, 1H ), 6.99-7.03 (m, 1H), 7.50 (d, 1H, J = 0.9 Hz) 7.83 (d, 1H, J = 0.9 Hz).

Compound Ij-124

¹H-NMR (DMSO-d₆) δ: 0.95-1.23 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.77-1.81 (m, 2H), 2.03-2.07 (m, 2H) , 2.74-2.80 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.61-3.73 (m, 1H), 7.00-7.04 (m, 1H), 7.09-7.12 (m, 1H), 7.29 -7.37 (m, 2H), 7.45-7.52 (m, 1H), 7.88-7.94 (m, 2H), 8.04-8.05 (m, 1H).

Compound Ij-125

¹H-NMR (DMSO-d₆) δ: 0.94-1.14 (m, 4H), 1.19 (t, 3H, J = 7.2 Hz), 1.32-1.50 (m, 1H), 1.79-1.83 (m, 2H), 1.97-2.03 (m, 2H) , 2.76-2.81 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.50-3.63 (m, 1H), 4.43 (q, 2H, J = 9.0 Hz), 7.00-7.04 (m, 1H ), 7.13-7.15 (m, 1H), 7.35 (s, 1H) 7.55 (s, 1H).

Compound Ij-126

¹H-NMR (DMSO-d₆) δ: 1.02-1.08 (m, 2H), 1.17-1.29 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.36-1.43 (m, 1H), 1.79-1.85 (m, 2H) , 2.05-2.11 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 2.99 (q, 2H, J = 7.5 Hz), 3.53-3.62 (m, 1H), 6.98 (t, 1H, J = 7.8 Hz), 7.03 (t, 1H, J = 6.3 Hz), 7.28 (dd, 1H, J = 7.5, 1.2 Hz), 7.63 (dd, 1H, J = 7.5, 1.2 Hz), 8.28 (d, 1H , J = 7.5 Hz).

Compound Ij-127

¹H-NMR (DMSO-d₆) δ: 0.97-1.05 (m, 2H), 1.18-1.24 (m, 2H), 1.16 (t, 3H, J = 7.5 Hz), 1.34-1.41 (m, 1H), 1.77-1.81 (m, 2H) , 2.02-2.08 (m, 2H), 2.76 (t, 2H, J = 6.0 Hz), 2.96 (q, 2H, J = 7.5 Hz), 3.55-3.64 (m, 1H), 7.00 (t, 1H, J = 7.8 Hz), 7.18 (dd, 1H, J = 8.4, 1.8 Hz), 7.32 (dd, 1H, J = 8.4, 0.6 Hz), 7.74 (d, 1H, J = 1.8 Hz), 8.04 (d, 1H , J = 7.8 Hz).

Compound Ij-128

¹H-NMR (DMSO-d₆) δ: 0.98-1.07 (m, 2H), 1.15-1.26 (m, 8H), 1.32-1.43 (m, 1H), 1.78-1.84 (m, 2H), 1.98-2.09 (m, 2H), 2.60 ( q, 2H, J = 7.5 Hz), 2.78 (t, 2H, J = 6.3 Hz), 2.96 (q, 2H, J = 7.5 Hz), 3.55-3.64 (m, 1H), 6.98-7.05 (m, 2H ), 7.27 (dd, 1H, J = 7.8, 1.8 Hz), 7.47 (m, 1H), 7.84 (d, 1H, J = 7.5 Hz).

Compound Ij-129

¹H-NMR (DMSO-d₆) δ: 0.92-1.15 (m, 2H), 1.15-1.35 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.48 (m, 1H), 1.78-1.88 (m, 2H) , 2.04-2.16 (m, 2H), 2.78-2.84 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.62-3.80 (m, 1H), 7.02 (t, 1H, J = 6.0 Hz ), 7.45 (d, 1H, J = 9.0 Hz), 8.09 (dd, 1H, J = 9.0, 2.4 Hz), 8.68 (d, 1H, J = 2.4 Hz), 8.70 (brs, 1H).

Compound Ij-130

¹H-NMR (DMSO-d₆) δ: 0.88-1.10 (m, 2H), 1.15-1.46 (m, 3H), 1.21 (d, 6H, J = 6.6 Hz), 1.78-1.88 (m, 2H), 1.98-2.08 (m, 2H) , 2.76-2.86 (m, 2H), 3.10-3.20 (m, 1H), 3.46-3.62 (m, 1H), 6.91-6.96 (m, 1H), 7.01 (brs, 1H), 7.64 (d, 1H, J = 7.8 Hz), 8.07 (d, 1H, J = 5.1 Hz), 8.35 (d, 1H, J = 7.8 Hz).

