ATE236148T1 - Synthese der terfenadin und deren derivate - Google Patents

Synthese der terfenadin und deren derivate

Info

Publication number
ATE236148T1
ATE236148T1 AT98901831T AT98901831T ATE236148T1 AT E236148 T1 ATE236148 T1 AT E236148T1 AT 98901831 T AT98901831 T AT 98901831T AT 98901831 T AT98901831 T AT 98901831T AT E236148 T1 ATE236148 T1 AT E236148T1
Authority
AT
Austria
Prior art keywords
terfenadine
synthesis
derivatives
processes
general formula
Prior art date
Application number
AT98901831T
Other languages
English (en)
Inventor
Chris Hugh Senanayake
Qun Kevin Fang
Scott Harold Wilkinson
Original Assignee
Sepracor Inc
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 Sepracor Inc filed Critical Sepracor Inc
Application granted granted Critical
Publication of ATE236148T1 publication Critical patent/ATE236148T1/de

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18Radicals substituted by singly bound oxygen or sulfur atoms
    • C07D317/20Free hydroxyl or mercaptan
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/76Esters of carboxylic acids having a carboxyl group bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/18Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D307/20Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/18Radicals substituted by singly bound oxygen or sulfur atoms
    • C07D317/22Radicals substituted by singly bound oxygen or sulfur atoms etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pulmonology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Furan Compounds (AREA)
AT98901831T 1997-02-04 1998-01-20 Synthese der terfenadin und deren derivate ATE236148T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/803,895 US5925761A (en) 1997-02-04 1997-02-04 Synthesis of terfenadine and derivatives
PCT/US1998/000898 WO1998033789A1 (en) 1997-02-04 1998-01-20 Synthesis of terfenadine and derivatives

Publications (1)

Publication Number Publication Date
ATE236148T1 true ATE236148T1 (de) 2003-04-15

Family

ID=25187720

Family Applications (1)

Application Number Title Priority Date Filing Date
AT98901831T ATE236148T1 (de) 1997-02-04 1998-01-20 Synthese der terfenadin und deren derivate

Country Status (11)

Country Link
US (2) US5925761A (de)
EP (1) EP0956286B1 (de)
JP (1) JP4330179B2 (de)
AT (1) ATE236148T1 (de)
AU (1) AU724665B2 (de)
CA (1) CA2279960C (de)
DE (1) DE69812895T2 (de)
DK (1) DK0956286T3 (de)
ES (1) ES2196531T3 (de)
PT (1) PT956286E (de)
WO (1) WO1998033789A1 (de)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6201124B1 (en) * 1995-12-21 2001-03-13 Albany Molecular Research, Inc. Process for production of piperidine derivatives
US6153754A (en) * 1995-12-21 2000-11-28 Albany Molecular Research, Inc. Process for production of piperidine derivatives
IN191492B (de) * 1999-05-25 2003-12-06 Ranbaxy Lab Ltd
IL158334A0 (en) * 2001-04-09 2004-05-12 Teva Pharma Polymorphs of fexofenadine hydrochloride
US20030021849A1 (en) * 2001-04-09 2003-01-30 Ben-Zion Dolitzky Polymorphs of fexofenadine hydrochloride
US20040044038A1 (en) * 2002-06-10 2004-03-04 Barnaba Krochmal Polymorphic form XVI of fexofenadine hydrochloride
SK285548B6 (sk) * 2002-11-13 2007-03-01 Zentiva, A. S. Spôsob prípravy terfenadinu a jeho derivátov
JP2007532687A (ja) * 2004-04-26 2007-11-15 テバ ファーマシューティカル インダストリーズ リミティド フェキソフェナジン塩酸塩の結晶形およびその製造方法
JP2008514641A (ja) * 2004-09-28 2008-05-08 テバ ファーマシューティカル インダストリーズ リミティド 結晶形フェキソフェナジン、およびその調製方法
WO2007135693A2 (en) * 2006-05-18 2007-11-29 Ind-Swift Laboratories Limited Intermediates useful for the preparation of antihistaminic piperidine derivative
PT2074122E (pt) 2006-09-15 2011-08-24 Pfizer Prod Inc Compostos de pirido(2,3-d)-pirimidinona e sua utilização como inibidores de pi3
US7868200B2 (en) * 2008-12-30 2011-01-11 Lyondellbasell Flavors & Fragrances, Llc Process for preparing alicyclic carboxylic acid compounds
KR102233327B1 (ko) * 2013-12-26 2021-03-26 스미또모 가가꾸 가부시끼가이샤 할로겐 치환 프탈리드의 제조 방법
CN104876853B (zh) * 2015-06-17 2017-06-16 苏州卫生职业技术学院 盐酸非索非那定的合成方法
US10092087B2 (en) 2016-06-03 2018-10-09 Israel Harry Zimmerman Self-righting toothbrush
US10485330B2 (en) 2017-02-20 2019-11-26 Israel Harry Zimmerman Self-righting toothbrush
US10517386B2 (en) 2017-03-30 2019-12-31 Israel Harry Zimmerman Self-righting toothbrush
USD874832S1 (en) 2018-03-23 2020-02-11 Israel Harry Zimmerman Toothbrush handle
USD876097S1 (en) 2018-03-23 2020-02-25 Israel Harry Zimmerman Toothbrush handle

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3141024A (en) * 1964-07-14 S-trimethoxy benzoyl amino
US3806526A (en) * 1972-01-28 1974-04-23 Richardson Merrell Inc 1-aroylalkyl-4-diphenylmethyl piperidines
US3965257A (en) * 1972-01-28 1976-06-22 Richardson-Merrell Inc. Compositions and methods for the treatment of the symptoms of histamine induced allergic reactions
US4254129A (en) * 1979-04-10 1981-03-03 Richardson-Merrell Inc. Piperidine derivatives
EP0479601B1 (de) * 1990-10-05 1999-12-15 Ajinomoto Co., Inc. Piperidinderivate und ihre Verwendung als antiarrhythmische Wirkstoffe
EP1688142A1 (de) * 1992-08-03 2006-08-09 Sepracor Inc. Terfenadin-Carboxylat und die Behandlung von Hautreizung
EP1369409B1 (de) * 1993-06-24 2006-04-05 AMR Technology, Inc. Verfahren zur Herstellung von Verbindungen geeignet als Zwischenprodukte
DK0705245T3 (da) * 1993-06-25 2003-04-14 Merrell Pharma Inc Nye mellemprodukter til fremstilling af antihistaminiske 4-diphenylmethyl/diphenylmethoxy-piperidinforbindelser
JPH10503752A (ja) * 1994-05-16 1998-04-07 メリル・フアーマシユウテイカルズ・インコーポレイテツド ラセミ形α−〔4−(1,1−ジメチルエチル)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および誘導体化合物の光学分割に有用な方法およびジアステレオマー塩

Also Published As

Publication number Publication date
DE69812895T2 (de) 2004-04-22
US6147217A (en) 2000-11-14
ES2196531T3 (es) 2003-12-16
EP0956286B1 (de) 2003-04-02
AU5826298A (en) 1998-08-25
PT956286E (pt) 2003-08-29
WO1998033789A1 (en) 1998-08-06
US5925761A (en) 1999-07-20
DE69812895D1 (de) 2003-05-08
JP4330179B2 (ja) 2009-09-16
DK0956286T3 (da) 2003-07-14
EP0956286A1 (de) 1999-11-17
AU724665B2 (en) 2000-09-28
CA2279960A1 (en) 1998-08-06
CA2279960C (en) 2007-07-17
JP2001511144A (ja) 2001-08-07

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