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MX2013014044A - Proceso para la produccion de intermediarios de estetrol. - Google Patents

Proceso para la produccion de intermediarios de estetrol.

Info

Publication number
MX2013014044A
MX2013014044A MX2013014044A MX2013014044A MX2013014044A MX 2013014044 A MX2013014044 A MX 2013014044A MX 2013014044 A MX2013014044 A MX 2013014044A MX 2013014044 A MX2013014044 A MX 2013014044A MX 2013014044 A MX2013014044 A MX 2013014044A
Authority
MX
Mexico
Prior art keywords
formula
compound
group
produce
4alkyl
Prior art date
Application number
MX2013014044A
Other languages
English (en)
Other versions
MX342537B (es
Inventor
Jean-Claude Pascal
Original Assignee
Estetra S A
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 Estetra S A filed Critical Estetra S A
Publication of MX2013014044A publication Critical patent/MX2013014044A/es
Publication of MX342537B publication Critical patent/MX342537B/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003Androstane derivatives
    • C07J1/0018Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J75/00Processes for the preparation of steroids in general
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0059Estrane derivatives substituted in position 17 by a keto group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La presente invención se relaciona con un proceso para la preparación de un compuesto de fórmula (I), que comprende las etapas de: (a) hacer reaccionar un compuesto de fórmula (II), con un agente sililante o uno acilante para producir un compuesto de fórmula (III), en donde P1 es un grupo protector que se selecciona de R2Si-R3R4 o R1CO-, R1 es un grupo que se selecciona de alquilo de 1 a 6 átomos de carbono o cicloalquilo de 3 a 6 átomos de carbono, cada grupo está opcionalmente sustituido por uno o más sustituyentes que se seleccionan independientemente de fluoro o alquilo de 1 a 4 átomos de carbono; R2, R3 y R4 son cada uno independientemente un grupo que se selecciona de alquilo de 1 a 6 átomos de carbono o fenilo, cada grupo está opcionalmente sustituido por uno o más sustituyentes que se seleccionan independientemente de fluoro o alquilo de 1 a 4 átomos de carbono; b) halogenación o sulfinilación del compuesto de fórmula (III) para producir un compuesto de fórmula (IV); en donde X es halo, o -O-SO-R5 y R5 es un grupo que se selecciona de arilo de 6 a 10 átomos de carbono o heteroarilo, cada grupo está opcionalmente sustituido por uno o más sustituyentes que se seleccionan independientemente de cloro o alquilo de 1 a 4 átomos de carbono; c) deshalogenación o desulfinilación del compuesto de fórmula (IV) para producir el compuesto de fórmula (V); y d) hacer reaccionar el compuesto de fórmula (V) con un agente reductor para producir un compuesto de fórmula (I).
MX2013014044A 2011-06-01 2012-06-01 Proceso para la produccion de intermediarios de estetrol. MX342537B (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161492297P 2011-06-01 2011-06-01
EP11168560 2011-06-01
PCT/EP2012/060446 WO2012164095A1 (en) 2011-06-01 2012-06-01 Process for the production of estetrol intermediates

Publications (2)

Publication Number Publication Date
MX2013014044A true MX2013014044A (es) 2014-08-21
MX342537B MX342537B (es) 2016-10-04

Family

ID=44588329

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2013014044A MX342537B (es) 2011-06-01 2012-06-01 Proceso para la produccion de intermediarios de estetrol.

Country Status (25)

Country Link
US (1) US11053273B2 (es)
EP (1) EP2714712B1 (es)
JP (1) JP6116550B2 (es)
KR (1) KR101957937B1 (es)
CN (1) CN103619867B (es)
AU (1) AU2012264601C1 (es)
BR (1) BR112013030833B1 (es)
CA (1) CA2835979C (es)
CY (1) CY1118164T1 (es)
DK (1) DK2714712T3 (es)
EA (1) EA025511B1 (es)
ES (1) ES2600703T3 (es)
HR (1) HRP20161369T1 (es)
HU (1) HUE031809T2 (es)
LT (1) LT2714712T (es)
ME (1) ME02585B (es)
MX (1) MX342537B (es)
PL (1) PL2714712T3 (es)
PT (1) PT2714712T (es)
RS (1) RS55293B1 (es)
SG (1) SG195121A1 (es)
SI (1) SI2714712T1 (es)
SM (1) SMT201600408B (es)
WO (1) WO2012164095A1 (es)
ZA (1) ZA201308445B (es)

Families Citing this family (14)

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PL2714712T3 (pl) 2011-06-01 2017-05-31 Estetra S.P.R.L. Metoda wytwarzania półproduktów estetrolu
MX341561B (es) 2011-06-01 2016-08-25 Estetra Sprl Proceso para la produccion de intermediarios de estetrol.
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
PL2764008T3 (pl) 2011-10-07 2017-04-28 Estetra S.P.R.L. Sposób wytwarzania estetrolu
JP6863547B2 (ja) 2015-06-18 2021-04-21 エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ エステトロール成分を含有する口腔内崩壊性投与単位
JP6866560B2 (ja) 2015-06-18 2021-04-28 エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ エステトロール成分を含有する口腔内崩壊性投与単位
MA44206B1 (fr) 2015-06-18 2021-04-30 Estetra Sprl Comprimé orodispersible comprenant estetrol
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
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TWI893101B (zh) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 具有降低之副作用之避孕組成物
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
WO2025046071A1 (en) 2023-08-30 2025-03-06 Estetra Srl Process for the production of estetrol intermediates

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JP6866560B2 (ja) 2015-06-18 2021-04-28 エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ エステトロール成分を含有する口腔内崩壊性投与単位
JP6863547B2 (ja) 2015-06-18 2021-04-21 エステトラ ソシエテ プリーヴ ア レスポンサビリテ リミテ エステトロール成分を含有する口腔内崩壊性投与単位
LT3310345T (lt) 2015-06-18 2021-06-25 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio

Also Published As

Publication number Publication date
PT2714712T (pt) 2016-11-08
AU2012264601C1 (en) 2018-01-25
CA2835979C (en) 2018-05-01
CA2835979A1 (en) 2012-12-06
BR112013030833B1 (pt) 2019-09-03
WO2012164095A1 (en) 2012-12-06
BR112013030833A2 (pt) 2016-09-06
PL2714712T3 (pl) 2017-05-31
HRP20161369T1 (hr) 2016-12-02
EP2714712B1 (en) 2016-08-24
MX342537B (es) 2016-10-04
NZ617591A (en) 2015-12-24
JP2014515391A (ja) 2014-06-30
SG195121A1 (en) 2013-12-30
US20140107091A1 (en) 2014-04-17
EP2714712A1 (en) 2014-04-09
CN103619867B (zh) 2015-12-23
SI2714712T1 (sl) 2016-11-30
HUE031809T2 (en) 2017-08-28
KR20140036206A (ko) 2014-03-25
EA201301315A1 (ru) 2014-05-30
LT2714712T (lt) 2016-11-25
ES2600703T3 (es) 2017-02-10
ZA201308445B (en) 2015-07-29
DK2714712T3 (en) 2016-12-05
KR101957937B1 (ko) 2019-03-14
SMT201600408B (es) 2017-01-10
AU2012264601B2 (en) 2017-02-16
US11053273B2 (en) 2021-07-06
CY1118164T1 (el) 2017-06-28
ME02585B (me) 2017-06-20
RS55293B1 (sr) 2017-03-31
EA025511B1 (ru) 2016-12-30
CN103619867A (zh) 2014-03-05
AU2012264601A1 (en) 2013-11-28
JP6116550B2 (ja) 2017-04-19

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