Compound Ij-131

¹H-NMR (DMSO-d₆) δ: 0.92-1.05 (m, 2H), 1.15-1.30 (m, 2H), 1.27 (s, 9H), 1.30-1.43 (m, 1H), 1.77-1.86 (m, 2H), 1.98-2.08 ( m, 2H), 2.86-2.92 (m, 2H), 3.35-3.50 (m, 1H), 3.73 (s, 3H), 6.69 (dd, 1H, J = 8.4, 2.0 Hz), 6.86 (t, 1H, J = 6.0 Hz), 7.01 (d, 1H, J = 2.0 Hz), 7.10 (d, 1H, J = 8.4 Hz), 7.62 (d, 1H, J = 7.6 Hz).

Compound Ij-132

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.15-1.33 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.42 (m, 1H), 1.76-1.86 (m, 2H) , 1.98-2.08 (m, 2H), 2.76-2.82 (m, 2H), 2.97 (q, 2H, J = 7.2 Hz), 3.40-3.58 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz ), 7.13 (d, 1H, J = 8.4 Hz), 7.20 (d, 1H, J = 8.4 Hz), 7.49 (s, 1H), 8.01 (d, 1H, J = 7.6 Hz).

Compound Ij-133

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.16-1.28 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.46 (m, 1H), 1.78-1.85 (m, 2H) , 2.04-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.55-3.70 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz ), 7.12 (t, 1H, J = 9.6 Hz), 7.48 (d, 1H, J = 7.6 Hz), 8.13 (d, 1H, J = 7.6 Hz).

Compound Ij-134

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.26 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.33-1.42 (m, 1H), 1.39-1.84 (m, 2H) , 2.05-2.09 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.61-3.75 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz ), 7.45 (dd, 1H, J = 7.5, 0.6 Hz), 7.60 (dd, 1H, J = 8.4, 1.5 Hz), 8.17 (d, 1H, J = 1.5 Hz), 8.50 (d, 1H, J = 7.5 Hz).

Compound Ij-135

¹H-NMR (DMSO-d₆) δ: 0.98-1.08 (m, 2H), 1.15-1.25 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.35-1.44 (m, 1H), 1.80-1.84 (m, 2H) , 2.05-2.08 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.19 (m, 1H), 3.62-3.78 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz ), 7.79 (d, 1H, J = 2.1 Hz), 8.10 (d, 1H, J = 2.1, 1.5 Hz), 8.52 (d, 1H, J = 6.9 Hz).

Compound Ij-136

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.17-1.24 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.33-1.41 (m, 1H), 1.78-1.83 (m, 2H) , 2.04-2.08 (m, 2H), 2.78 (t, 2H, J = 6.3 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.56-3.67 (m, 1H), 7.00-7.04 (m, 2H ), 7.39 (d, 1H, J = 2.1 Hz), 7.66 (dd, 1H, J = 8.4, 1.8 Hz), 8.14 (d, 1H, J = 7.5 Hz).

Compound Ij-137

¹H-NMR (DMSO-d₆) δ: 0.96-1.10 (m, 2H), 1.12-1.28 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.31 (t, 3H, J = 6.9 Hz), 1.33-1.46 (m , 1H), 1.76-1.85 (m, 2H), 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.22 (m, 1H), 3.50-3.64 (m, 1H), 3.98 (q, 2H, J = 6.9 Hz), 6.78 (dd, 1H, J = 8.7, 2.7 Hz), 6.98 (t, 1H, J = 6.0 Hz), 7.23-7.27 (m, 2H), 7.68 (d, 1H, J = 7.2 Hz).

Compound Ij-138

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 2H), 1.14-1.26 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.45 (m, 1H), 1.77-1.86 (m, 2H) , 2.03-2.12 (m, 2H), 2.76-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.52-3.68 (m, 1H), 6.97-7.06 (m, 2H), 7.34 (dd, 1H, J = 8.4, 4.8 Hz), 7.56 (dd, 1H, J = 8.4, 2.4 Hz), 7.91 (d, 1H, J = 7.6 Hz).

Compound Ij-139

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.16-1.32 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.78-1.86 (m, 2H) , 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.21 (m, 1H), 3.58-3.76 (m, 1H), 7.00 (t, 1H, J = 6.0 Hz), 8.19 -8.23 (m, 2H), 8.52 (d, 1H, J = 6.9 Hz).

