CN107163038B - 化学方法 - Google Patents

化学方法 Download PDF

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Publication number
CN107163038B
CN107163038B CN201710384492.2A CN201710384492A CN107163038B CN 107163038 B CN107163038 B CN 107163038B CN 201710384492 A CN201710384492 A CN 201710384492A CN 107163038 B CN107163038 B CN 107163038B
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China
Prior art keywords
formula
process according
compound
solvent
toluene
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CN201710384492.2A
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English (en)
Chinese (zh)
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CN107163038A (zh
Inventor
F.霍斯纳
J.B.斯特拉钱
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Glaxo Group Ltd
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Glaxo Group Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/10—Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms
    • C07D211/14—Heterocyclic 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 radicals containing only carbon and hydrogen atoms attached to ring carbon atoms with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pulmonology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Steroid Compounds (AREA)
CN201710384492.2A 2012-08-15 2013-08-14 化学方法 Active CN107163038B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261683369P 2012-08-15 2012-08-15
US61/683369 2012-08-15
CN201380043392.3A CN104619706B (zh) 2012-08-15 2013-08-14 化学方法

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN201380043392.3A Division CN104619706B (zh) 2012-08-15 2013-08-14 化学方法

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CN107163038A CN107163038A (zh) 2017-09-15
CN107163038B true CN107163038B (zh) 2020-07-28

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CN201710384492.2A Active CN107163038B (zh) 2012-08-15 2013-08-14 化学方法
CN201380043392.3A Active CN104619706B (zh) 2012-08-15 2013-08-14 化学方法

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US (2) US9273001B2 (enAn)
EP (2) EP2885298B1 (enAn)
JP (2) JP6389174B2 (enAn)
KR (1) KR20150043465A (enAn)
CN (2) CN107163038B (enAn)
AU (3) AU2013304102B2 (enAn)
BR (1) BR112015003101B1 (enAn)
CA (1) CA2881935A1 (enAn)
ES (2) ES2678697T3 (enAn)
IN (1) IN2015KN00323A (enAn)
RU (1) RU2644160C2 (enAn)
WO (1) WO2014027045A1 (enAn)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2959699T3 (es) 2014-05-28 2024-02-27 Glaxosmithkline Ip Dev Ltd Furoato de fluticasona en el tratamiento de la EPOC
WO2016071792A1 (en) 2014-11-03 2016-05-12 Laboratorio Chimico Internazionale S.P.A. Method for the preparation of 1-(2-halogen-ethyl)-4 piperidine-carboxylic acid ethyl esters
PT108370B (pt) * 2015-03-30 2018-10-25 Hovione Farm S A Processo de preparação de brometo de aclidínio
EP3248970A1 (en) 2016-05-27 2017-11-29 Zentiva K.S. Forms of umeclidinium bromide
PT109740B (pt) * 2016-11-14 2020-07-30 Hovione Farmaciencia Sa Processo para a preparação de brometo de umeclidínio
CN108069956B (zh) * 2016-11-18 2021-03-16 扬州奥锐特药业有限公司 1-氮杂双环[2,2,2]辛-4-基苯基酮化合物及其制备方法和应用
IT201700058796A1 (it) * 2017-05-30 2018-11-30 Olon Spa Procedimento per la preparazione di un nuovo intermedio di sintesi dell’umeclidinio.
CN107935917A (zh) * 2017-10-30 2018-04-20 广东莱佛士制药技术有限公司 一种1‑(2‑氯乙基)‑4‑哌啶甲酸酯的合成方法
CN109956938A (zh) * 2017-12-26 2019-07-02 天津金耀集团有限公司 乌美溴铵中间体晶型及其制备方法和以该中间体制备乌美溴铵的方法
CN108558860B (zh) * 2018-06-04 2020-12-25 成都伊诺达博医药科技有限公司 一种合成芜地溴铵的方法
PT115583B (pt) * 2019-06-17 2022-05-02 Hovione Farm S A Processo contínuo para a preparação de medicamentos anticolinérgicos
PT117440B (pt) 2021-09-03 2024-04-26 Hovione Farm S A Processo para a preparação de aminas cíclicas cloroaquilo substituídas
WO2024251812A1 (en) 2023-06-07 2024-12-12 Pharmazell Gmbh A process for the preparation of umeclidinium bromide intermediate
CN117310022B (zh) * 2023-09-22 2024-05-17 山东泰合医药科技有限公司 一种分离和检测乌美溴铵中间体奎宁环二苯甲醇有关物质的方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1976701A (zh) * 2004-04-27 2007-06-06 葛兰素集团有限公司 毒蕈碱性乙酰胆碱受体拮抗剂
WO2012106190A1 (en) * 2011-01-31 2012-08-09 Bristol-Myers Squibb Company C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity

Family Cites Families (6)

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Publication number Priority date Publication date Assignee Title
US3998832A (en) * 1975-04-16 1976-12-21 G. D. Searle & Co. Anti-diarrheal compounds
US4540780A (en) * 1983-06-02 1985-09-10 Warner-Lambert Company Diphenylmethylene piperidines
FR2816618B1 (fr) * 2000-11-15 2002-12-27 Aventis Pharma Sa Derives heterocyclylalcoyl piperidine, leur preparation et les compositions qui les contiennent
GB0519879D0 (en) * 2005-09-30 2005-11-09 Astrazeneca Ab Chemical process
JP4841279B2 (ja) * 2006-03-23 2011-12-21 一般財団法人 化学物質評価研究機構 被検物質の発がん性予測方法
WO2011029896A1 (en) 2009-09-11 2011-03-17 Glaxo Group Limited Methods of preparation of muscarinic acetylcholine receptor antagonists

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1976701A (zh) * 2004-04-27 2007-06-06 葛兰素集团有限公司 毒蕈碱性乙酰胆碱受体拮抗剂
WO2012106190A1 (en) * 2011-01-31 2012-08-09 Bristol-Myers Squibb Company C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Discovery of Novel 1-Azoniabicyclo[2.2.2]octane Muscarinic Acetylcholine Receptor Antagonists;Dramane I.Laine等;《J. Med. Chem.》;20090324;第52卷(第8期);第2495、2500-2501页 *

Also Published As

Publication number Publication date
EP3401316B1 (en) 2021-08-04
CA2881935A1 (en) 2014-02-20
US20150232423A1 (en) 2015-08-20
ES2678697T3 (es) 2018-08-16
WO2014027045A1 (en) 2014-02-20
JP2015524832A (ja) 2015-08-27
US9273001B2 (en) 2016-03-01
RU2644160C2 (ru) 2018-02-08
RU2015104269A (ru) 2016-10-10
US9657011B2 (en) 2017-05-23
JP2018203752A (ja) 2018-12-27
US20160159786A1 (en) 2016-06-09
BR112015003101B1 (pt) 2022-06-14
AU2013304102B2 (en) 2016-09-01
ES2893473T3 (es) 2022-02-09
AU2016213768A1 (en) 2016-09-01
EP2885298A1 (en) 2015-06-24
IN2015KN00323A (enAn) 2015-07-10
CN107163038A (zh) 2017-09-15
CN104619706A (zh) 2015-05-13
JP6799037B2 (ja) 2020-12-09
JP6389174B2 (ja) 2018-09-12
EP3401316A1 (en) 2018-11-14
CN104619706B (zh) 2017-06-20
AU2016262787A1 (en) 2016-12-15
EP2885298B1 (en) 2018-06-13
AU2016213768B2 (en) 2018-01-04
KR20150043465A (ko) 2015-04-22
BR112015003101A2 (pt) 2017-07-04
AU2013304102A1 (en) 2015-02-26

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