RS54880B1 - Postupak proizvodnje intermedijarnih proizvoda estetrola - Google Patents
Postupak proizvodnje intermedijarnih proizvoda estetrolaInfo
- 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
Links
Classifications
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- 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
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- 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
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- 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
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.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161492300P | 2011-06-01 | 2011-06-01 | |
EP11168561 | 2011-06-01 | ||
EP12729054.2A EP2714710B1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
PCT/EP2012/060447 WO2012164096A1 (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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
US11053274B2 (en) | 2011-06-01 | 2021-07-06 | Estetra S.P.R.L. | Process for the production of estetrol intermediates |
EP2383279A1 (en) | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
US8987484B2 (en) | 2011-10-07 | 2015-03-24 | Estetra S.P.R.L. | Process for the production of estetrol |
PL3310333T3 (pl) | 2015-06-18 | 2020-07-13 | Estetra Sprl | Ulegająca rozpadowi w jamie ustnej jednostka dawkowana zawierająca składnik estetrolowy |
GEP20217308B (en) | 2015-06-18 | 2021-10-25 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
MA44205B1 (fr) | 2015-06-18 | 2021-04-30 | Estetra Sprl | Comprimé orodispersible comprenant estetrol |
DK3310346T3 (da) | 2015-06-18 | 2021-05-25 | Estetra Sprl | Orodispersibel tablet indeholdende estetrol |
CN105837424A (zh) * | 2016-03-31 | 2016-08-10 | 常州大学 | 一种1-氯-3-甲基-3-丁烯-2-酮的合成方法 |
CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
JP6935766B2 (ja) | 2018-02-15 | 2021-09-15 | 日本精工株式会社 | スピンドル装置 |
JOP20200260A1 (ar) | 2018-04-19 | 2019-10-19 | Estetra Sprl | مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث |
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 |
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 |
IT201900021879A1 (it) | 2019-11-22 | 2021-05-22 | 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 |
JP2022549585A (ja) | 2019-09-27 | 2022-11-28 | インダストリアレ チミカ ソシエタ ア レスポンサビリタ リミタータ | (15α,16α,17β)-エストラ-1,3,5(10)-トリエン-3,15,16,17-テトロール(エステトロール)および当該製法の中間体を調製するためのプロセス |
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 |
WO2023051937A1 (en) | 2021-10-01 | 2023-04-06 | Industriale Chimica S.R.L. | Process for preparing (15alpha,16alpha,17 eta)-estra-1,3,5(10)-triene-3,15,16,17-tetrol (estetrol) monohydrate |
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CA2835979C (en) | 2011-06-01 | 2018-05-01 | Estetra S.A. | Process for the production of estetrol intermediates |
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GEP20217308B (en) | 2015-06-18 | 2021-10-25 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
MA44205B1 (fr) | 2015-06-18 | 2021-04-30 | Estetra Sprl | Comprimé orodispersible comprenant estetrol |
DK3310346T3 (da) | 2015-06-18 | 2021-05-25 | Estetra Sprl | Orodispersibel tablet indeholdende estetrol |
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2012
- 2012-06-01 US US14/122,872 patent/US11053274B2/en active Active
- 2012-06-01 DK DK12729054.2T patent/DK2714710T3/en active
- 2012-06-01 RS RS20160478A patent/RS54880B1/sr unknown
- 2012-06-01 CN CN201280026162.1A patent/CN103703014A/zh active Pending
- 2012-06-01 AU AU2012264602A patent/AU2012264602B2/en active Active
- 2012-06-01 CA CA2835981A patent/CA2835981C/en active Active
- 2012-06-01 ME MEP-2016-130A patent/ME02454B/me unknown
- 2012-06-01 KR KR1020137031483A patent/KR101994805B1/ko active IP Right Grant
- 2012-06-01 SI SI201230598A patent/SI2714710T1/sl unknown
- 2012-06-01 PT PT127290542T patent/PT2714710T/pt unknown
- 2012-06-01 BR BR112013030830A patent/BR112013030830B1/pt active IP Right Grant
- 2012-06-01 MX MX2013014045A patent/MX341561B/es active IP Right Grant
- 2012-06-01 EP EP12729054.2A patent/EP2714710B1/en active Active
- 2012-06-01 HU HUE12729054A patent/HUE029252T2/en unknown
- 2012-06-01 JP JP2014513214A patent/JP6425540B2/ja active Active
- 2012-06-01 PL PL12729054T patent/PL2714710T3/pl unknown
- 2012-06-01 SG SG2013086681A patent/SG195118A1/en unknown
- 2012-06-01 ES ES12729054.2T patent/ES2579175T3/es active Active
- 2012-06-01 EA EA201301316A patent/EA023991B1/ru unknown
- 2012-06-01 WO PCT/EP2012/060447 patent/WO2012164096A1/en active Application Filing
- 2012-06-01 CN CN201710354709.5A patent/CN107266514A/zh active Pending
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2013
- 2013-11-11 ZA ZA2013/08446A patent/ZA201308446B/en unknown
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2016
- 2016-06-15 CY CY20161100525T patent/CY1118150T1/el unknown
- 2016-06-17 HR HRP20160692TT patent/HRP20160692T2/hr unknown
- 2016-06-30 SM SM201600206T patent/SMT201600206B/it unknown
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2017
- 2017-08-10 JP JP2017155801A patent/JP6479912B2/ja active Active
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