Compound Ij-140

¹H-NMR (DMSO-d₆) δ: 0.96-1.12 (m, 2H), 1.12-1.30 (m, 2H), 1.21 (d, 6H, J = 6.6 Hz), 1.32-1.46 (m, 1H), 1.78-1.86 (m, 2H) , 2.02-2.16 (m, 2H), 2.78-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.58-3.78 (m, 1H), 7.01 (t, 1H, J = 6.0 Hz), 8.08 (dd, 1H, J = 8.4, 2.7 Hz), 8.19 (d, 1H, J = 2.7 Hz), 8.38 (d, 1H, J = 7.2 Hz).

Compound Ij-141

¹H-NMR (DMSO-d₆) δ: 0.97-1.08 (m, 2H), 1.15-1.22 (m, 5H), 1.34-1.42 (m, 1H), 1.78-1.83 (m, 2H), 2.04-2.08 (m, 2H), 2.78 ( t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.53-3.62 (m, 1H), 3.81 (s, 1H), 7.02 (t, 1H, J = 6.3 Hz), 7.41 (s, 1H), 7.53 (s, 1H), 7.88 (d, 1H, J = 7.5 Hz).

Compound Ij-142

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.17-1.30 (m, 2H), 1.18 (t, 3H, J = 7.5 Hz), 1.32-1.41 (m, 1H), 1.79-1.84 (m, 2H) , 2.01-2.05 (m, 2H), 2.77 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.41-3.58 (m, 1H), 6.97 (dd, 1H, J = 8.4, 2.4 Hz), 6.99-7.03 (m, 1H), 7.27 (d, 1H, J = 2.4 Hz), 7.34 (dd, 1H, J = 8.4, 0.3 Hz), 8.07-8.14 (m, 1H) .

Compound Ij-143

¹H-NMR (DMSO-d₆) δ: 0.94-1.08 (m, 2H), 1.16-1.33 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.33-1.45 (m, 1H), 1.77-1.86 (m, 2H) , 2.00-2.08 (m, 2H), 2.74-2.82 (m, 2H), 2.98 (q, 2H, J = 7.2 Hz), 3.38-3.54 (m, 1H), 6.90-7.00 (m, 1H), 7.02 (t, 1H, J = 4.5 Hz), 7.19 (dd, 1H, J = 8.4, 5.1 Hz), 7.33 (dd, 1H, J = 8.4, 2.7 Hz), 7.88 (d, 1H, J = 7.8 Hz) .

Compound Ij-144

¹H-NMR (DMSO-d₆) δ: 0.94-1.06 (m, 2H), 1.19-1.29 (m, 2H), 1.18 (t, 3H, J = 7.2 Hz), 1.31-1.41 (m, 1H), 1.79-1.84 (m, 2H) , 2.01-2.05 (m, 2H), 2.77 (t, 2H, J = 6.0 Hz), 2.98 (q, 2H, J = 6.9 Hz), 3.41-3.57 (m, 1H), 6.71-6.79 (m, 1H ), 7.06-7.08 (m, 2H), 7.31 (dd, 1H, J = 8.7, 4.8 Hz), 8.03 (d, 1H, J = 7.8 Hz).

Compound Ij-145

¹H-NMR (DMSO-d₆) δ: 0.95-1.16 (m, 2H), 1.18-1.44 (m, 3H), 1.21 (d, 6H, J = 6.6 Hz), 1.78-1.86 (m, 2H), 2.02-2.12 (m, 2H) , 2.78-2.84 (m, 2H), 3.10-3.20 (m, 1H), 3.40-3.58 (m, 1H), 6.95 (t, 1H, J = 7.8 Hz), 7.01 (brs, 1H), 7.09 (t , 1H, J = 6.9 Hz), 7.22 (d, 1H, J = 6.6 Hz), 7.31 (d, 1H, J = 7.8 Hz), 7.83 (d, 1H, J = 7.8 Hz).

Compound Ij-146

Compound Ij-147

Compound Ij-148

Compound Ij-149

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.13-1.30 (m, 2H), 1.19 (t, 3H, J = 7.5 Hz), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 2.02 -2.14 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.98 (q, 2H, J = 7.5 Hz), 3.56-3.70 (m, 1H), 6.95-7.05 (m, 2H), 7.20 (t, 1H, J = 7.8 Hz), 7.37 (d, 1H, J = 7.8 Hz), 7.64 (d, 1H, J = 7.5 Hz), 7.92 (d, 1H, J = 7.5 Hz). Melting points: 168-169 ℃ Anal. Calcd for C₁₆H_{twenty three}N_ThreeO₂S₂: C, 54.36; H, 6.56; N, 11.89; S, 18.14.Found: C, 54.33; H, 6.55; N, 11.89; S, 18.05.

