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WO2013034780A3 - Process for the preparation of estetrol and related compounds - Google Patents

Process for the preparation of estetrol and related compounds Download PDF

Info

Publication number
WO2013034780A3
WO2013034780A3 PCT/EP2012/076358 EP2012076358W WO2013034780A3 WO 2013034780 A3 WO2013034780 A3 WO 2013034780A3 EP 2012076358 W EP2012076358 W EP 2012076358W WO 2013034780 A3 WO2013034780 A3 WO 2013034780A3
Authority
WO
WIPO (PCT)
Prior art keywords
estetrol
preparation
formula
related compounds
solvate
Prior art date
Application number
PCT/EP2012/076358
Other languages
French (fr)
Other versions
WO2013034780A2 (en
Inventor
Juan José FERREIRO GIL
Jesús Miguel IGLESIAS RETUERTO
Francisco Javier GALLO NIETO
Original Assignee
Crystal Pharma, S.A.U.
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 Crystal Pharma, S.A.U. filed Critical Crystal Pharma, S.A.U.
Priority to PCT/EP2012/076358 priority Critical patent/WO2013034780A2/en
Publication of WO2013034780A2 publication Critical patent/WO2013034780A2/en
Publication of WO2013034780A3 publication Critical patent/WO2013034780A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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

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

The invention relates to a process for obtaining Estetrol and derivatives thereof of formula (I) or a salt or solvate thereof, wherein R represents H or anhydroxyl protecting group; the process comprising reacting a compound of formula (II) or a salt or solvate thereof, wherein R is as defined previously, with an oxidizing agent; the invention also relates to said 3-OH protected derivatives of formula (I) and intermediate products useful in the process.
PCT/EP2012/076358 2012-12-20 2012-12-20 Process for the preparation of estetrol and related compounds WO2013034780A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/EP2012/076358 WO2013034780A2 (en) 2012-12-20 2012-12-20 Process for the preparation of estetrol and related compounds

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/EP2012/076358 WO2013034780A2 (en) 2012-12-20 2012-12-20 Process for the preparation of estetrol and related compounds

Publications (2)

Publication Number Publication Date
WO2013034780A2 WO2013034780A2 (en) 2013-03-14
WO2013034780A3 true WO2013034780A3 (en) 2013-10-03

Family

ID=47435979

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2012/076358 WO2013034780A2 (en) 2012-12-20 2012-12-20 Process for the preparation of estetrol and related compounds

Country Status (1)

Country Link
WO (1) WO2013034780A2 (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6254289B2 (en) * 2013-09-18 2017-12-27 クリスタル ファルマ、エセ、ア、ウＣｒｙｓｔａｌ Ｐｈａｒｍａ，Ｓ．Ａ．Ｕ． Estetrol manufacturing process
HU231240B1 (en) * 2019-09-03 2022-04-28 Richter Gedeon Nyrt. Industrial process for the preparation of high-purity estetrol
CH721078B1 (en) * 2019-09-27 2025-03-14 Ind Chimica Srl Process for the preparation of (15alpha,16alpha,17beta)-estra-1,3,5(10)-triene-3,15,16,17-tetrol monohydrate (estetrol monohydrate)
IT201900017414A1 (en) * 2019-09-27 2021-03-27 Ind Chimica Srl Process for the preparation of (15α, 16α, 17β) -estra-1,3,5 (10) -trene-3,15,16,17-tetrol (Estetrol) and intermediates of said process
IT202100019631A1 (en) 2021-07-23 2023-01-23 Newchem S P A METHOD FOR PRODUCING ESTETROL AND ITS INTERMEDIATE
WO2023021026A1 (en) 2021-08-17 2023-02-23 Aspen Oss B.V. A synthetic pathway to estra-1,3,5(10)-triene-3,15a,16a,17b-tetrol
CA3232558A1 (en) * 2021-10-01 2023-04-06 Roberto Lenna Process for preparing (15alpha,16alpha,17 eta)-estra-1,3,5(10)-triene-3,15,16,17-tetrol (estetrol) monohydrate
WO2024160373A1 (en) 2023-02-02 2024-08-08 Industriale Chimica S.R.L. PROCESS FOR PREPARING (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL (ESTETROL) MONOHYDRATE

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004041839A2 (en) * 2002-11-08 2004-05-21 Pantarhei Bioscience B.V. Synthesis of estetrol via estrone derived steroids
EP2383279A1 (en) * 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
WO2013050553A1 (en) * 2011-10-07 2013-04-11 Estetra S.A. Process for the production of estetrol

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002094276A1 (en) 2001-05-18 2002-11-28 Pantarhei Bioscience B.V. Pharmaceutical composition for use in hormone replacement therapy
EP1260225A1 (en) 2001-05-18 2002-11-27 Pantarhei Bioscience B.V. A pharmaceutical composition for use in hormone replacement therapy
DK1390042T3 (en) 2001-05-23 2008-03-31 Pantarhei Bioscience Bv System for administering a drug comprising tetrahydroxylated estrogen for use in hormonal contraception
US7871995B2 (en) 2001-05-23 2011-01-18 Pantarhei Bioscience B.V. Drug delivery system comprising a tetrahydroxylated estrogen for use in hormonal contraception
ES2278925T3 (en) 2001-11-15 2007-08-16 Pantarhei Bioscience B.V. USE OF ESTROGENIC COMPOUNDS IN COMBINATION WITH PROGESTOGENIC COMPOUNDS IN HORMONAL REPLACEMENT THERAPIES.
CN100352445C (en) 2002-06-11 2007-12-05 潘塔希生物科学股份有限公司 A method of treating human skin and a skin care composition for use in such a method
CA2489271C (en) 2002-06-11 2011-12-06 Pantarhei Bioscience B.V. Method of treating or preventing immune mediated disorders and pharmaceutical formulation for use therein
WO2004006936A1 (en) 2002-07-12 2004-01-22 Pantarhei Biosciences B.V. Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
EP1971344B1 (en) 2006-01-09 2010-09-22 Pantarhei Bioscience B.V. A method of treating an acute vascular disorder
CA2674325A1 (en) 2007-01-08 2008-07-17 Pantarhei Bioscience B.V. Method of treating or preventing infertility in a female mammal and pharmaceutical kit for use in such method

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004041839A2 (en) * 2002-11-08 2004-05-21 Pantarhei Bioscience B.V. Synthesis of estetrol via estrone derived steroids
EP2383279A1 (en) * 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
WO2013050553A1 (en) * 2011-10-07 2013-04-11 Estetra S.A. Process for the production of estetrol

Also Published As

Publication number Publication date
WO2013034780A2 (en) 2013-03-14

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