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FR3087439B1 - Procédé pour la préparation de 3α-hydroxy-5α-prégnan-20-one (brexanolone) - Google Patents

Procédé pour la préparation de 3α-hydroxy-5α-prégnan-20-one (brexanolone) Download PDF

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Publication number
FR3087439B1
FR3087439B1 FR1911134A FR1911134A FR3087439B1 FR 3087439 B1 FR3087439 B1 FR 3087439B1 FR 1911134 A FR1911134 A FR 1911134A FR 1911134 A FR1911134 A FR 1911134A FR 3087439 B1 FR3087439 B1 FR 3087439B1
Authority
FR
France
Prior art keywords
brexanolone
pregnan
hydroxy
preparation
synthesis
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
FR1911134A
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English (en)
Other versions
FR3087439A1 (fr
Inventor
Claudio Delfrate
Davide Rigamonti
Tea Borelli
Roberto Lenna
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Industriale Chimica SRL
Original Assignee
Industriale Chimica SRL
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.)
Filing date
Publication date
Application filed by Industriale Chimica SRL filed Critical Industriale Chimica SRL
Publication of FR3087439A1 publication Critical patent/FR3087439A1/fr
Application granted granted Critical
Publication of FR3087439B1 publication Critical patent/FR3087439B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J33/00—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002—Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne un nouveau procédé pour la synthèse de 3α-hydroxy-5α-prégnan-20-one, couramment appelée brexanolone, de formule (1) présentée ci-dessous :
FR1911134A 2018-10-22 2019-10-08 Procédé pour la préparation de 3α-hydroxy-5α-prégnan-20-one (brexanolone) Active FR3087439B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT102018000009683A IT201800009683A1 (it) 2018-10-22 2018-10-22 Processo per la preparazione di 3α-idrossi-5α-pregnan-20-one (brexanolone)
IT102018000009683 2018-10-22

Publications (2)

Publication Number Publication Date
FR3087439A1 FR3087439A1 (fr) 2020-04-24
FR3087439B1 true FR3087439B1 (fr) 2022-12-23

Family

ID=65324443

Family Applications (1)

Application Number Title Priority Date Filing Date
FR1911134A Active FR3087439B1 (fr) 2018-10-22 2019-10-08 Procédé pour la préparation de 3α-hydroxy-5α-prégnan-20-one (brexanolone)

Country Status (13)

Country Link
US (1) US12077559B2 (fr)
CN (1) CN112888701B (fr)
AR (1) AR116790A1 (fr)
AU (1) AU2019369041B2 (fr)
BR (1) BR112021007009A2 (fr)
CA (1) CA3116467A1 (fr)
CH (1) CH716822B1 (fr)
DE (1) DE112019005261T5 (fr)
ES (1) ES2837136B2 (fr)
FR (1) FR3087439B1 (fr)
GB (1) GB2593352B (fr)
IT (1) IT201800009683A1 (fr)
WO (1) WO2020083839A1 (fr)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT202000021316A1 (it) 2020-09-09 2022-03-09 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI (3α,5α)-3-IDROSSI-3-METIL-PREGNAN-20-ONE (GANAXOLONE)
CN112501235B (zh) * 2020-11-19 2022-12-02 华东师范大学 一种利用单烯醇酮醋酸酯制备布瑞诺龙的方法
CN112516086B (zh) * 2020-12-08 2022-05-20 武汉久安药物研究院有限公司 注射用布瑞诺龙脂肪乳及其制备方法
CN114031660A (zh) * 2021-11-24 2022-02-11 南京迈诺威医药科技有限公司 一种17α-孕烯醇酮的制备方法
CN113861255B (zh) * 2021-11-24 2022-09-02 南京迈诺威医药科技有限公司 一种别孕烷醇酮有关物质的制备方法
IT202100030671A1 (it) 2021-12-03 2023-06-03 Ind Chimica Srl PROCESSO PER LA PREPARAZIONE DI (3a,5a)-20-OSSOPREGNAN-3-IL GLICIL-L-VALINATO CLORIDRATO
CN115806577A (zh) * 2023-02-03 2023-03-17 北京鑫开元医药科技有限公司 一种布瑞诺龙的制备方法

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB442319A (en) 1933-12-23 1936-02-06 Schering Kahlbaum Ag Process for the production of pregnanolones
US3152121A (en) * 1962-03-16 1964-10-06 Upjohn Co 20-ketals of 3-hydroxy-5 beta-pregnan-20-one
FR2720747B1 (fr) * 1994-06-02 1996-07-12 Roussel Uclaf Nouveau procédé de préparation d'un stéroïde 16béta-méthyl et nouveaux intermédiaires.
US5795985A (en) * 1996-03-05 1998-08-18 Ciba Specialty Chemicals Corporation Phenyl alkyl ketone substituted by cyclic amine and a process for the preparation thereof
NZ597940A (en) * 2009-08-13 2013-03-28 Marinus Pharmaceuticals Inc Method for making 3alpha-hydroxy, 3beta- methyl-5alpha-pregnan-20-one (ganaxolone)
FR2973031B1 (fr) 2011-03-23 2013-11-29 Univ Strasbourg Derives de l'allopregnanolone et de l'epiallopregnanolone et leurs utilisations pour traiter un etat neuropathologique
US9038590B2 (en) 2012-12-09 2015-05-26 Crossroads Machine, Inc. Adjustable venturi mixing valve assembly

Also Published As

Publication number Publication date
GB202106894D0 (en) 2021-06-30
BR112021007009A2 (pt) 2021-07-13
CN112888701A (zh) 2021-06-01
IT201800009683A1 (it) 2020-04-22
DE112019005261T5 (de) 2021-07-01
US20210388020A1 (en) 2021-12-16
CN112888701B (zh) 2025-02-28
AU2019369041A1 (en) 2021-06-10
ES2837136A2 (es) 2021-06-29
GB2593352A (en) 2021-09-22
AR116790A1 (es) 2021-06-16
CA3116467A1 (fr) 2020-04-30
GB2593352B (en) 2022-07-27
CH716822B1 (it) 2023-01-13
ES2837136R1 (es) 2023-08-18
ES2837136B2 (es) 2024-02-12
US12077559B2 (en) 2024-09-03
FR3087439A1 (fr) 2020-04-24
WO2020083839A1 (fr) 2020-04-30
AU2019369041B2 (en) 2024-06-27

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