JP6188960B2 - ブレクスピプラゾール、重要な中間体およびその塩の製造方法 - Google Patents

ブレクスピプラゾール、重要な中間体およびその塩の製造方法 Download PDF

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JP6188960B2
JP6188960B2 JP2016548404A JP2016548404A JP6188960B2 JP 6188960 B2 JP6188960 B2 JP 6188960B2 JP 2016548404 A JP2016548404 A JP 2016548404A JP 2016548404 A JP2016548404 A JP 2016548404A JP 6188960 B2 JP6188960 B2 JP 6188960B2
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acid
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JP2016535081A (ja
JP2016535081A5 (enExample
Inventor
正 劉
正 劉
春暉 呉
春暉 呉
永建 柳
永建 柳
容霞 張
容霞 張
洋 何
洋 何
広輝 田
広輝 田
敬山 瀋
敬山 瀋
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Shanghai Institute of Materia Medica of CAS
Vigonvita Life Sciences Co Ltd
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Shanghai Institute of Materia Medica of CAS
Suzhou Vigonvita Life Sciences Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2016548404A 2013-10-18 2014-10-20 ブレクスピプラゾール、重要な中間体およびその塩の製造方法 Active JP6188960B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201310493206.8 2013-10-18
CN201310493206.8A CN104557896A (zh) 2013-10-18 2013-10-18 布瑞哌唑、其关键中间体及其盐的制备方法
PCT/CN2014/000921 WO2015054976A1 (zh) 2013-10-18 2014-10-20 布瑞哌唑、其关键中间体及其盐的制备方法

Publications (3)

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JP2016535081A JP2016535081A (ja) 2016-11-10
JP2016535081A5 JP2016535081A5 (enExample) 2017-08-03
JP6188960B2 true JP6188960B2 (ja) 2017-08-30

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JP2016548404A Active JP6188960B2 (ja) 2013-10-18 2014-10-20 ブレクスピプラゾール、重要な中間体およびその塩の製造方法

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Country Link
US (1) US10100044B2 (enExample)
EP (1) EP3059237A4 (enExample)
JP (1) JP6188960B2 (enExample)
CN (2) CN104557896A (enExample)
WO (1) WO2015054976A1 (enExample)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105732572A (zh) * 2014-12-10 2016-07-06 苏州鹏旭医药科技有限公司 一种Brexpiprazole中间体的制备方法及Brexpiprazole中间体
CN105985314A (zh) * 2015-02-05 2016-10-05 苏州旺山旺水生物医药有限公司 布瑞哌唑类似物的制备方法
CN104844586A (zh) * 2015-04-16 2015-08-19 重庆医药工业研究院有限责任公司 一种依匹哌唑无定型物及其制备方法
CN104829588B (zh) * 2015-04-30 2017-03-29 苏州苏旺森生物医药科技有限公司 一种苯并[b]噻吩的制备方法及其中间体
CN105061414B (zh) * 2015-07-21 2019-01-01 杭州新博思生物医药有限公司 一锅法制备Brexpiprazole
WO2017025987A1 (en) * 2015-08-11 2017-02-16 Mylan Laboratories Limited Process for the preparation of brexpiprazole
EP3150591A1 (en) 2015-10-02 2017-04-05 Crystal Pharma S.A.U Process and intermediates for the preparation of benzo[b]thiophene compounds
WO2017078621A1 (en) * 2015-11-03 2017-05-11 Scinopharm Taiwan, Ltd. Processes for preparing brexpiprazole
CN105461704A (zh) * 2015-12-15 2016-04-06 南京艾德凯腾生物医药有限责任公司 一种依匹哌唑的制备方法
US10464931B2 (en) 2015-12-28 2019-11-05 Honour (R&D) Process for the preparation of Quinolin-2(1H)-one derivatives
CN106938982A (zh) * 2016-01-05 2017-07-11 连云港皓海医药科技有限公司 布瑞哌唑的制备方法及用于制备布瑞哌唑的化合物
CN105399736B (zh) * 2016-01-07 2018-10-19 安徽省逸欣铭医药科技有限公司 一种依匹哌唑新的制备方法
US20170320862A1 (en) 2016-05-03 2017-11-09 Cadila Healthcare Limited Process for the preparation of brexpiprazole and intermediates thereof
CN106645494B (zh) * 2016-12-29 2019-09-06 成都百裕制药股份有限公司 依匹哌唑起始物料有关物质的检测方法
WO2020087031A1 (en) 2018-10-26 2020-04-30 The Research Foundation For The State University Of New York Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia
CN109694343B (zh) * 2018-12-19 2020-07-28 帕潘纳(北京)科技有限公司 一种杂环羧酸类化合物的脱羧方法
CN110483476B (zh) * 2019-08-15 2020-11-27 绍兴文理学院 一种催化法制备苯并硒吩类化合物的工艺
CN110483475B (zh) * 2019-08-15 2020-11-27 绍兴文理学院 一种氧化银催化法制备苯并噻吩类化合物的方法
CN111423452B (zh) * 2020-03-26 2023-08-22 江西青峰药业有限公司 瑞卢戈利的中间体及其制备方法和应用
CN115894435B (zh) * 2022-11-14 2024-11-22 山东厚德精诚药业有限公司 一种1-(苯并[b]噻吩-4-基)哌嗪盐酸盐的合成方法
CN116969960A (zh) * 2023-07-25 2023-10-31 乳源东阳光药业有限公司 酪氨酸激酶抑制剂的中间体的制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4977154A (en) * 1985-12-12 1990-12-11 Warner-Lambert Company 5-amino and 5-hydroxy-6-fluoroquinolones as antibacterial agents
US5436246A (en) * 1992-09-17 1995-07-25 Merrell Dow Pharmaceuticals Inc. Serotonin receptor agents
MX2007001106A (es) * 2004-07-28 2007-03-15 Glaxo Group Ltd Derivados de piperazina utiles para el tratamiento de trastornos gastrointestinales.
JP4315393B2 (ja) * 2005-04-14 2009-08-19 大塚製薬株式会社 複素環化合物
TWI320783B (en) * 2005-04-14 2010-02-21 Otsuka Pharma Co Ltd Heterocyclic compound
JP4540700B2 (ja) * 2006-10-13 2010-09-08 大塚製薬株式会社 医薬
JP2011136906A (ja) * 2008-04-18 2011-07-14 Otsuka Pharmaceut Co Ltd 複素環化合物
KR101911121B1 (ko) * 2011-07-28 2018-10-23 오쓰까 세이야꾸 가부시키가이샤 벤조[b]티오펜 화합물의 제조 방법
CN104892589A (zh) * 2014-03-07 2015-09-09 中国科学院上海药物研究所 一类杂环化合物、其制备方法和用途

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Publication number Publication date
CN104557896A (zh) 2015-04-29
CN105473579B (zh) 2018-04-13
EP3059237A1 (en) 2016-08-24
CN105473579A (zh) 2016-04-06
EP3059237A4 (en) 2016-08-24
JP2016535081A (ja) 2016-11-10
WO2015054976A1 (zh) 2015-04-23
US20160272624A1 (en) 2016-09-22
US10100044B2 (en) 2018-10-16

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