MX348917B - Proceso para la producción de estetrol. - Google Patents
Proceso para la producción de estetrol.Info
- Publication number
- MX348917B MX348917B MX2014003723A MX2014003723A MX348917B MX 348917 B MX348917 B MX 348917B MX 2014003723 A MX2014003723 A MX 2014003723A MX 2014003723 A MX2014003723 A MX 2014003723A MX 348917 B MX348917 B MX 348917B
- Authority
- MX
- Mexico
- Prior art keywords
- formula
- compound
- group
- 4alkyl
- 6alkyl
- Prior art date
Links
- AJIPIJNNOJSSQC-NYLIRDPKSA-N estetrol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H]([C@H](O)[C@@H]4O)O)[C@@H]4[C@@H]3CCC2=C1 AJIPIJNNOJSSQC-NYLIRDPKSA-N 0.000 title 1
- 229950009589 estetrol Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 7
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000001153 fluoro group Chemical group F* 0.000 abstract 4
- 125000001424 substituent group Chemical group 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- MHAJPDPJQMAIIY-UHFFFAOYSA-N Hydrogen peroxide Chemical compound OO MHAJPDPJQMAIIY-UHFFFAOYSA-N 0.000 abstract 2
- 125000006239 protecting group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000011630 iodine Substances 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 229910000487 osmium oxide Inorganic materials 0.000 abstract 1
- 239000007800 oxidant agent Substances 0.000 abstract 1
- JIWAALDUIFCBLV-UHFFFAOYSA-N oxoosmium Chemical compound [Os]=O JIWAALDUIFCBLV-UHFFFAOYSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- CQLFBEKRDQMJLZ-UHFFFAOYSA-M silver acetate Chemical compound [Ag+].CC([O-])=O CQLFBEKRDQMJLZ-UHFFFAOYSA-M 0.000 abstract 1
- 229940071536 silver acetate Drugs 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- 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
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- 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)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La presente invención se refiere a un proceso para la preparación de un compuesto de la fórmula (I), hidratos o solventes del mismo; (I) tal proceso comprende las etapas de (a) hacer reaccionar un compuesto de la fórmula (II) con un agente de acilación y un agente de sililación para producir un compuesto de la fórmula (III), (II) (III) en donde P1 es un grupo protector seleccionado de R1CO-, o R2Si(R3) (R4)-,P2 es un grupo protector seleccionado de (R6R5R7)C-CO-, o (R2)Si(R3) (R4)-, en donde R1 es un grupo seleccionado de C1- 6alquilo o C3-6cicloalquilo, cada grupo es opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados de flúor o C1-4alquilo; R2, R3 Y R4 son cada uno independientemente un grupo seleccionado de C1-6alquilo o fenilo, cada grupo es opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados de flúor o C1-4alquilo; R5 es un grupo seleccionado de C1-6alquilo o fenilo, cada grupo es opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados de flúor o C1-4alquilo; R6 y R7 son cada uno independientemente hidrógeno o un grupo seleccionado de C1-6alquilo o fenilo, cada grupo es opcionalmente sustituido por uno o más sustituyentes independientemente seleccionados de flúor o C1-4alquilo; b) hacer reaccionar el compuesto de la fórmula (III) en presencia de al menos un agente oxidante seleccionado de una sal de permanganato, óxido de osmio, peróxido de hidrógeno o yodo y acetato de plata para producir un compuesto de la fórmula (IV); y (IV)5 c) Desproteger el compuesto de la fórmula (IV) para producir el compuesto de la fórmula (I).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161544591P | 2011-10-07 | 2011-10-07 | |
