JP3684332B2 - エナンチオ選択的合成 - Google Patents

エナンチオ選択的合成 Download PDF

Info

Publication number
JP3684332B2
JP3684332B2 JP2000564945A JP2000564945A JP3684332B2 JP 3684332 B2 JP3684332 B2 JP 3684332B2 JP 2000564945 A JP2000564945 A JP 2000564945A JP 2000564945 A JP2000564945 A JP 2000564945A JP 3684332 B2 JP3684332 B2 JP 3684332B2
Authority
JP
Japan
Prior art keywords
formula
compound
temperature
acid addition
sufficient
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Fee Related
Application number
JP2000564945A
Other languages
English (en)
Japanese (ja)
Other versions
JP2002522533A (ja
Inventor
リチャード ダブリュー． ドレイパー，
ラダ ブイ． イエール，
ユーリー ルー，
ユージーン ジェイ． ベイター，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme LLC
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
Publication of JP2002522533A publication Critical patent/JP2002522533A/ja
Application granted granted Critical
Publication of JP3684332B2 publication Critical patent/JP3684332B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/22—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4
    • C07D311/26—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4
    • C07D311/60—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4 with aryl radicals attached in position 2

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Catalysts (AREA)
  • Steroid Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
JP2000564945A 1998-08-14 1999-08-12 エナンチオ選択的合成 Expired - Fee Related JP3684332B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US13421698A 1998-08-14 1998-08-14
US09/134,216 1998-08-14
PCT/US1999/016711 WO2000009493A1 (en) 1998-08-14 1999-08-12 Enantioselective synthesis

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2005112900A Division JP4461048B2 (ja) 1998-08-14 2005-04-08 エナンチオ選択的合成

Publications (2)

Publication Number Publication Date
JP2002522533A JP2002522533A (ja) 2002-07-23
JP3684332B2 true JP3684332B2 (ja) 2005-08-17

Family

ID=22462296

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2000564945A Expired - Fee Related JP3684332B2 (ja) 1998-08-14 1999-08-12 エナンチオ選択的合成
JP2005112900A Expired - Fee Related JP4461048B2 (ja) 1998-08-14 2005-04-08 エナンチオ選択的合成

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2005112900A Expired - Fee Related JP4461048B2 (ja) 1998-08-14 2005-04-08 エナンチオ選択的合成

Country Status (10)

Country Link
EP (1) EP1104414B1 (enExample)
JP (2) JP3684332B2 (enExample)
CN (1) CN1146554C (enExample)
AT (1) ATE232525T1 (enExample)
AU (1) AU5459399A (enExample)
CA (1) CA2340343C (enExample)
DE (1) DE69905376T2 (enExample)
ES (1) ES2188222T3 (enExample)
WO (1) WO2000009493A1 (enExample)
ZA (1) ZA200100875B (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3205648A1 (en) 2010-06-10 2017-08-16 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
EP2791132A4 (en) 2011-12-14 2015-08-05 Seragon Pharmaceuticals Inc ESTROGEN RECEPTOR MODULATORS AND USES THEREOF
BR112014014767A2 (pt) 2011-12-16 2017-06-13 Olema Pharmaceuticals Inc novos compostos de benzopirano, composições e usos dos mesmos

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
US5254568A (en) * 1990-08-09 1993-10-19 Council Of Scientific & Industrial Research Benzopyrans as antiestrogenic agents
US6060503A (en) * 1991-12-02 2000-05-09 Endorecherche, Inc. Benzopyran-containing compounds and method for their use
US5407947A (en) * 1993-11-05 1995-04-18 Eli Lilly And Company Methods for inhibiting bone loss using pyrolidine and piperidine substituted benzopyrans
AU8102398A (en) * 1997-07-09 1999-02-08 Central Drug Research Institute (dl)-2,3-diaryl-2h-1-benzopyrans
AU8102498A (en) * 1997-07-09 1999-02-08 Central Drug Research Institute Preparation of diaryl-benzopyrans
US6465445B1 (en) * 1998-06-11 2002-10-15 Endorecherche, Inc. Medical uses of a selective estrogen receptor modulator in combination with sex steroid precursors