Compound Ij-150

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.19 (t, 3H, J = 7.2 Hz), 1.39 (m, 1H), 1.77-1.87 (m, 2H), 1.99 -2.12 (m, 2H), 2.78 (t, 2H, J = 6.6 Hz), 2.98 (q, 2H, J = 7.2 Hz), 3.40-3.58 (m, 1H), 6.95 (t, 1H, J = 7.8 Hz), 7.02 (t, 1H, J = 6.0 Hz), 7.09 (t, 1H, J = 7.8 Hz), 7.22 (d, 1H, J = 7.5 Hz), 7.31 (d, 1H, J = 8.1 Hz) , 7.83 (d, 1H, J = 7.8 Hz). Melting point: 170-171 ° C Anal. Calcd for C₁₆H_{twenty three}N_ThreeO_ThreeS: C, 56.95; H, 6.87; N, 12.45; S, 9.50. Found: C, 56.91; H, 6.91; N, 12.43; S, 9.51.

Compound Ij-151

¹H-NMR (DMSO-d₆) δ: 0.92-1.10 (m, 2H), 1.12-1.30 (m, 2H), 1.21 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.76-1.87 (m, 2H), 2.02 -2.14 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.22 (m, 1H), 3.54-3.70 (m, 1H), 6.83 (t, 1H, J = 10.5 Hz), 6.99 (t, 1H, J = 5.4 Hz), 7.17 (dd, 1H, J = 10.5, 2.1 Hz), 7.63 (dd, 1H, J = 8.4, 5.7 Hz), 8.10 (d, 1H, J = 7.5 Hz ). Melting point: 165-166 ° C Anal. Calcd for C₁₇H_{twenty four}FN_ThreeO₂S₂: C, 52.96; H, 6.27; F, 4.93; N, 10.90; S, 16.63. Found: C, 52.99; H, 6.31; F, 5.00; N, 10.91; S, 16.84.

Compound Ij-152

¹H-NMR (DMSO-d₆) δ: 0.92-1.09 (m, 2H), 1.11-1.28 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.75-1.82 (m, 2H), 2.02 -2.12 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.20 (m, 1H), 3.52-3.67 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.03 (td, 1H, J = 9.6, 2.7 Hz), 7.34 (dd, 1H, J = 9.0, 5.1 Hz), 7.57 (dd, 1H, J = 9.0, 2.7 Hz), 7.91 (d, 1H, J = 7.2 Hz). Melting point: 151-152 ° C Anal. Calcd for C₁₇H_{twenty four}FN_ThreeO₂S₂: C, 52.96; H, 6.27; F, 4.93; N, 10.90; S, 16.63.Found: C, 52.97; H, 6.28; F, 4.90; N, 10.87; S, 16.71.

Compound Ij-153

¹H-NMR (DMSO-d₆) δ: 0.94-1.12 (m, 2H), 1.14-1.31 (m, 2H), 1.22 (d, 6H, J = 6.6 Hz), 1.39 (m, 1H), 1.76-1.87 (m, 2H), 2.02 -2.15 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.22 (m, 1H), 3.55-3.70 (m, 1H), 6.84-6.94 (m, 1H), 6.99 (t , 1H, J = 6.0 Hz), 7.18-7.28 (m, 2H), 8.21 (d, 1H, J = 7.2 Hz).

Compound Ij-154

¹H-NMR (DMSO-d₆) δ: 0.93-1.10 (m, 2H), 1.13-1.30 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.76-1.87 (m, 2H), 2.02 -2.14 (m, 2H), 2.81 (t, 2H, J = 6.0 Hz), 3.08-3.22 (m, 1H), 3.54-3.70 (m, 1H), 6.98 (t, 1H, J = 6.0 Hz), 7.02 (dd, 1H, J = 8.1, 2.1 Hz), 7.39 (d, 1H, J = 2.1 Hz), 7.66 (d, 1H, J = 8.1 Hz), 8.15 (d, 1H, J = 7.5 Hz). Melting point: 166-167 ℃ Anal. Calcd for C₁₇H_{twenty four}ClN_ThreeO₂S₂: C, 50.79; H, 6.02; Cl, 8.82; N, 10.45; S, 15.95.Found: C, 50.84; H, 6.04; Cl, 8.80; N, 10.44; S, 16.00.