| EP11184278 | 2011-10-07 | ||
| PCT/EP2012/069761 WO2013050553A1 (en) | 2011-10-07 | 2012-10-05 | Process for the production of estetrol |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2014003723A MX2014003723A (es) | 2014-10-13 |
| MX348917B true MX348917B (es) | 2017-07-04 |
Family
ID=48043195
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2014003723A MX348917B (es) | 2011-10-07 | 2012-10-05 | Proceso para la producción de estetrol. |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8987484B2 (es) |
| EP (1) | EP2764008B1 (es) |
| JP (1) | JP6196625B2 (es) |
| KR (1) | KR102007874B1 (es) |
| CN (1) | CN103890001B (es) |
| AU (1) | AU2012320423C1 (es) |
| BR (1) | BR112014008196B8 (es) |
| CA (1) | CA2847813C (es) |
| CL (1) | CL2014000802A1 (es) |
| CY (1) | CY1118674T1 (es) |
| DK (1) | DK2764008T3 (es) |
| EA (1) | EA024003B1 (es) |
| ES (1) | ES2593316T3 (es) |
| HR (1) | HRP20161282T1 (es) |
| HU (1) | HUE028963T2 (es) |
| IN (1) | IN2014MN00841A (es) |
| LT (1) | LT2764008T (es) |
| ME (1) | ME02527B (es) |
| MX (1) | MX348917B (es) |
| PL (1) | PL2764008T3 (es) |
| PT (1) | PT2764008T (es) |
| RS (1) | RS55231B1 (es) |
| SG (1) | SG11201401282PA (es) |
| SI (1) | SI2764008T1 (es) |
| SM (1) | SMT201600375B (es) |
| WO (1) | WO2013050553A1 (es) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112013030833B1 (pt) | 2011-06-01 | 2019-09-03 | Estetra S A | processo para a preparação de um composto de fórmula (i) e processo para a preparação de estetrol |
| WO2012164096A1 (en) | 2011-06-01 | 2012-12-06 | Estetra S.A. | 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 |
| WO2013034780A2 (en) * | 2012-12-20 | 2013-03-14 | Crystal Pharma, S.A.U. | Process for the preparation of estetrol and related compounds |
| EP3046928B1 (en) | 2013-09-18 | 2017-02-08 | Crystal Pharma, S.A.U. | Process for the preparation of estetrol |
| LT3310345T (lt) | 2015-06-18 | 2021-06-25 | Estetra Sprl | Burnoje disperguojama tabletė, turinti estetrolio |
| RS57328B1 (sr) | 2015-06-18 | 2018-08-31 | Mithra Pharmaceuticals S A | Orodisperzibilna dozna jedinica koja sadrži estetrolsku komponentu |
| WO2016203044A1 (en) | 2015-06-18 | 2016-12-22 | Mithra Pharmaceuticals S.A. | Orodispersible tablet containing estetrol |
| NZ737945A (en) | 2015-06-18 | 2023-06-30 | Estetra Sprl | Orodispersible dosage unit containing an estetrol component |
| CA3178291A1 (en) | 2016-08-05 | 2018-04-12 | Estetra Srl | Method for the management of dysmenorrhea and menstrual pain |
| CR20200486A (es) | 2018-04-19 | 2021-01-27 | Estetra Sprl | Compuestos y sus usos para aliviar los síntomas asociados a la menopausa |
| 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 |
| EP3647413A1 (en) * | 2018-10-31 | 2020-05-06 | Centro de Investigaciones Energéticas, Medioambientales y Tecnológicas O.A., M.P. (CIEMAT) | Improvements for performing and facilitating the recovery after hematopoietic stem cell transplantation |
| HU231240B1 (hu) | 2019-09-03 | 2022-04-28 | Richter Gedeon Nyrt. | Ipari eljárás nagytisztaságú ösztetrol hatóanyag előállítására |
| CN114514237B (zh) | 2019-09-27 | 2024-07-26 | 工业化学有限公司 | 用于制备(15α,16α,17β)-雌-1,3,5(10)-三烯-3,15,16,17-四醇(雌四醇)的工艺及所述工艺的中间体 |
| 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 |
| TWI893101B (zh) | 2020-04-16 | 2025-08-11 | 比利時商埃斯特拉有限責任公司 | 具有降低之副作用之避孕組成物 |
