CY1118150T1 - Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrol - Google Patents

Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrol

Info

Publication number
CY1118150T1
CY1118150T1 CY20161100525T CY161100525T CY1118150T1 CY 1118150 T1 CY1118150 T1 CY 1118150T1 CY 20161100525 T CY20161100525 T CY 20161100525T CY 161100525 T CY161100525 T CY 161100525T CY 1118150 T1 CY1118150 T1 CY 1118150T1
Authority
CY
Cyprus
Prior art keywords
compound
formula
reacting
produce
group
Prior art date
Application number
CY20161100525T
Other languages
English (en)
Inventor
Jean-Claude Pascal
Original Assignee
Estetra S.P.R.L.
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.P.R.L. filed Critical Estetra S.P.R.L.
Publication of CY1118150T1 publication Critical patent/CY1118150T1/el

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J75/00—Processes for the preparation of steroids in general
    • 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
    • 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
    • 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
    • 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
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • 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)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Η παρούσα εφεύρεση σχετίζεται με μια μέθοδο για την παρασκευή μιας ένωσης του τύπου (I), η οποία μέθοδος περιλαμβάνει τα εξής στάδια: α) αντίδραση μιας ένωσης του τύπου (II), με έναν παράγοντα ακυλίωσης ή σιλυλίωσης για παραγωγή μιας ένωσης του τύπου (III), όπου τα Ρ1 και Ρ2 είναι το καθένα ανεξάρτητα μια προστατευτική ομάδα που επιλέγεται από R2-Si-R3R4 ή R1CO-, όπου το R1 είναι μια ομάδα που επιλέγεται από C1-6αλκυλο ή C3-6κυκλοαλκυλο, όπου κάθε ομάδα είναι προαιρετικώς υποκατεστημένη από έναν ή περισσότερους υποκατάστατες που επιλέγονται ανεξάρτητα από φθόριο ή C1-4αλκυλο· τα R2, R3 και R4 είναι το καθένα ανεξάρτητα μια ομάδα που επιλέγεται από C1-6αλκυλο ή φαινυλο, όπου κάθε ομάδα είναι προαιρετικώς υποκατεστημένη από έναν ή περισσότερους υποκατάστατες που επιλέγονται ανεξάρτητα από φθορο ή C1-4αλκυλο· β) αντίδραση της ένωσης του τύπου (III) παρουσία οξεικού παλλαδίου ή παραγώγου αυτού για παραγωγή ένωσης του τύπου (IV)· και γ) αντίδραση της ένωσης του τύπου (IV) με αναγωγικό παράγοντα για παραγωγή ένωσης του τύπου (I).
CY20161100525T 2011-06-01 2016-06-15 Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrol CY1118150T1 (el)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201161492300P 2011-06-01 2011-06-01
EP11168561 2011-06-01
PCT/EP2012/060447 WO2012164096A1 (en) 2011-06-01 2012-06-01 Process for the production of estetrol intermediates
EP12729054.2A EP2714710B1 (en) 2011-06-01 2012-06-01 Process for the production of estetrol intermediates

Publications (1)

Publication Number Publication Date
CY1118150T1 true CY1118150T1 (el) 2017-06-28

Family

ID=45003353

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20161100525T CY1118150T1 (el) 2011-06-01 2016-06-15 Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrol

Country Status (24)

Country Link
US (1) US11053274B2 (el)
EP (1) EP2714710B1 (el)
JP (2) JP6425540B2 (el)
KR (1) KR101994805B1 (el)
CN (2) CN107266514A (el)
AU (1) AU2012264602B2 (el)
BR (1) BR112013030830B1 (el)
CA (1) CA2835981C (el)
CY (1) CY1118150T1 (el)
DK (1) DK2714710T3 (el)
EA (1) EA023991B1 (el)
ES (1) ES2579175T3 (el)
HR (1) HRP20160692T2 (el)
HU (1) HUE029252T2 (el)
ME (1) ME02454B (el)
MX (1) MX341561B (el)
PL (1) PL2714710T3 (el)
PT (1) PT2714710T (el)
RS (1) RS54880B1 (el)
SG (1) SG195118A1 (el)
SI (1) SI2714710T1 (el)
SM (1) SMT201600206B (el)
WO (1) WO2012164096A1 (el)
ZA (1) ZA201308446B (el)

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Publication number Publication date
JP2014518199A (ja) 2014-07-28
KR20140036205A (ko) 2014-03-25
RS54880B1 (sr) 2016-10-31
EP2714710A1 (en) 2014-04-09
CN107266514A (zh) 2017-10-20
JP6425540B2 (ja) 2018-11-21
SI2714710T1 (sl) 2016-08-31
HRP20160692T2 (hr) 2016-09-23
HRP20160692T1 (hr) 2016-08-12
MX341561B (es) 2016-08-25
ES2579175T3 (es) 2016-08-05
WO2012164096A1 (en) 2012-12-06
EP2714710B1 (en) 2016-04-06
JP6479912B2 (ja) 2019-03-06
SG195118A1 (en) 2013-12-30
US20140107358A1 (en) 2014-04-17
HUE029252T2 (en) 2017-02-28
EA023991B1 (ru) 2016-08-31
JP2018024673A (ja) 2018-02-15
CN103703014A (zh) 2014-04-02
CA2835981C (en) 2018-07-24
PT2714710T (pt) 2016-07-12
PL2714710T3 (pl) 2017-03-31
ZA201308446B (en) 2016-08-31
NZ617613A (en) 2015-12-24
MX2013014045A (es) 2014-08-22
BR112013030830B1 (pt) 2019-12-03
SMT201600206B (it) 2016-08-31
US11053274B2 (en) 2021-07-06
CA2835981A1 (en) 2012-12-06
BR112013030830A2 (pt) 2016-08-30
KR101994805B1 (ko) 2019-07-01
AU2012264602B2 (en) 2017-03-09
ME02454B (me) 2016-09-20
DK2714710T3 (en) 2016-06-27
EA201301316A1 (ru) 2014-04-30

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