Compound Ij-155

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.20-1.34 (m, 2H), 1.22 (d, 6H, J = 6.8 Hz), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 1.99 -2.14 (m, 2H), 2.80 (t, 2H, J = 6.4 Hz), 3.10-3.20 (m, 1H), 3.42-3.54 (m, 1H), 6.74 (td, 1H, J = 8.8, 2.8 Hz ), 6.98 (t, 1H, J = 5.6 Hz), 7.06 (dd, 1H, J = 9.6, 2.8 Hz), 7.30 (dd, 1H, J = 8.0, 4.4 Hz), 8.02 (d, 1H, J = 8.0 Hz). Anal. Calcd for C₁₇H_{twenty four}FN_ThreeO_ThreeS: C, 55.27; H, 6.55; F, 5.14; N, 11.37; S, 8.68. Found: C, 55.16; H, 6.50; F, 5.16; N, 11.30; S, 8.42.

Compound Ij-156

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.20-1.34 (m, 2H), 1.22 (d, 6H, J = 6.9 Hz), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 2.00 -2.14 (m, 2H), 2.81 (t, 2H, J = 6.3 Hz), 3.10-3.21 (m, 1H), 3.38-3.54 (m, 1H), 6.90-7.00 (m, 2H), 7.19 (dd , 1H, J = 8.4, 4.8 Hz), 7.33 (dd, 1H, J = 8.4, 2.4 Hz), 7.86 (d, 1H, J = 7.8 Hz). Melting point: 170-171 ° C Anal. Calcd for C₁₇H_{twenty four}FN_ThreeO_ThreeS: C, 55.27; H, 6.55; F, 5.14; N, 11.37; S, 8.68. Found: C, 55.31; H, 6.59; F, 5.13; N, 11.46; S, 8.59.

Compound Ij-157

¹H-NMR (DMSO-d₆) δ: 0.88-1.20 (m, 4H), 1.20 (d, 6H, J = 6.9 Hz), 1.36 (m, 1H), 1.75-1.83 (m, 2H), 2.02-2.13 (m, 2H), 2.79 (t, 2H, J = 6.0 Hz), 3.05-3.25 (m, 2H), 5.36 (d, 1H, J = 7.8 Hz), 5.76 (d, 1H, J = 2.4 Hz), 6.95 (t, 1H, J = 6.9 Hz), 7.30 (td, 1H, J = 7.5, 1.8 Hz), 7.42 (td, 1H, J = 7.8, 1.5 Hz), 7.53-7.60 (m, 2H), 7.84 (d, 1H, J = 2.7 Hz). Melting point: 142-143 ° C

Compound Ij-158

¹H-NMR (DMSO-d₆) δ: 0.92-1.08 (m, 2H), 1.19-1.34 (m, 2H), 1.27 (s, 9H), 1.38 (m, 1H), 1.78-1.86 (m, 2H), 1.99-2.14 (m, 2H), 2.88 (t, 2H, J = 6.3 Hz), 3.40-3.56 (m, 1H), 6.75 (td, 1H, J = 8.7, 2.7 Hz), 6.87 (t, 1H, J = 6.0 Hz), 7.06 (dd, 1H, J = 9.3, 2.7 Hz), 7.31 (dd, 1H, J = 8.7, 4.5 Hz), 8.02 (d, 1H, J = 7.8 Hz). Melting point: 220-221 ° C Anal. Calcd for C₁₈H₂₆FN_ThreeO_ThreeS: C, 56.38; H, 6.83; F, 4.95; N, 10.96; S, 8.36. Found: C, 56.41; H, 6.90; F, 4.96; N, 11.07; S, 8.36.

Compound Ij-159

¹H-NMR (DMSO-d₆) δ: 0.91-1.08 (m, 2H), 1.16-1.46 (m, 3H), 1.27 (s, 9H), 1.77-1.87 (m, 2H), 1.98-2.10 (m, 2H), 2.89 (t, 2H, J = 6.0 Hz), 3.38-3.54 (m, 1H), 6.88 (t, 1H, J = 5.7 Hz), 6.90-7.00 (m, 1H), 7.19 (dd, 1H, J = 8.7, 5.1 Hz ), 7.34 (dd, 1H, J = 8.7, 2.7 Hz), 7.88 (d, 1H, J = 7.5 Hz). Anal. Calcd for C₁₈H₂₆FN_ThreeO_ThreeS: C, 56.38; H, 6.83; F, 4.95; N, 10.96; S, 8.36. Found: C, 56.39; H, 6.93; F, 4.98; N, 11.09; S, 8.29.

