RS54880B1 - Postupak proizvodnje intermedijarnih proizvoda estetrola - Google Patents

Postupak proizvodnje intermedijarnih proizvoda estetrola

Info

Publication number
RS54880B1
RS54880B1 RS20160478A RSP20160478A RS54880B1 RS 54880 B1 RS54880 B1 RS 54880B1 RS 20160478 A RS20160478 A RS 20160478A RS P20160478 A RSP20160478 A RS P20160478A RS 54880 B1 RS54880 B1 RS 54880B1
Authority
RS
Serbia
Prior art keywords
compound
formula
reacting
produce
group selected
Prior art date
Application number
RS20160478A
Other languages
English (en)
Inventor
Jean-Claude Pascal
Original Assignee
Estetra Sprl
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 Sprl filed Critical Estetra Sprl
Publication of RS54880B1 publication Critical patent/RS54880B1/sr

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

Postupak pripremanja jedinjenja formule (I)naznačen time, što se postupak sastoji oda) reagovanja jedinjenja formule (II), sa sredstvom za acilovanje ili sililovanje da se proizvede jedinjenje formule (III), pri čemu P1 i P2 svaki nezavisno predstavlja zaštitnu grupu odabranu od R2-Si-R3R4, ili R1CO-, pri čemu je R1 grupa odabrana od C1-6alkil ili C3-6cikloalkil, gde je svaka od grupa opciono supstituisana sa jednim ili više supstituenata nezavisno odabranih od fluoro ili C1-4alkila; R2, R3 i R4 su svaki nezavisno grupa odabrana od C1- 6alkila ili fenila, gde je svaka od ovih grupa opciono supstituisana sa jednim ili više supstituenata nezavisno odabranih od fluoro ili C1-4alkila;b) reagovanja jedinjenja formule (III) u prisustvu paladijum acetata ili paladijum hlorida da se proizvede jedinjenje formule (IV); ic) reagovanja jedinjenja formule (IV) sa redukcionim sredstvom da se proizvede jedinjenje formule (I).Prijava sadrži još 13 patentnih zahteva.
RS20160478A 2011-06-01 2012-06-01 Postupak proizvodnje intermedijarnih proizvoda estetrola RS54880B1 (sr)

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
RS54880B1 true RS54880B1 (sr) 2016-10-31

Family

ID=45003353

Family Applications (1)

Application Number Title Priority Date Filing Date
RS20160478A RS54880B1 (sr) 2011-06-01 2012-06-01 Postupak proizvodnje intermedijarnih proizvoda estetrola

Country Status (24)

Country Link
US (1) US11053274B2 (sr)
EP (1) EP2714710B1 (sr)
JP (2) JP6425540B2 (sr)
KR (1) KR101994805B1 (sr)
CN (2) CN103703014A (sr)
AU (1) AU2012264602B2 (sr)
BR (1) BR112013030830B1 (sr)
CA (1) CA2835981C (sr)
CY (1) CY1118150T1 (sr)
DK (1) DK2714710T3 (sr)
EA (1) EA023991B1 (sr)
ES (1) ES2579175T3 (sr)
HR (1) HRP20160692T2 (sr)
HU (1) HUE029252T2 (sr)
ME (1) ME02454B (sr)
MX (1) MX341561B (sr)
PL (1) PL2714710T3 (sr)
PT (1) PT2714710T (sr)
RS (1) RS54880B1 (sr)
SG (1) SG195118A1 (sr)
SI (1) SI2714710T1 (sr)
SM (1) SMT201600206B (sr)
WO (1) WO2012164096A1 (sr)
ZA (1) ZA201308446B (sr)

Families Citing this family (18)

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CA2835979C (en) 2011-06-01 2018-05-01 Estetra S.A. Process for the production of estetrol intermediates
PL2714710T3 (pl) 2011-06-01 2017-03-31 Estetra S.P.R.L. Sposób wytwarzania estetrolowych związków pośrednich
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
JP6196625B2 (ja) 2011-10-07 2017-09-13 エステトラ エス．ペ．エール．エル． エステトロールを製造するための方法
RS61777B1 (sr) 2015-06-18 2021-06-30 Estetra Sprl Oralno-disperzibilna tableta koja sadrži estetrol
ME03728B (me) 2015-06-18 2021-01-20 Estetra Sprl Orodisperzibilna dozna jedinica koja sadrži komponentu estetrola
MY195019A (en) 2015-06-18 2023-01-03 Estetra Sprl Orodispersible dosage unit containing an estetrol component
SI3310345T1 (sl) 2015-06-18 2021-05-31 Estetra Sprl Orodisperzibilna tableta, ki vsebuje estetrol
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TWI801561B (zh) 2018-04-19 2023-05-11 比利時商依思特拉私人有限責任公司 化合物及其用於緩解絕經相關症狀的用途
JOP20200260A1 (ar) 2018-04-19 2019-10-19 Estetra Sprl مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث
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IT201900017414A1 (it) 2019-09-27 2021-03-27 Ind Chimica Srl Processo per la preparazione di (15α,16α,17β)-estra-1,3,5(10)-triene-3,15,16,17-tetrolo (Estetrolo) ed intermedi di detto processo
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Also Published As

Publication number Publication date
BR112013030830A2 (pt) 2016-08-30
HRP20160692T2 (hr) 2016-09-23
CN107266514A (zh) 2017-10-20
DK2714710T3 (en) 2016-06-27
KR101994805B1 (ko) 2019-07-01
PL2714710T3 (pl) 2017-03-31
JP6425540B2 (ja) 2018-11-21
CN103703014A (zh) 2014-04-02
MX341561B (es) 2016-08-25
WO2012164096A1 (en) 2012-12-06
ME02454B (me) 2016-09-20
SMT201600206B (it) 2016-08-31
CY1118150T1 (el) 2017-06-28
BR112013030830B1 (pt) 2019-12-03
EA201301316A1 (ru) 2014-04-30
PT2714710T (pt) 2016-07-12
KR20140036205A (ko) 2014-03-25
EP2714710B1 (en) 2016-04-06
NZ617613A (en) 2015-12-24
JP2018024673A (ja) 2018-02-15
SG195118A1 (en) 2013-12-30
US20140107358A1 (en) 2014-04-17
JP2014518199A (ja) 2014-07-28
ES2579175T3 (es) 2016-08-05
JP6479912B2 (ja) 2019-03-06
HRP20160692T1 (hr) 2016-08-12
HUE029252T2 (en) 2017-02-28
US11053274B2 (en) 2021-07-06
CA2835981A1 (en) 2012-12-06
SI2714710T1 (sl) 2016-08-31
EA023991B1 (ru) 2016-08-31
EP2714710A1 (en) 2014-04-09
ZA201308446B (en) 2016-08-31
MX2013014045A (es) 2014-08-22
CA2835981C (en) 2018-07-24
AU2012264602B2 (en) 2017-03-09

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