Also Published As

Publication number Publication date
ES2188222T3 (es) 2003-06-16
WO2000009493A1 (en) 2000-02-24
JP2002522533A (ja) 2002-07-23
CN1322200A (zh) 2001-11-14
CN1146554C (zh) 2004-04-21
CA2340343C (en) 2007-04-24
AU5459399A (en) 2000-03-06
ATE232525T1 (de) 2003-02-15
JP4461048B2 (ja) 2010-05-12
ZA200100875B (en) 2002-06-26
CA2340343A1 (en) 2000-02-24
DE69905376D1 (de) 2003-03-20
HK1036978A1 (en) 2002-01-25
DE69905376T2 (de) 2003-10-09
JP2005206610A (ja) 2005-08-04
EP1104414A1 (en) 2001-06-06
EP1104414B1 (en) 2003-02-12

Similar Documents

Publication Publication Date Title
JP4377219B2 (ja) Ｒ−及びｓ−シタロプラムの混合物を分離することによってラセミシタロプラム及びｓ−もしくはｒ−シタロプラムを製造する方法
US8288569B2 (en) Carbonyl asymmetric alkylation
US20110092719A1 (en) Preparation of Escitalopram, Its Salts and Intermediates
JP2009523749A5 (enExample)
US6262270B1 (en) Enantioselective synthesis
JP4505335B2 (ja) ラセミ体シタロプラムジオール（ｒａｃｅｍｉｃｃｉｔａｌｏｐｒａｍｄｉｏｌ）および／またはＳ−もしくはＲ−シタロプラムジオールの製造方法、およびラセミ体シタロプラム、Ｒ−シタロプラムおよび／またはＳ−シタロプラムを製造するために、上記ジオールを使用する方法。
JP4461048B2 (ja) エナンチオ選択的合成
US6846957B2 (en) Synthesis of 3-aminomethyl-1-propanol, a fluoxetine precursor
RU2470018C2 (ru) Новые производные пирокатехина
JP4451600B2 (ja) ビペリデンの製造方法
EP1281707B1 (en) Process for the preparation of 5-subtituted isobenzofurans
JPH11504650A (ja) アルファ−（置換アルキルフェニル）−４−（ヒドロキシジフェニルメチル）−１−ピペリジンブタノール誘導体、その製造および抗ヒスタミン剤、抗アレルギー剤および気管支拡張剤としてのその使用
JP2010527345A (ja) エスシタロプラムの調製方法
AU2002325385A1 (en) Process for the preparation of 5-substituted isobenzofurans
JP2004529883A (ja) シタロプラムの調製方法
HK1036978B (en) Enantioselective synthesis
IL158926A (en) Process for making bifridan
CN108084049B (zh) 一种泊沙康唑中间体的制备方法
MXPA01001643A (es) Sintesis enantioselectiva
JP4032593B2 (ja) ４−アミノテトラヒドロピラン誘導体の製法
EP1678122A1 (en) Improved process for the manufacture of citalopram hydrobromide
WO2008052930A2 (en) Preparation of 4-alk0xy-7- (tetrahydropyran-4-yl) benzothiazol-2-amine derivatives
JPH11286485A (ja) 光学活性アミノアルコ―ル類の製造方法
KR20050102948A (ko) 수마트립탄의 제조방법
HU221922B1 (hu) Eljárás paroxetinsók, valamint azok hidrátjai előállítására

Legal Events

Date Code Title Description
A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20040520

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20040818

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20041209

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050408

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20050426

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20050519

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20050530

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090603

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090603

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090603

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20090603

Year of fee payment: 4

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100603

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100603

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20100603

Year of fee payment: 5

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110603

Year of fee payment: 6

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110603

Year of fee payment: 6

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110603

Year of fee payment: 6

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20110603

Year of fee payment: 6

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120603

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120603

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120603

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120603

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20120603

Year of fee payment: 7

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20130603

Year of fee payment: 8

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20130603

Year of fee payment: 8

S531 Written request for registration of change of domicile

Free format text: JAPANESE INTERMEDIATE CODE: R313531

S533 Written request for registration of change of name

Free format text: JAPANESE INTERMEDIATE CODE: R313533

R350 Written notification of registration of transfer

Free format text: JAPANESE INTERMEDIATE CODE: R350

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

R250 Receipt of annual fees

Free format text: JAPANESE INTERMEDIATE CODE: R250

LAPS Cancellation because of no payment of annual fees