Compound Ij-160

¹H-NMR (DMSO-d₆) δ: 0.95 (t, 3H, J = 7.8 Hz), 0.92-1.07 (m, 2H), 1.21 (d, 3H, J = 6.9 Hz), 1.20-1.47 (m, 4H), 1.77-1.96 (m , 3H), 1.98-2.08 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.85-2.98 (m, 1H), 3.42-3.57 (m, 1H), 6.71-6.80 (m, 1H ), 7.00 (t, 1H, J = 5.7 Hz), 7.06 (dd, 1H, J = 9.3, 2.7 Hz), 7.31 (dd, 1H, J = 8.7, 4.5 Hz), 8.02 (d, 1H, J = 7.8 Hz). Melting point: 172-173 ° C Anal. Calcd for C₁₈H₂₆FN_ThreeO_ThreeS: C, 56.38; H, 6.83; F, 4.95; N, 10.96; S, 8.36. Found: C, 56.37; H, 6.84; F, 5.04; N, 11.12; S, 8.14.

Compound Ij-161

¹H-NMR (DMSO-d₆) δ: 0.95 (t, 3H, J = 7.5 Hz), 0.92-1.08 (m, 2H), 1.21 (d, 3H, J = 6.9 Hz), 1.20-1.47 (m, 4H), 1.77-1.96 (m , 3H), 1.98-2.08 (m, 2H), 2.79 (t, 2H, J = 6.3 Hz), 2.85-2.98 (m, 1H), 3.38-3.56 (m, 1H), 6.90-6.98 (m, 1H ), 7.00 (t, 1H, J = 6.0 Hz), 7.19 (dd, 1H, J = 8.7, 5.1 Hz), 7.33 (dd, 1H, J = 8.7, 2.7 Hz), 7.88 (d, 1H, J = 7.8 Hz). Melting point: 173-174 ° C Anal. Calcd for C₁₈H₂₆FN_ThreeO_ThreeS: C, 56.38; H, 6.83; F, 4.95; N, 10.96; S, 8.36. Found: C, 56.45; H, 6.80; F, 4.93; N, 11.02; S, 8.54.

Test example 1 Brain transportability and drug-drug interaction via P-gp For brain transportability (brain / plasma partition coefficient; Kp), mice (Jcl; C57BL / 6J mouse, ♂, 7 weeks) were administered intravenously (0.5 (mg / 2 mL / kg) and evaluated from plasma and brain concentrations. As a result, the brain Kp value (Kp _Cont. ) Of compound (I-72) was 1.29, indicating high brain migration.
In order to examine the interaction between drugs via P-gp in vivo, the brain Kp value (Kp _CSA ) in the presence of cyclosporin A 20 mg / kg, a P-gp inhibitor, was measured and the control group (Kp _Cont. ). Compound (I-72) had a Kp _CSA of 1.14, a Kp ratio with Kp _Cont. (Kp _CSA / Kp _Cont. ) Of 0.9, and no drug-drug interaction via P-gp was observed.

For comparative reference, amide compound B having a similar structure was tested in the same evaluation system _. As a result, Kp _{Cont. And} Kp _CSA were 0.04, 0.84 and Kp ratio were 20.5, respectively _. The drug was strongly pumped out and drug-drug interactions were observed.

試験例２−２ ヒトＮＰＹ Ｙ５受容体に対する親和性
ヒトＮＰＹ Ｙ５受容体をコードするcDNA配列（WO96／16542号参照）を、発現ベクター pME18S（Takebe et al. Mol. Cell. Biol. 8, 466-472）にクローニングした。得られた発現ベクターを、LipofectAMINE試薬（商標、Gibco BRL社）を用いて、宿主細胞CHOに、使用説明書にしたがってトランスフェクションし、ＮＰＹ Ｙ５受容体安定発現細胞を得た。
ＮＰＹ Ｙ５受容体を発現させたCHO細胞から調製した膜標品を、本発明に係る化合物および30,000 cpmの[¹²⁵I]ペプタイドＹＹ（終濃度60 pM：アマーシャム社製）とともに、アッセイ緩衝液（0.1% 牛血清アルブミンを含む20 mM HEPES-Hanks緩衝液、pH 7.4）中で、25℃、2時間インキュベーションした後、1% ポリエチレンイミン処理したグラスフィルターGF/Cにて濾過した。50 mM Tris-HCl緩衝液、pH 7.4にて洗浄後、ガンマカウンターにてグラスフィルター上の放射活性を求めた。非特異的結合は200 nMペプタイドＹＹ存在下で測定し、特異的ペプタイドＹＹ結合に対する被検化合物の50%阻害濃度（IC₅₀値）を求めた[Inui, A. et al. Endocrinology 131, 2090-2096 (1992) 参照]。
本発明に係る化合物は、ヒトＮＰＹ Ｙ５受容体に対するペプタイドＹＹ（ＮＰＹと同属物質）の結合を阻害した。即ち、本化合物はヒトＮＰＹ Ｙ５受容体に対して親和性を示した。 Test Example 2-1 Affinity for mouse NPY Y5 receptor cDNA sequence encoding mouse NPY Y5 receptor (see Biochim. Biophys. Acta 1328: 83-89, 1997) was expressed in expression vector pME18S (Takebe et al. Mol. Cell. Biol. 8, 466-472). The obtained expression vector was transfected into host cell CHO using LipofectAMINE reagent (trademark, Gibco BRL) according to the instruction manual to obtain NPY Y5 receptor stably expressing cells.
Membrane preparations prepared from CHO cells expressing mouse NPY Y5 receptor were combined with the compounds of the present invention and 30,000 cpm [ ¹²⁵ I] peptide YY (final concentration 60 pM, manufactured by Amersham) with assay buffer ( After incubating in 20 mM HEPES-Hanks buffer solution (pH 7.4) containing 0.1% bovine serum albumin at 25 ° C. for 2 hours, it was filtered through a glass filter GF / C treated with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer, pH 7.4, the radioactivity on the glass filter was determined with a gamma counter. Nonspecific binding was measured in the presence of 200 nM peptide YY, and the 50% inhibitory concentration (IC ₅₀ value) of the test compound for specific peptide YY binding was determined [Inui, A. et al. Endocrinology 131, 2090- 2096 (1992)]. The results are shown in Table 1.
The compound according to the present invention inhibited the binding of peptide YY (similar substance to NPY) to mouse NPY Y5 receptor. That is, this compound showed affinity for the mouse NPY Y5 receptor.

Test Example 2-2 Affinity for human NPY Y5 receptor cDNA sequence encoding human NPY Y5 receptor (see WO96 / 16542) was expressed in expression vector pME18S (Takebe et al. Mol. Cell. Biol. 8, 466- 472). The obtained expression vector was transfected into host cell CHO using LipofectAMINE reagent (trademark, Gibco BRL) according to the instruction manual to obtain NPY Y5 receptor stably expressing cells.
Membrane preparations prepared from CHO cells expressing the NPY Y5 receptor were combined with the compounds of the present invention and 30,000 cpm [ ¹²⁵ I] peptide YY (final concentration 60 pM, manufactured by Amersham) with an assay buffer (0.1 After incubating in 20 mM HEPES-Hanks buffer solution (pH 7.4) containing 2% bovine serum albumin at 25 ° C. for 2 hours, the solution was filtered through a glass filter GF / C treated with 1% polyethyleneimine. After washing with 50 mM Tris-HCl buffer, pH 7.4, the radioactivity on the glass filter was determined with a gamma counter. Nonspecific binding was measured in the presence of 200 nM peptide YY, and the 50% inhibitory concentration (IC ₅₀ value) of the test compound for specific peptide YY binding was determined [Inui, A. et al. Endocrinology 131, 2090- 2096 (1992)].
The compound according to the present invention inhibited the binding of peptide YY (NPY and related substances) to the human NPY Y5 receptor. That is, this compound showed affinity for the human NPY Y5 receptor.

Test Example 3 Inhibition of cAMP production in CHO cells CHO cells expressing human NPY Y5 receptor were cultured at 37 ° C. for 20 minutes in the presence of 0.1 mM isobutylmethylxanthine (SIGMA) and 0.2 mM RO-201724 (Calbiochem). After incubation, the compound according to the present invention was added and incubated for 10 minutes, and then 50 nM NPY and 10 μM forskolin (Sigma) were added and incubated for 30 minutes. After stopping the reaction by adding 1N HCl, the amount of cAMP in the supernatant was measured using an EIA kit (manufactured by Amersham LIFE SIENCE). The inhibitory action of NPY on cAMP production by forskolin stimulation was taken as 100%, and the 50% inhibitory concentration (IC ₅₀ value) of the compound according to the present invention for this NPY action was determined.

