CY1118164T1 - Διεργασια για την παραγωγη ενδιαμεσων οιστετρολης - Google Patents
Διεργασια για την παραγωγη ενδιαμεσων οιστετροληςInfo
- Publication number
- CY1118164T1 CY1118164T1 CY20161101090T CY161101090T CY1118164T1 CY 1118164 T1 CY1118164 T1 CY 1118164T1 CY 20161101090 T CY20161101090 T CY 20161101090T CY 161101090 T CY161101090 T CY 161101090T CY 1118164 T1 CY1118164 T1 CY 1118164T1
- Authority
- CY
- Cyprus
- Prior art keywords
- compound
- formula
- group
- produce
- optionally substituted
- Prior art date
Links
Classifications
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- 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
- C07J1/0003—Androstane derivatives
- C07J1/0018—Androstane derivatives substituted in position 17 beta, not substituted in position 17 alfa
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J75/00—Processes for the preparation of steroids in general
-
- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/02—Drugs for genital or sexual disorders; Contraceptives for disorders of the vagina
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/18—Feminine contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- 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
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Dermatology (AREA)
- Gynecology & Obstetrics (AREA)
- Diabetes (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Η παρούσα εφεύρεση αναφέρεται σε μια διεργασία για την παρασκευή μιας ένωσης του τύπου (I) περιλαμβάνουσα τα στάδια (a) αντίδρασης μιας ένωσης του τύπου (II) με ένα σιλυλιωτικό ή ένα ακυλιωτικό μέσο προς παραγωγή μιας ένωσης του τύπου (III), όπου το Ρ1 είναι μια προστατευτική ομάδα που επιλέγεται από R2Si-R3R4 ή R1CO-, το R1 είναι μια ομάδα που επιλέγεται από C1-6αλκύλιο ή C3-6κυκλοαλκύλιο, κάθε ομάδα είναι προαιρετικώς υποκατεστημένη με έναν ή περισσότερους υποκατάστατες ανεξαρτήτως επιλεγμένους από φθορο ή C1-4αλκύλιο· τα R2, R3 και R4 το καθένα ανεξαρτήτως είναι μια ομάδα που επιλέγεται από C1-6αλκύλιο ή φαινύλιο, κάθε ομάδα είναι προαιρετικώς υποκατεστημένη με έναν ή περισσότερους υποκατάστατες ανεξαρτήτως επιλεγμένους από φθορο ή C1-4αλκύλιο· b) αλογόνωσης ή σουλφινυλίωσης της ένωσης του τύπου (III) προς παραγωγή μιας ένωσης του τύπου (IV)· όπου το Χ είναι αλογονο-, ή -O-SO-R5, και το R5 είναι μια ομάδα που επιλέγεται από C6-10αρύλιο ή ετεροαρύλιο, κάθε ομάδα είναι προαιρετικώς υποκατεστημένη με έναν ή περισσότερους υποκατάστατες ανεξαρτήτως επιλεγμένους από χλωρο ή C1-4αλκύλιο· c) απο-αλογόνωσης ή αποσουλφινυλίωσης της ένωσης του τύπου (IV) προς παραγωγή της ένωσης του τύπου (V)· και d) αντίδρασης της ένωσης του τύπου (V) με ένα αναγωγικό μέσο προς παραγωγή της ένωσης του τύπου (Ι).
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161492297P | 2011-06-01 | 2011-06-01 | |
EP11168560 | 2011-06-01 | ||
EP12729053.4A EP2714712B1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
PCT/EP2012/060446 WO2012164095A1 (en) | 2011-06-01 | 2012-06-01 | Process for the production of estetrol intermediates |
Publications (1)
Publication Number | Publication Date |
---|---|
CY1118164T1 true CY1118164T1 (el) | 2017-06-28 |
Family
ID=44588329
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CY20161101090T CY1118164T1 (el) | 2011-06-01 | 2016-10-26 | Διεργασια για την παραγωγη ενδιαμεσων οιστετρολης |
Country Status (25)
Country | Link |
---|---|
US (1) | US11053273B2 (el) |
EP (1) | EP2714712B1 (el) |
JP (1) | JP6116550B2 (el) |
KR (1) | KR101957937B1 (el) |
CN (1) | CN103619867B (el) |
AU (1) | AU2012264601C1 (el) |
BR (1) | BR112013030833B1 (el) |
CA (1) | CA2835979C (el) |
CY (1) | CY1118164T1 (el) |
DK (1) | DK2714712T3 (el) |
EA (1) | EA025511B1 (el) |
ES (1) | ES2600703T3 (el) |
HR (1) | HRP20161369T1 (el) |
HU (1) | HUE031809T2 (el) |
LT (1) | LT2714712T (el) |
ME (1) | ME02585B (el) |
MX (1) | MX342537B (el) |
PL (1) | PL2714712T3 (el) |
PT (1) | PT2714712T (el) |
RS (1) | RS55293B1 (el) |
SG (1) | SG195121A1 (el) |
SI (1) | SI2714712T1 (el) |
SM (1) | SMT201600408B (el) |
WO (1) | WO2012164095A1 (el) |
ZA (1) | ZA201308445B (el) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI2714710T1 (sl) | 2011-06-01 | 2016-08-31 | Estetra S.P.R.L. | Postopek za proizvodnjo intermediatov estetrola |
SG195121A1 (en) | 2011-06-01 | 2013-12-30 | 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 |
CN103890001B (zh) | 2011-10-07 | 2016-05-04 | 埃斯特拉有限责任公司 | 用于制备雌四醇的方法 |
CN116077455A (zh) | 2015-06-18 | 2023-05-09 | 埃斯特拉有限责任公司 | 含雌四醇组分的口腔分散剂量单位 |
ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
SI3310346T1 (sl) | 2015-06-18 | 2021-07-30 | Estetra Sprl | Orodisperzibilna tableta, ki vsebuje estetrol |
CA2988498C (en) | 2015-06-18 | 2022-02-08 | Mithra Pharmaceuticals S.A. | 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 |
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 |
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 |
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NZ720906A (en) | 2013-12-12 | 2022-04-29 | Estetra Sprl | Orally disintegrating solid dosage unit containing an estetrol component |
SI3310346T1 (sl) | 2015-06-18 | 2021-07-30 | Estetra Sprl | Orodisperzibilna tableta, ki vsebuje estetrol |
CA2988498C (en) | 2015-06-18 | 2022-02-08 | Mithra Pharmaceuticals S.A. | Orodispersible dosage unit containing an estetrol component |
ES2877186T3 (es) | 2015-06-18 | 2021-11-16 | Estetra Sprl | Comprimido orodispersable que contiene estetrol |
CN116077455A (zh) | 2015-06-18 | 2023-05-09 | 埃斯特拉有限责任公司 | 含雌四醇组分的口腔分散剂量单位 |
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