MX341561B - Proceso para la produccion de intermediarios de estetrol. - Google Patents
Proceso para la produccion de intermediarios de estetrol.Info
- Publication number
- MX341561B MX341561B MX2013014045A MX2013014045A MX341561B MX 341561 B MX341561 B MX 341561B MX 2013014045 A MX2013014045 A MX 2013014045A MX 2013014045 A MX2013014045 A MX 2013014045A MX 341561 B MX341561 B MX 341561B
- Authority
- MX
- Mexico
- Prior art keywords
- formula
- compound
- reacting
- group
- produce
- 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
-
- 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)
- 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
La presente invención se relaciona con un proceso para la preparación de un compuesto de fórmula (I), el proceso comprende las etapas de: (a) hacer reaccionar un compuesto de fórmula (II), con un agente acilante o un sililante para producir un compuesto de fórmula (III), en donde P1 y P2son cada uno independientemente un grupo protector que se selecciona de R2Si-R3R4 o R1CO-, en donde R1 es un grupo que se selecciona de alquilo de 1 a 4 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) hacer reaccionar el compuesto de fórmula (III) en presencia de acetato de paladio o un derivado del mismo para producir un compuesto de fórmula (IV); y c) hacer reaccionar el compuesto de fórmula (IV) con un agente reductor para producir el compuesto de fórmula (I).
Applications Claiming Priority (3)
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 |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2013014045A MX2013014045A (es) | 2014-08-22 |
MX341561B true MX341561B (es) | 2016-08-25 |
Family
ID=45003353
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2013014045A MX341561B (es) | 2011-06-01 | 2012-06-01 | Proceso para la produccion de intermediarios de estetrol. |
Country Status (24)
Country | Link |
---|---|
US (1) | US11053274B2 (es) |
EP (1) | EP2714710B1 (es) |
JP (2) | JP6425540B2 (es) |
KR (1) | KR101994805B1 (es) |
CN (2) | CN103703014A (es) |
AU (1) | AU2012264602B2 (es) |
BR (1) | BR112013030830B1 (es) |
CA (1) | CA2835981C (es) |
CY (1) | CY1118150T1 (es) |
DK (1) | DK2714710T3 (es) |
EA (1) | EA023991B1 (es) |
ES (1) | ES2579175T3 (es) |
HR (1) | HRP20160692T2 (es) |
HU (1) | HUE029252T2 (es) |
ME (1) | ME02454B (es) |
MX (1) | MX341561B (es) |
PL (1) | PL2714710T3 (es) |
PT (1) | PT2714710T (es) |
RS (1) | RS54880B1 (es) |
SG (1) | SG195118A1 (es) |
SI (1) | SI2714710T1 (es) |
SM (1) | SMT201600206B (es) |
WO (1) | WO2012164096A1 (es) |
ZA (1) | ZA201308446B (es) |
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
- 2012-06-01 SG SG2013086681A patent/SG195118A1/en unknown
- 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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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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