Test example 4
Using a Y1-expressing cell (human neuroblastoma, SK-N-MC) membrane sample and a Y2-expressing cell (human neuroblastoma, SMS-KAN) membrane sample, the test was performed in the same manner as in Test Example 2-2. The affinity of the compounds of the invention for the NPY Y1 receptor and NPY Y2 receptor was measured. From the result, it was confirmed that the compound according to the present invention has NPY Y5 receptor selectivity.

Test Example 5
Under ether anesthesia, male C57BL / 6J mice (12-14 weeks old, 25-30 g) were incised through the midline from the outer occipital crest to the back of the nose to expose the upper skull. A hole with a diameter of about 1 mm was drilled with an electric drill at a position about 1 mm backward from the exposed part bregma toward the lambda and about 1 mm on the left side from the midline. A 0.5% hydroxypropylmethylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd.) aqueous solution (Vehicle) or a test substance suspended in this aqueous solution is forcibly administered orally to mice after waking up from anesthesia. NPY Y5 receptor specific agonist ([cPP ^1-7 , NPY ^19-23 , Ala ³¹ , Aib ³² , Gln ³⁴ ] -hPancreatic Polypeptide: manufactured by Tocris) 0.1 nmol was previously cannulated from the head opening Was injected. The amount of food intake of the mice was measured 2 hours and 4 hours after the injection, and the feeding suppression rate was calculated by the following formula. Feeding inhibition rate (%) = [1- (test substance oral administration / feeding amount of Y5 agonist injection group−feeding amount of vehicle oral administration / saline injection group) / vehicle oral administration / feeding of Y5 injection group Amount-Vehicle oral administration / Saline injection group food intake)] × 100. As a result, when the compound used in the present invention was administered at a dose of 1.5 mg / kg or 6 mg / kg, the amount of food intake was significantly suppressed as compared with the case where 0.5% hydroxypropylmethylcellulose was administered. Table 2 shows the results of the feeding suppression rate at 4 hours.

Test Example 6
Tests suspended in 0.5% hydroxypropylmethylcellulose (manufactured by Shin-Etsu Chemical Co., Ltd.) aqueous solution or in male C57BL / 6J mice (13-14 weeks old, body weight 28-33 g) whose body weight was increased by feeding high fat diet The substance was orally administered by gavage twice a day for 3 weeks every day, and daily changes in body weight of the 0.5% hydroxymethylcellulose solution (Vehicle) administration group and the test substance administration group were investigated. During the compound administration period, feeding with a high fat diet was continued. As a result, when the compound used in the present invention was administered twice daily at a dose of 6.25 mg / kg, body weight gain was significantly suppressed as compared with the case where 0.5% hydroxypropylmethylcellulose was administered.

Formulation Examples Formulation examples shown below are merely illustrative and are not intended to limit the scope of the invention.
Formulation Example 1 Tablet Compound (I-1) 15 mg
Starch 15mg
Lactose 15mg
Crystalline cellulose 19mg
Polyvinyl alcohol 3mg
30ml distilled water
Calcium stearate 3mg
Ingredients other than calcium stearate are uniformly mixed, crushed and granulated, and dried to obtain granules of an appropriate size. Next, calcium stearate is added and compressed to form tablets.

Formulation Example 2 Capsule Compound (I-2) 10 mg
Magnesium stearate 10mg
Lactose 80mg
Are mixed uniformly to make a powder as a fine powder or powder. It is filled into a capsule container to form a capsule.

Formulation Example 3 Granules Compound (I-3) 30 g
Lactose 265g
Magnesium stearate 5g
After mixing well, compression molding, pulverizing, sizing, and sieving to make granules of appropriate size.

  As is clear from the above test examples, the compound according to the present invention exhibits NPY Y5 receptor antagonistic action, feeding inhibitory action, and body weight inhibitory action. Therefore, the present invention is very useful as an appetite suppressant or anti-obesity agent.

Claims (4)

formula:

In it indicated the reduction compounds, oral agent containing a pharmaceutically acceptable salt or solvate thereof. A tablet, an oral agent according to claim 1 Symbol placement. A capsule, oral agent according to claim 1 Symbol placement. A granule, oral agent according to claim 1 Symbol placement.