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

    • 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
    • C07J1/0003—Androstane derivatives
    • C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens
    • 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

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (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 (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2714710B1 (en) 2011-06-01 2016-04-06 Estetra S.P.R.L. Process for the production of estetrol intermediates
ES2600703T3 (es) 2011-06-01 2017-02-10 Estetra S.P.R.L. Proceso para la producción de intermediarios de estetrol
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
DK2764008T3 (en) 2011-10-07 2016-11-07 Estetra Sprl A process for the preparation of estetrol
TN2017000499A1 (en) 2015-06-18 2019-04-12 Mithra Pharmaceuticals S A Orodispersible dosage unit containing an estetrol component
GEP20217243B (en) 2015-06-18 2021-04-26 Sprl Estetra Orodispersible dosage unit containing an estetrol component
ES2877186T3 (es) 2015-06-18 2021-11-16 Estetra Sprl Comprimido orodispersable que contiene estetrol
LT3310346T (lt) 2015-06-18 2021-06-10 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio
KR20220144885A (ko) 2016-08-05 2022-10-27 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 월경통 및 생리통의 관리방법
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LT3310346T (lt) 2015-06-18 2021-06-10 Estetra Sprl Burnoje disperguojama tabletė, turinti estetrolio

Also Published As

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

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