WO2014183730A3 - 一种他达那非的制备方法 - Google Patents

一种他达那非的制备方法 Download PDF

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Publication number
WO2014183730A3
WO2014183730A3 PCT/CN2014/082175 CN2014082175W WO2014183730A3 WO 2014183730 A3 WO2014183730 A3 WO 2014183730A3 CN 2014082175 W CN2014082175 W CN 2014082175W WO 2014183730 A3 WO2014183730 A3 WO 2014183730A3
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WO
WIPO (PCT)
Prior art keywords
ring closure
tadalafil
chloroacetylation
condensation
solvent during
Prior art date
Application number
PCT/CN2014/082175
Other languages
English (en)
French (fr)
Other versions
WO2014183730A2 (zh
Inventor
赵金召
张梅
彭学东
王龙
Original Assignee
张家港威胜生物医药有限公司
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.)
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Publication date
Application filed by 张家港威胜生物医药有限公司 filed Critical 张家港威胜生物医药有限公司
Publication of WO2014183730A2 publication Critical patent/WO2014183730A2/zh
Publication of WO2014183730A3 publication Critical patent/WO2014183730A3/zh

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    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Indole Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

公开了一种他达那非的制备方法，所述方法以D-色氨酸甲酯盐酸盐、胡椒醛为起始原料，依次经过缩合环合、氯乙酰化、胺解环合反应，得到他达那非。在所述方法中，缩合环合反应采用异丙醇或硝基甲烷作溶剂，氯乙酰化反应以乙酸乙酯作溶剂。
PCT/CN2014/082175 2013-05-14 2014-07-14 一种他达那非的制备方法 WO2014183730A2 (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201310175955.6 2013-05-14
CN2013101759556A CN103232451A (zh) 2013-05-14 2013-05-14 一种他达那非的简易制备工艺

Publications (2)

Publication Number Publication Date
WO2014183730A2 WO2014183730A2 (zh) 2014-11-20
WO2014183730A3 true WO2014183730A3 (zh) 2015-01-08

Family

ID=48880531

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2014/082175 WO2014183730A2 (zh) 2013-05-14 2014-07-14 一种他达那非的制备方法

Country Status (2)

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CN (1) CN103232451A (zh)
WO (1) WO2014183730A2 (zh)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103232451A (zh) * 2013-05-14 2013-08-07 张家港威胜生物医药有限公司 一种他达那非的简易制备工艺
CN104140424B (zh) * 2014-07-23 2015-10-28 齐鲁天和惠世制药有限公司 一种制备他达拉非的方法
CN105753763A (zh) * 2014-12-18 2016-07-13 广州医药研究总院有限公司 他达那非中间体的制备方法
CN105503866B (zh) * 2015-12-31 2018-05-08 湖南千金湘江药业股份有限公司 酰化物中间体及其合成方法和在制备他达拉非方面的应用
CN105541835B (zh) * 2015-12-31 2017-12-05 湖南千金湘江药业股份有限公司 顺式四氢咔啉中间体及其合成方法和在制备他达拉非方面的应用
CN105541840B (zh) * 2015-12-31 2017-12-05 湖南千金湘江药业股份有限公司 关键中间体及其合成方法和在制备他达拉非方面的应用
CN105524062B (zh) * 2015-12-31 2018-01-30 湖南千金湘江药业股份有限公司 他达拉非的合成方法
CN106977516B (zh) * 2017-03-02 2019-06-18 山东裕欣药业有限公司 一种他达拉非的制备方法
RU2692764C1 (ru) * 2019-04-26 2019-06-27 Общество с ограниченной ответственностью "Балтфарма" Способ получения тадалафила
CN110606847A (zh) * 2019-07-30 2019-12-24 中国医药集团总公司四川抗菌素工业研究所 一种他达拉非顺式中间体的制备方法及其应用
CN110804055B (zh) * 2019-11-27 2020-09-29 株洲千金药业股份有限公司 一种他达拉非杂质g的制备方法
CN110790764B (zh) * 2019-11-27 2021-04-06 四川省通园制药集团有限公司 一种一锅法制备他达拉非的方法
CN114437070A (zh) * 2022-01-19 2022-05-06 广西-东盟食品检验检测中心 一种他达拉非新型衍生物的制备方法

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5859006A (en) * 1994-01-21 1999-01-12 Icos Corporation Tetracyclic derivatives; process of preparation and use
CN101155809A (zh) * 2005-04-12 2008-04-02 特瓦制药工业有限公司 他达那非中间体的制备
CN103232451A (zh) * 2013-05-14 2013-08-07 张家港威胜生物医药有限公司 一种他达那非的简易制备工艺

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20090113346A (ko) * 2005-02-25 2009-10-29 테바 파마슈티컬 인더스트리즈 리미티드 입도가 큰 타달라필 및 이의 제조 방법

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5859006A (en) * 1994-01-21 1999-01-12 Icos Corporation Tetracyclic derivatives; process of preparation and use
CN101155809A (zh) * 2005-04-12 2008-04-02 特瓦制药工业有限公司 他达那非中间体的制备
CN103232451A (zh) * 2013-05-14 2013-08-07 张家港威胜生物医药有限公司 一种他达那非的简易制备工艺

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
YU , YINGHUI ET AL.: "Diastereoselective Synthesis of Tadalafil", CHEMICAL WORLD, vol. 48, no. 8, 25 August 2007 (2007-08-25), pages 483 - 486, XP009158498 *

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Publication number Publication date
CN103232451A (zh) 2013-08-07
WO2014183730A2 (zh) 2014-11-20

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