WO2017188644A3 - 트레프로스티닐의 제조방법 및 이를 위한 중간체 - Google Patents

트레프로스티닐의 제조방법 및 이를 위한 중간체 Download PDF

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Publication number
WO2017188644A3
WO2017188644A3 PCT/KR2017/004131 KR2017004131W WO2017188644A3 WO 2017188644 A3 WO2017188644 A3 WO 2017188644A3 KR 2017004131 W KR2017004131 W KR 2017004131W WO 2017188644 A3 WO2017188644 A3 WO 2017188644A3
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WO
WIPO (PCT)
Prior art keywords
intermediate therefor
preparing treprostinil
treprostinil
preparing
therefor
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PCT/KR2017/004131
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English (en)
French (fr)
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WO2017188644A2 (ko
Inventor
신현익
이효선
이경진
이기영
오창영
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연성정밀화학(주)
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Application filed by 연성정밀화학(주) filed Critical 연성정밀화학(주)
Priority to EP17789829.3A priority Critical patent/EP3450421B1/en
Priority to JP2018556315A priority patent/JP6837494B2/ja
Priority to CN201780026219.0A priority patent/CN109071406B/zh
Priority to US16/096,766 priority patent/US10800737B2/en
Publication of WO2017188644A2 publication Critical patent/WO2017188644A2/ko
Publication of WO2017188644A3 publication Critical patent/WO2017188644A3/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C29/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
    • C07C29/56—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by isomerisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C405/00—Compounds containing a five-membered ring having two side-chains in ortho position to each other, and having oxygen atoms directly attached to the ring in ortho position to one of the side-chains, one side-chain containing, not directly attached to the ring, a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, and the other side-chain having oxygen atoms attached in gamma-position to the ring, e.g. prostaglandins ; Analogues or derivatives thereof
    • C07C405/005—Analogues or derivatives having the five membered ring replaced by other rings
    • C07C405/0075—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system
    • C07C405/0083—Analogues or derivatives having the five membered ring replaced by other rings having the side-chains or their analogues or derivatives attached to a condensed ring system which is only ortho or peri condensed, e.g. carbacyclins
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J31/00—Catalysts comprising hydrides, coordination complexes or organic compounds
    • B01J31/02—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides
    • B01J31/12—Catalysts comprising hydrides, coordination complexes or organic compounds containing organic compounds or metal hydrides containing organo-metallic compounds or metal hydrides
    • B01J31/122—Metal aryl or alkyl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C29/00—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring
    • C07C29/62—Preparation of compounds having hydroxy or O-metal groups bound to a carbon atom not belonging to a six-membered aromatic ring by introduction of halogen; by substitution of halogen atoms by other halogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/22—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system
    • C07C35/37—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring polycyclic, at least one hydroxy group bound to a condensed ring system with a hydroxy group on a condensed system having three rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/09—Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid esters or lactones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/30—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
    • C07C67/333—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton
    • C07C67/343—Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/44—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 ortho- or peri-condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B51/00—Introduction of protecting groups or activating groups, not provided for in the preceding groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2603/00—Systems containing at least three condensed rings
    • C07C2603/02—Ortho- or ortho- and peri-condensed systems
    • C07C2603/04—Ortho- or ortho- and peri-condensed systems containing three rings
    • C07C2603/06—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members
    • C07C2603/10—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings
    • C07C2603/12—Ortho- or ortho- and peri-condensed systems containing three rings containing at least one ring with less than six ring members containing five-membered rings only one five-membered ring
    • C07C2603/14—Benz[f]indenes; Hydrogenated benz[f]indenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C59/00—Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C59/40—Unsaturated compounds
    • C07C59/58—Unsaturated compounds containing ether groups, groups, groups, or groups
    • C07C59/72—Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Materials Engineering (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

본 발명은 고순도의 트레프로스티닐을 경제적이고 효율적으로 제조하는 방법 및 이를 위한 중간체에 관한 것이다.
PCT/KR2017/004131 2016-04-28 2017-04-18 트레프로스티닐의 제조방법 및 이를 위한 중간체 WO2017188644A2 (ko)

Priority Applications (4)

Application Number Priority Date Filing Date Title
EP17789829.3A EP3450421B1 (en) 2016-04-28 2017-04-18 Method for preparing treprostinil and intermediate therefor
JP2018556315A JP6837494B2 (ja) 2016-04-28 2017-04-18 トレプロスチニルの製造方法及びそのための中間体
CN201780026219.0A CN109071406B (zh) 2016-04-28 2017-04-18 制备曲前列环素的方法及用于其的中间体
US16/096,766 US10800737B2 (en) 2016-04-28 2017-04-18 Method for preparing treprostinil and intermediate therefor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2016-0052378 2016-04-28
KR1020160052378A KR101830693B1 (ko) 2016-04-28 2016-04-28 트레프로스티닐의 제조방법 및 이를 위한 중간체