| IT202100019631A1 (it) | 2021-07-23 | 2023-01-23 | Newchem S P A | Metodo per produrre estetrolo e i suoi intermedi |
| 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 |
| GB2626482B (en) | 2021-10-01 | 2025-04-30 | Ind Chimica Srl | Process for preparing (15alpha,16alpha,17beta)-estra-1,3,5-(10)-triene-3,15,16,17-tetrol(estetrol) monohydrate |
| CN120958008A (zh) | 2023-02-02 | 2025-11-14 | 工业化学有限公司 | 制备(15α,16α,17β)-雌甾-1,3,5(10)-三烯-3,15,16,17-四醇（雌四醇）一水合物的方法 |
| CN121605114A (zh) * | 2023-08-30 | 2026-03-03 | 埃斯特拉私人有限责任公司 | 雌四醇中间体的制造方法 |
| WO2025181200A1 (en) | 2024-02-28 | 2025-09-04 | Estetra Srl | Estetrol polymorphic form and production thereof |
| HUP2400151A1 (hu) | 2024-02-28 | 2025-09-28 | Richter Gedeon Nyrt | Ösztetrol-monohidrát kristályosítási eljárás |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW548277B (en) * | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
| US6706700B2 (en) * | 1999-12-02 | 2004-03-16 | Akzo-Nobel, N.V. | 14β,15β-methylene-17α-hydroxymethyl-androgens |
| AU2003279624A1 (en) * | 2002-11-08 | 2004-06-07 | Pantarhei Bioscience B.V. | Synthesis of estetrol via estrone derived steroids |
| UA89964C2 (ru) * | 2004-09-08 | 2010-03-25 | Н.В. Органон | 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ |
| WO2012164096A1 (en) | 2011-06-01 | 2012-12-06 | Estetra S.A. | Process for the production of estetrol intermediates |
| BR112013030833B1 (pt) | 2011-06-01 | 2019-09-03 | Estetra S A | processo para a preparação de um composto de fórmula (i) e processo para a preparação de estetrol |
| EP2383279A1 (en) * | 2011-07-19 | 2011-11-02 | Pantarhei Bioscience B.V. | Process for the preparation of estetrol |
-
2012
- 2012-10-05 EP EP12778664.8A patent/EP2764008B1/en active Active
- 2012-10-05 AU AU2012320423A patent/AU2012320423C1/en active Active
- 2012-10-05 WO PCT/EP2012/069761 patent/WO2013050553A1/en not_active Ceased
- 2012-10-05 DK DK12778664.8T patent/DK2764008T3/en active
- 2012-10-05 SI SI201230705A patent/SI2764008T1/sl unknown
- 2012-10-05 EA EA201490713A patent/EA024003B1/ru unknown
- 2012-10-05 PL PL12778664T patent/PL2764008T3/pl unknown
- 2012-10-05 HU HUE12778664A patent/HUE028963T2/en unknown
- 2012-10-05 JP JP2014533925A patent/JP6196625B2/ja active Active
- 2012-10-05 LT LTEP12778664.8T patent/LT2764008T/lt unknown
- 2012-10-05 HR HRP20161282TT patent/HRP20161282T1/hr unknown
- 2012-10-05 CA CA2847813A patent/CA2847813C/en active Active
- 2012-10-05 ME MEP-2016-229A patent/ME02527B/me unknown
- 2012-10-05 CN CN201280049319.2A patent/CN103890001B/zh active Active
- 2012-10-05 KR KR1020147007408A patent/KR102007874B1/ko active Active
- 2012-10-05 SG SG11201401282PA patent/SG11201401282PA/en unknown
- 2012-10-05 RS RS20160859A patent/RS55231B1/sr unknown
- 2012-10-05 ES ES12778664.8T patent/ES2593316T3/es active Active
- 2012-10-05 MX MX2014003723A patent/MX348917B/es active IP Right Grant
- 2012-10-05 US US14/349,940 patent/US8987484B2/en active Active
- 2012-10-05 BR BR112014008196A patent/BR112014008196B8/pt active IP Right Grant
- 2012-10-05 PT PT127786648T patent/PT2764008T/pt unknown
-
2014
- 2014-04-02 CL CL2014000802A patent/CL2014000802A1/es unknown
- 2014-05-05 IN IN841MUN2014 patent/IN2014MN00841A/en unknown
-
2016
- 2016-10-10 CY CY20161101001T patent/CY1118674T1/el unknown
- 2016-10-17 SM SM201600375T patent/SMT201600375B/it unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |