PE20030926A1 - Proceso para la preparacion de 7-alfa-metilesteroides - Google Patents
Proceso para la preparacion de 7-alfa-metilesteroidesInfo
- Publication number
- PE20030926A1 PE20030926A1 PE2003000062A PE2003000062A PE20030926A1 PE 20030926 A1 PE20030926 A1 PE 20030926A1 PE 2003000062 A PE2003000062 A PE 2003000062A PE 2003000062 A PE2003000062 A PE 2003000062A PE 20030926 A1 PE20030926 A1 PE 20030926A1
- Authority
- PE
- Peru
- Prior art keywords
- steroid
- copper
- formula
- grignard reagent
- preparation
- Prior art date
Links
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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0085—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being a saturated hydrocarbon 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
-
- 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
- C07J1/0081—Substituted in position 17 alfa and 17 beta
- C07J1/0088—Substituted in position 17 alfa and 17 beta the substituent in position 17 alfa being an unsaturated hydrocarbon group
- C07J1/0096—Alkynyl derivatives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
- C07J5/0007—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa
- C07J5/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond not substituted in position 17 alfa not substituted in position 16
-
- 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)
- Steroid Compounds (AREA)
Abstract
SE REFIERE A UN PROCESO PARA LA PREPARACION DE 7O-ESTEROIDES DE FORMULA I DONDE R1 ES H, METIL, ENTRE OTROS; R2 ES (CH2)nOH DONDE n ES 0-2: POR UNA ADICION DE 1,6-CONJUGADO MEDIADO CON COBRE DE REACTIVO DE GRIGNARD CH3MgX DONDE X ES HALOGENO, PARA LOS 3-CETOESTEROIDES 4,6-NO SATURADO DE FORMULA II, COMPRENDIENDO PROTECCION AL GRUPO HIDROXI DEL ESTEROIDE DE FORMULA II CON UN GRUPO DE TRIALQUILSILIL SEGUIDO POR EL TRATAMIENTO DEL ESTEROIDE PROTEGIDO DE OH CON EL REACTIVO DE GRIGNARD. EL SOLVENTE DE LA REACCION ES TETRAHIDROFURANO, ETER DIETIL; LA CONCENTRACION DEL ESTEROIDE AL REACTIVO DE GRIGNARD ES DE 1:1 A 1:7 Y SE USA ACETATO DE COBRE (II) DEL CATALIZADOR DE COBRE O CLORURO DE COBRE (II) Y LA REACCION SE LLEVA A -78°C A O°C. EL COMPUESTO ESTEROIDE ES 21-HIDROXI-19-NORPREGN-4,6-DIEN-3-ONA.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02075230 | 2002-01-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20030926A1 true PE20030926A1 (es) | 2003-10-29 |
Family
ID=8185555
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2003000062A PE20030926A1 (es) | 2002-01-21 | 2003-01-20 | Proceso para la preparacion de 7-alfa-metilesteroides |
Country Status (28)
Country | Link |
---|---|
US (2) | US20050090476A1 (es) |
EP (1) | EP1470151B1 (es) |
JP (1) | JP5250174B2 (es) |
KR (1) | KR100937179B1 (es) |
CN (1) | CN100372864C (es) |
AR (1) | AR038165A1 (es) |
AT (1) | ATE453659T1 (es) |
AU (1) | AU2003205604B8 (es) |
BR (1) | BRPI0306736B8 (es) |
CA (1) | CA2472379C (es) |
DE (1) | DE60330749D1 (es) |
EC (1) | ECSP045180A (es) |
EG (1) | EG23417A (es) |
ES (1) | ES2336439T3 (es) |
HR (1) | HRP20040634B1 (es) |
IL (2) | IL162770A0 (es) |
IS (1) | IS2740B (es) |
MX (1) | MXPA04007049A (es) |
NO (1) | NO327095B1 (es) |
NZ (1) | NZ533970A (es) |
PE (1) | PE20030926A1 (es) |
PL (1) | PL208163B1 (es) |
RO (1) | RO122913B1 (es) |
RS (1) | RS51490B (es) |
RU (1) | RU2305105C2 (es) |
TW (1) | TWI322813B (es) |
WO (1) | WO2003059931A1 (es) |
ZA (1) | ZA200405257B (es) |
Families Citing this family (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE10213371C1 (de) * | 2002-03-21 | 2003-12-24 | Schering Ag | Verfahren zur Herstellung von 7alpha-Methylsteroiden |
GB0304927D0 (en) * | 2003-03-04 | 2003-04-09 | Resolution Chemicals Ltd | Process for the production of tibolone |
KR100716981B1 (ko) * | 2004-09-30 | 2007-05-10 | 삼성전자주식회사 | 대중교통의 최적경로 검색방법 및 이를 이용한 휴대용 기기 |
CA2765610A1 (en) * | 2009-06-29 | 2011-01-06 | Merz Pharma Gmbh & Co. Kgaa | Method of preparing 3,3,5,5-tetramethylcyclohexanone |
CN111944001A (zh) * | 2020-07-09 | 2020-11-17 | 浙江神洲药业有限公司 | 一种替勃龙的制备方法 |
Family Cites Families (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3341557A (en) * | 1961-06-05 | 1967-09-12 | Upjohn Co | 7-methyltestosterones |
US3470216A (en) * | 1966-11-29 | 1969-09-30 | Du Pont | Selected 17,17-difluoro unsaturated androstanes |
FR2054527B1 (es) * | 1969-07-28 | 1973-06-08 | Roussel Uclaf | |
US3798213A (en) * | 1971-01-25 | 1974-03-19 | Merck & Co Inc | 7 alpha-methyl-20-spiroxane-3-ones and process |
DE2558088C2 (de) * | 1975-12-19 | 1985-05-30 | Schering AG, 1000 Berlin und 4709 Bergkamen | Verfahren zur Herstellung von 4-Androsten-3,17-dion-Derivaten |
JPS56145239A (en) * | 1980-04-11 | 1981-11-11 | Sumitomo Chem Co Ltd | Novel bicyclooctane derivative and its preparation |
US4298559A (en) * | 1980-07-23 | 1981-11-03 | Dow Corning Corporation | High yield silicon carbide from alkylated or arylated pre-ceramic polymers |
US6548491B2 (en) * | 1997-12-24 | 2003-04-15 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
US6054446A (en) * | 1997-12-24 | 2000-04-25 | Sri International | Anti-estrogenic steroids, and associated pharmaceutical compositions and methods of use |
EP1212345B1 (en) * | 1999-04-06 | 2003-08-06 | Akzo Nobel N.V. | Orally active 7-alpha-alkyl androgens |
TW548277B (en) * | 1999-07-16 | 2003-08-21 | Akzo Nobel Nv | Orally active androgens |
PL202999B1 (pl) * | 1999-12-02 | 2009-08-31 | Organon Nv | Androgeny zawierające pierścień cyklopropanowy w pozycjach 14, 15 i zastosowanie takich androgenów |
US6784170B2 (en) * | 2000-02-11 | 2004-08-31 | Sri International | Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one |
BR0112791A (pt) * | 2000-07-28 | 2003-06-24 | Akzo Nobel Nv | Composto esteroidal 16alfa-substituido, uso do mesmo, métodos de tratamento para ativação seletiva de receptores de estrogênio do subtipo alfa, e para terapia de reposição hormonal ou contracepção, e, composição farmacêutica |
US20040010138A1 (en) * | 2002-03-21 | 2004-01-15 | Schering Ag | Process for the production of 7alpha-methyl steroids |
US7304157B2 (en) * | 2004-09-28 | 2007-12-04 | Bristol-Myers Squibb Company | Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones |
-
2003
- 2003-01-14 RS YUP-630/04A patent/RS51490B/sr unknown
- 2003-01-14 JP JP2003560033A patent/JP5250174B2/ja not_active Expired - Lifetime
- 2003-01-14 AU AU2003205604A patent/AU2003205604B8/en not_active Expired
- 2003-01-14 RO ROA200400656A patent/RO122913B1/ro unknown
- 2003-01-14 US US10/502,259 patent/US20050090476A1/en not_active Abandoned
- 2003-01-14 DE DE60330749T patent/DE60330749D1/de not_active Expired - Lifetime
- 2003-01-14 CN CNB038024918A patent/CN100372864C/zh not_active Expired - Lifetime
- 2003-01-14 CA CA2472379A patent/CA2472379C/en not_active Expired - Lifetime
- 2003-01-14 WO PCT/EP2003/000339 patent/WO2003059931A1/en active IP Right Grant
- 2003-01-14 BR BRPI0306736A patent/BRPI0306736B8/pt not_active IP Right Cessation
- 2003-01-14 MX MXPA04007049A patent/MXPA04007049A/es active IP Right Grant
- 2003-01-14 EP EP03702441A patent/EP1470151B1/en not_active Expired - Lifetime
- 2003-01-14 KR KR1020047010985A patent/KR100937179B1/ko active IP Right Grant
- 2003-01-14 IL IL16277003A patent/IL162770A0/xx unknown
- 2003-01-14 PL PL371583A patent/PL208163B1/pl unknown
- 2003-01-14 TW TW092100693A patent/TWI322813B/zh not_active IP Right Cessation
- 2003-01-14 AT AT03702441T patent/ATE453659T1/de not_active IP Right Cessation
- 2003-01-14 RU RU2004125580/04A patent/RU2305105C2/ru active
- 2003-01-14 NZ NZ533970A patent/NZ533970A/en not_active IP Right Cessation
- 2003-01-14 ES ES03702441T patent/ES2336439T3/es not_active Expired - Lifetime
- 2003-01-19 EG EG2003010051A patent/EG23417A/xx active
- 2003-01-20 AR ARP030100149A patent/AR038165A1/es unknown
- 2003-01-20 PE PE2003000062A patent/PE20030926A1/es active IP Right Grant
-
2004
- 2004-06-28 IS IS7339A patent/IS2740B/is unknown
- 2004-06-29 IL IL162770A patent/IL162770A/en active IP Right Grant
- 2004-07-01 ZA ZA2004/05257A patent/ZA200405257B/en unknown
- 2004-07-06 EC EC2004005180A patent/ECSP045180A/es unknown
- 2004-07-12 HR HRP20040634AA patent/HRP20040634B1/hr not_active IP Right Cessation
- 2004-08-19 NO NO20043455A patent/NO327095B1/no not_active IP Right Cessation
-
2010
- 2010-04-22 US US12/765,629 patent/US20100204497A1/en not_active Abandoned
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Legal Events
Date | Code | Title | Description |
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FC | Refusal | ||
FG | Grant, registration |