Publications (2)

Publication Number Publication Date
WO2017188644A2 WO2017188644A2 (ko) 2017-11-02
WO2017188644A3 true WO2017188644A3 (ko) 2018-01-18

Family

ID=60159843

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2017/004131 WO2017188644A2 (ko) 2016-04-28 2017-04-18 트레프로스티닐의 제조방법 및 이를 위한 중간체

Country Status (6)

Country Link
US (1) US10800737B2 (ko)
EP (1) EP3450421B1 (ko)
JP (1) JP6837494B2 (ko)
KR (1) KR101830693B1 (ko)
CN (1) CN109071406B (ko)
WO (1) WO2017188644A2 (ko)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4306076A (en) * 1980-04-23 1981-12-15 The Upjohn Company Inter-phenylene CBA compounds
CN101891596A (zh) * 2009-05-22 2010-11-24 上海天伟生物制药有限公司 一种新化合物及其制备方法和用途
WO2014203278A2 (en) * 2013-06-19 2014-12-24 Msn Laboratories Private Limited NOVEL PROCESS FOR THE PREPARATION OF (1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-HEXAHYDRO-2-HYDROXY-1-[(3S)-3-HYDROXYOCTYL]-1H-BENZ[f]INDEN-5-YL]OXY]ACETIC ACID
WO2015073314A1 (en) * 2013-11-13 2015-05-21 Cayman Chemical Company Incorporated Amine salts of a prostacyclin analog
WO2016055819A1 (en) * 2014-10-08 2016-04-14 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Process for the preparation of treprostinil

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1201712A (en) 1980-02-28 1986-03-11 Paul A. Aristoff Carbacyclin analogs
US4306075A (en) 1980-03-28 1981-12-15 The Upjohn Company Composition and process
KR100437873B1 (ko) 2001-05-08 2004-06-26 연성정밀화학(주) 프로스타글란딘 유도체의 제조방법 및 그의 입체특이적출발물질
KR100903311B1 (ko) * 2002-09-18 2009-06-17 연성정밀화학(주) 프로스타글란딘 유도체의 제조방법 및 그를 위한 출발물질
KR101868166B1 (ko) * 2010-06-03 2018-06-15 유나이티드 세러퓨틱스 코오포레이션 트레프로스티닐의 제조
US8524939B2 (en) 2011-08-24 2013-09-03 Chirogate International Inc. Intermediates for the synthesis of benzindene prostaglandins and preparations thereof
HUE034485T2 (en) * 2012-06-15 2018-02-28 Scipharm Sarl Process for the preparation of treprostinil and its derivatives

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4306076A (en) * 1980-04-23 1981-12-15 The Upjohn Company Inter-phenylene CBA compounds
CN101891596A (zh) * 2009-05-22 2010-11-24 上海天伟生物制药有限公司 一种新化合物及其制备方法和用途
WO2014203278A2 (en) * 2013-06-19 2014-12-24 Msn Laboratories Private Limited NOVEL PROCESS FOR THE PREPARATION OF (1R,2R,3aS,9aS)-[[2,3,3a,4,9,9a-HEXAHYDRO-2-HYDROXY-1-[(3S)-3-HYDROXYOCTYL]-1H-BENZ[f]INDEN-5-YL]OXY]ACETIC ACID
WO2015073314A1 (en) * 2013-11-13 2015-05-21 Cayman Chemical Company Incorporated Amine salts of a prostacyclin analog
WO2016055819A1 (en) * 2014-10-08 2016-04-14 CHINOIN Gyógyszer és Vegyészeti Termékek Gyára Zrt. Process for the preparation of treprostinil

Also Published As

Publication number Publication date
KR20170123126A (ko) 2017-11-07
CN109071406A (zh) 2018-12-21
JP6837494B2 (ja) 2021-03-03
EP3450421B1 (en) 2020-11-18
US10800737B2 (en) 2020-10-13
KR101830693B1 (ko) 2018-02-21
WO2017188644A2 (ko) 2017-11-02
EP3450421A2 (en) 2019-03-06
EP3450421A4 (en) 2019-12-04
JP2019514911A (ja) 2019-06-06
US20190119205A1 (en) 2019-04-25
CN109071406B (zh) 2021-05-04

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