ATE450520T1 - Stereoselektive alkylierung von chirale 2-methyl- 4-geschützte piperazinen - Google Patents

Stereoselektive alkylierung von chirale 2-methyl- 4-geschützte piperazinen

Info

Publication number
ATE450520T1
ATE450520T1 AT03733842T AT03733842T ATE450520T1 AT E450520 T1 ATE450520 T1 AT E450520T1 AT 03733842 T AT03733842 T AT 03733842T AT 03733842 T AT03733842 T AT 03733842T AT E450520 T1 ATE450520 T1 AT E450520T1
Authority
AT
Austria
Prior art keywords
chiral
methyl
stereoselective alkylation
protected piperazines
piperazines
Prior art date
Application number
AT03733842T
Other languages
English (en)
Inventor
Wenxue Wu
Hongbiao Liao
David Tsai
David Andrews
Dinesh Gala
Gary Lee
Martin Schwartz
Timothy Mcallister
Xiaoyong Fu
Donal Maloney
T Thiruvengadam
Chou-Hang Tann
Original Assignee
Schering Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of ATE450520T1 publication Critical patent/ATE450520T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/63—Esters of sulfonic acids
    • C07C309/72—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/73—Esters of sulfonic acids having sulfur atoms of esterified sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton to carbon atoms of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/51—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition
    • C07C45/511—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups
    • C07C45/512—Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by pyrolysis, rearrangement or decomposition involving transformation of singly bound oxygen functional groups to >C = O groups the singly bound functional group being a free hydroxyl group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
    • C07D295/205—Radicals derived from carbonic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AT03733842T 2002-03-29 2003-03-27 Stereoselektive alkylierung von chirale 2-methyl- 4-geschützte piperazinen ATE450520T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US36870702P 2002-03-29 2002-03-29
PCT/US2003/009275 WO2003084942A2 (en) 2002-03-29 2003-03-27 Stereoselective alkylation of chiral 2-methyl-4-protected piperazines

Publications (1)

Publication Number Publication Date
ATE450520T1 true ATE450520T1 (de) 2009-12-15

Family

ID=28791901

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03733842T ATE450520T1 (de) 2002-03-29 2003-03-27 Stereoselektive alkylierung von chirale 2-methyl- 4-geschützte piperazinen

Country Status (13)

Country Link
US (3) US6872826B2 (de)
EP (3) EP1490346B1 (de)
JP (2) JP2005526826A (de)
CN (2) CN100343240C (de)
AR (1) AR039196A1 (de)
AT (1) ATE450520T1 (de)
AU (1) AU2003239128A1 (de)
CA (1) CA2480481A1 (de)
DE (1) DE60330323D1 (de)
ES (1) ES2335488T3 (de)
MX (1) MXPA04009414A (de)
WO (1) WO2003084942A2 (de)
ZA (1) ZA200406469B (de)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1548010A4 (de) * 2002-09-05 2007-08-01 Toray Finechemicals Co Ltd Verfahren zur herstellung eines oxycarbonylsubstituierten piperazinderivats
JP2004143087A (ja) * 2002-10-24 2004-05-20 Central Glass Co Ltd 光学活性２−アルコキシ−１−（トリフルオロメチル置換フェニル）エタノール誘導体の製造方法
US20090299063A1 (en) * 2005-03-29 2009-12-03 Paul Shapiro Inhibitors for Extracellular Signal-Regulated Kinase Docking Domains and Uses Therefor
JP2007099659A (ja) * 2005-10-03 2007-04-19 Toray Fine Chemicals Co Ltd ピペラジンカルボン酸エステルの製造法
JP5727482B2 (ja) 2009-08-24 2015-06-03 ニューラルステム， インコーポレイテッド 神経刺激性ピペラジンの合成
CN102241611B (zh) * 2011-05-18 2014-02-26 江阴市雪豹精细化工研究所 S（一）对甲基苯磺酰基丙酸乙酯的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5889006A (en) * 1995-02-23 1999-03-30 Schering Corporation Muscarinic antagonists
CA2296314A1 (en) * 1997-07-25 1999-02-04 Merck & Co., Inc. Cyclic amine modulators of chemokine receptor activity
TR200103214T2 (tr) * 1999-05-04 2002-03-21 Schering Corporation CCR5 antagonistleri olarak yararlì piperazin trevleri.
US6391865B1 (en) 1999-05-04 2002-05-21 Schering Corporation Piperazine derivatives useful as CCR5 antagonists
CN1242995C (zh) * 1999-05-21 2006-02-22 比奥维特罗姆股份公司 化合物,它们的用途和制备方法
SE0001899D0 (sv) * 2000-05-22 2000-05-22 Pharmacia & Upjohn Ab New compounds
JP4807675B2 (ja) * 2001-02-26 2011-11-02 東レ・ファインケミカル株式会社 高純度ピペラジン誘導体塩酸塩の製造方法

Also Published As

Publication number Publication date
MXPA04009414A (es) 2005-01-25
WO2003084942A3 (en) 2004-05-06
JP2010111684A (ja) 2010-05-20
DE60330323D1 (de) 2010-01-14
ZA200406469B (en) 2005-09-20
EP2141143A2 (de) 2010-01-06
JP2005526826A (ja) 2005-09-08
EP2141153A3 (de) 2010-05-26
EP1490346A2 (de) 2004-12-29
US6872826B2 (en) 2005-03-29
US7745626B2 (en) 2010-06-29
EP2141153A2 (de) 2010-01-06
EP1490346B1 (de) 2009-12-02
CN101092401A (zh) 2007-12-26
US20100249411A1 (en) 2010-09-30
EP2141143A3 (de) 2010-05-05
WO2003084942A2 (en) 2003-10-16
AR039196A1 (es) 2005-02-09
HK1067126A1 (en) 2005-04-01
ES2335488T3 (es) 2010-03-29
CA2480481A1 (en) 2003-10-16
US20050171120A1 (en) 2005-08-04
CN100343240C (zh) 2007-10-17
CN1642930A (zh) 2005-07-20
US20030208074A1 (en) 2003-11-06
AU2003239128A1 (en) 2003-10-20

Similar Documents

Publication Publication Date Title
DE60315846D1 (de) Zusammenbau von chirurgischem klammerwerkzeug
ATE414699T1 (de) Inhibitoren von tyrosinkinasen
DE60321130D1 (de) Variation von parametern zur neurostimulation
DE60233133D1 (de) Polymorphe formen von 1-ä4-(5-cyanoindol-3-yl)butylü-4-(2-carbamoylbenzofuran-5-yl) piperazin-hydrochlorid
DK1472255T3 (da) Aza-arylpiperaziner
DE50212455D1 (de) Verwendung von Dimerdiolen
ATE510556T1 (de) Verwendung von erythropoietin
DE602004013990D1 (de) Ernen von spänen
ATE477803T1 (de) Metabolit von quetiapine
DE60324253D1 (de) Spezifische multiplex-analyse von nukleinsäuren
DE60327426D1 (de) Markierung von substraten
DE60220192D1 (de) Defragmentierung von uebertragungssequenzen
DE60318401D1 (de) Hydrierung von terephthalsäurerestehaltigen polyesteroligomeren
DE50311406D1 (de) Verwendung von Formkörpern
DE60330323D1 (de) Stereoselektive alkylierung von chirale 2-methyl-4-geschützte piperazinen
DE10256898A8 (de) Elektrochemischer Nachweis von Nukleinsäuren
NO20022596A (no) Stikkpilleapplikator
ATE556564T1 (de) Zuweisung von zeitschlitzen
DE60031450D1 (de) Polymorph v von torasemid
DE60216525D1 (de) Reinigungsverfahren von aromaten
DE50203046D1 (de) Verwendung von Esterquats
ATE394140T1 (de) Verwendung neuer etonogestrelester
DE50205590D1 (de) Ummantelung von leiterbahnen
ATE499348T1 (de) Stabiler polymorph von bifeprunoxmesilat
DE60216986D1 (de) Neue verwendung von pipatalin

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties