CY1118150T1 - Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrol - Google Patents
Μεθοδος για την παραγωγη ενδιαμεσων ενωσεων estetrolInfo
- 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
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
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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
- 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
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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)
- 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
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).
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) | CN103703014A (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) |
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 |
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 |
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 |
KR20220144885A (ko) | 2016-08-05 | 2022-10-27 | 에스테트라, 소시에떼 아 레스폰서빌리떼 리미떼 | 월경통 및 생리통의 관리방법 |
JP6935766B2 (ja) | 2018-02-15 | 2021-09-15 | 日本精工株式会社 | スピンドル装置 |
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 |
US20220348607A1 (en) | 2019-09-27 | 2022-11-03 | Industriale Chimica S.R.L. | Process for preparing (15alpha,16alpha,17beta)-estra-1,3,5(10)-triene- 3,15,16,17-tetrol (estetrol) and intermediates of said process |
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 |
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 |
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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RS61777B1 (sr) | 2015-06-18 | 2021-06-30 | Estetra Sprl | Oralno-disperzibilna tableta koja sadrži estetrol |
SI3310345T1 (sl) | 2015-06-18 | 2021-05-31 | Estetra Sprl | Orodisperzibilna tableta, ki vsebuje estetrol |
MY195019A (en) | 2015-06-18 | 2023-01-03 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
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2012
- 2012-06-01 PL PL12729054T patent/PL2714710T3/pl unknown
- 2012-06-01 PT PT127290542T patent/PT2714710T/pt unknown
- 2012-06-01 KR KR1020137031483A patent/KR101994805B1/ko active IP Right Grant
- 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 RS RS20160478A patent/RS54880B1/sr unknown
- 2012-06-01 CA CA2835981A patent/CA2835981C/en active Active
- 2012-06-01 CN CN201280026162.1A patent/CN103703014A/zh active Pending
- 2012-06-01 US US14/122,872 patent/US11053274B2/en active Active
- 2012-06-01 SI SI201230598A patent/SI2714710T1/sl unknown
- 2012-06-01 JP JP2014513214A patent/JP6425540B2/ja active Active
- 2012-06-01 EP EP12729054.2A patent/EP2714710B1/en active Active
- 2012-06-01 HU HUE12729054A patent/HUE029252T2/en unknown
- 2012-06-01 DK DK12729054.2T patent/DK2714710T3/en active
- 2012-06-01 CN CN201710354709.5A patent/CN107266514A/zh active Pending
- 2012-06-01 WO PCT/EP2012/060447 patent/WO2012164096A1/en active Application Filing
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- 2012-06-01 ME MEP-2016-130A patent/ME02454B/me unknown
- 2012-06-01 EA EA201301316A patent/EA023991B1/ru unknown
- 2012-06-01 AU AU2012264602A patent/AU2012264602B2/en active Active
- 2012-06-01 ES ES12729054.2T patent/ES2579175T3/es active Active
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2016
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2017
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