WO2021010681A3 - (3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 및 이에 사용되는 중간체의 제조방법 - Google Patents

(3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 및 이에 사용되는 중간체의 제조방법 Download PDF

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Publication number
WO2021010681A3
WO2021010681A3 PCT/KR2020/009130 KR2020009130W WO2021010681A3 WO 2021010681 A3 WO2021010681 A3 WO 2021010681A3 KR 2020009130 W KR2020009130 W KR 2020009130W WO 2021010681 A3 WO2021010681 A3 WO 2021010681A3
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WO
WIPO (PCT)
Prior art keywords
preparing
hydroxymethylphenylamino
pyrrole
carbonyl
isopropyl
Prior art date
Application number
PCT/KR2020/009130
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English (en)
French (fr)
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WO2021010681A2 (ko
Inventor
박은정
정서희
박상욱
이원일
손세일
유진호
Original Assignee
대원제약주식회사
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Priority to CN202080049765.8A priority Critical patent/CN114096523A/zh
Publication of WO2021010681A2 publication Critical patent/WO2021010681A2/ko
Publication of WO2021010681A3 publication Critical patent/WO2021010681A3/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/337—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

본 발명은(3R,5R)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시 메틸 페닐 아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법을 제공한다. 본 발명의 제조방법은 (3R,5R)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 주요 구조부들 각각을 개별적으로 합성한 후 커플링 하는 수렴합성 방식으로 수행된다. 이에 따라, 유연물질을 용이하게 제어하고 제조시간을 단축시킬 수 있어 화합물의 생산성을 향상시킬 수 있고, 최종 화합물의 수율 또한 높일 수 있다.
PCT/KR2020/009130 2019-07-12 2020-07-10 (3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 및 이에 사용되는 중간체의 제조방법 WO2021010681A2 (ko)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202080049765.8A CN114096523A (zh) 2019-07-12 2020-07-10 制备(3r,5r)-7-(2-(4-氟苯基)-5-异丙基-3-苯基-4-((4-羟甲基苯基氨基)羰基)-吡咯-1-基)-3,5-二羟基庚酸半钙盐的方法以及制备其所用中间体的方法

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020190084527A KR102218320B1 (ko) 2019-07-12 2019-07-12 (3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 및 이에 사용되는 중간체의 제조방법
KR10-2019-0084527 2019-07-12

Publications (2)

Publication Number Publication Date
WO2021010681A2 WO2021010681A2 (ko) 2021-01-21
WO2021010681A3 true WO2021010681A3 (ko) 2021-03-11

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2020/009130 WO2021010681A2 (ko) 2019-07-12 2020-07-10 (3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 및 이에 사용되는 중간체의 제조방법

Country Status (3)

Country Link
KR (1) KR102218320B1 (ko)
CN (1) CN114096523A (ko)
WO (1) WO2021010681A2 (ko)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004106299A2 (en) * 2003-05-30 2004-12-09 Ranbaxy Laboratories Limited Substituted pyrrole derivatives and their use as hmg-co inhibitors
US20080153896A1 (en) * 2006-07-14 2008-06-26 Gyan Chand Yadav Polymorphic Forms of an HMG-CoA Reductase Inhibitor and Uses Thereof
KR101329112B1 (ko) * 2005-11-08 2013-11-14 랜박시 래보러터리스 리미티드 (3ｒ,5ｒ)-7-〔2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-〔(4-히드록시 메틸 페닐 아미노)카르보닐〕-피롤-1-일〕-3,5-디히드록시 헵탄산 헤미 칼슘염의 제조 방법
KR20160117843A (ko) * 2015-03-31 2016-10-11 대원제약주식회사 결정형 및 이의 제조방법
CN106397296A (zh) * 2016-08-29 2017-02-15 江苏阿尔法药业有限公司 一种阿托伐他汀的制备工艺

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1980890A (zh) * 2004-05-31 2007-06-13 兰贝克赛实验室有限公司 阿托伐他汀的制备方法
CN101304968A (zh) * 2005-11-08 2008-11-12 兰贝克赛实验室有限公司 (3r,5r)-7-[2-(4-氟苯基)-5-异丙基-3-苯基-4-[(4-羟甲基苯基氨基)羰基]-吡咯-1-基]-3,5-二羟基庚酸半钙盐的制备方法
CN102382006A (zh) * 2011-11-11 2012-03-21 连云港宏业化工有限公司 2-[2-（4-氟苯基）-2-氧代-1-苯基乙基]-4-甲基-3-氧代-n-苯基戊酰胺的合成方法
KR102001835B1 (ko) * 2018-08-24 2019-07-19 대원제약주식회사 (3r,5r)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시메틸페닐아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 이에 사용되는 중간체, 및 중간체의 제조방법

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004106299A2 (en) * 2003-05-30 2004-12-09 Ranbaxy Laboratories Limited Substituted pyrrole derivatives and their use as hmg-co inhibitors
KR101329112B1 (ko) * 2005-11-08 2013-11-14 랜박시 래보러터리스 리미티드 (3ｒ,5ｒ)-7-〔2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-〔(4-히드록시 메틸 페닐 아미노)카르보닐〕-피롤-1-일〕-3,5-디히드록시 헵탄산 헤미 칼슘염의 제조 방법
US20080153896A1 (en) * 2006-07-14 2008-06-26 Gyan Chand Yadav Polymorphic Forms of an HMG-CoA Reductase Inhibitor and Uses Thereof
KR20160117843A (ko) * 2015-03-31 2016-10-11 대원제약주식회사 결정형 및 이의 제조방법
CN106397296A (zh) * 2016-08-29 2017-02-15 江苏阿尔法药业有限公司 一种阿托伐他汀的制备工艺

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Publication number Publication date
CN114096523A (zh) 2022-02-25
KR102218320B1 (ko) 2021-02-23
WO2021010681A2 (ko) 2021-01-21
KR20210008263A (ko) 2021-01-21

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