MXPA04005188A - Metodo para la produccion de 6-alfa-fluorocorticosteroides. - Google Patents

Metodo para la produccion de 6-alfa-fluorocorticosteroides.

Info

Publication number
MXPA04005188A
MXPA04005188A MXPA04005188A MXPA04005188A MXPA04005188A MX PA04005188 A MXPA04005188 A MX PA04005188A MX PA04005188 A MXPA04005188 A MX PA04005188A MX PA04005188 A MXPA04005188 A MX PA04005188A MX PA04005188 A MXPA04005188 A MX PA04005188A
Authority
MX
Mexico
Prior art keywords
alpha
corticosteroids
fluoro
production
hydroxy
Prior art date
Application number
MXPA04005188A
Other languages
English (en)
Inventor
Zarbov Martin
Original Assignee
Taro Pharma Ind
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Taro Pharma Ind filed Critical Taro Pharma Ind
Publication of MXPA04005188A publication Critical patent/MXPA04005188A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

Un metodo para producir un corticosteroide 6a-fluorinado o un derivado del mismo haciendo reaccionar un 17-hidroxi-21-ester epoxido de Formula II con una agente de fluorizacion estereoselectivo para formar estereoselectivamente un compuesto 21-ester-17-hidroxi 6a-fluorinado de -Formula VII, R1 puede ser OC(O)-Rd; R4 puede ser C(O)-Rd; R3 puede ser H o Rd. Cada Rd puede ser igual o diferente y se selecciona independientemente a partir de alquilo de 1 a 4 atomos de carbono, arilo y heteroarilo. La linea punteada puede ser un enlace simple o doble. R4 puede ser, por ejemplo, acetilo; R3 puede ser, por ejemplo, alfa- o beta- metilo; R1 puede ser, por ejemplo, acetato o propionato. El agente de fluorizacion estereoselectivo empleado en la reaccion puede ser, por ejemplo, un compuesto fluoroquinuclidio, por ejemplo, Selectfluor(r).
MXPA04005188A 2001-11-29 2002-11-27 Metodo para la produccion de 6-alfa-fluorocorticosteroides. MXPA04005188A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US33375201P 2001-11-29 2001-11-29
PCT/US2002/038124 WO2003047329A2 (en) 2001-11-29 2002-11-27 Method for the preparation of 6-alpha-fluoro corticosteroids

Publications (1)

Publication Number Publication Date
MXPA04005188A true MXPA04005188A (es) 2004-08-11

Family

ID=23304110

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA04005188A MXPA04005188A (es) 2001-11-29 2002-11-27 Metodo para la produccion de 6-alfa-fluorocorticosteroides.

Country Status (10)

Country Link
US (2) US7098328B2 (es)
EP (1) EP1465855A2 (es)
JP (1) JP2005530679A (es)
CN (1) CN1596241A (es)
AU (1) AU2002359523A1 (es)
BR (1) BR0214520A (es)
CA (1) CA2473471A1 (es)
IL (1) IL162140A0 (es)
MX (1) MXPA04005188A (es)
WO (1) WO2003047329A2 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003047329A2 (en) 2001-11-29 2003-06-12 Taro Pharmaceuticals U.S.A., Inc. Method for the preparation of 6-alpha-fluoro corticosteroids
WO2006089406A1 (en) * 2005-02-22 2006-08-31 Gemin X Biotechnologies Inc. Diterpenoid compounds, compositions thereof and their use as anti-cancer or anti-fungal agents
US20070167420A1 (en) * 2005-04-07 2007-07-19 Daniella Gutman Process for preparing a crystalline form of halobetasol propionate
WO2012011106A1 (en) 2010-07-20 2012-01-26 Taro Pharmaceutical Industries Ltd. Process for the preparation of 17-desoxy-corticosteroids
ITMI20122200A1 (it) 2012-12-20 2014-06-21 Trifarma Spa Processo per la preparazione di 6-alfa-fluoro pregnani
CN109206467B (zh) * 2017-06-30 2022-09-09 天津药业研究院股份有限公司 一种丙酸氯倍他索的制备方法
CN112110972B (zh) * 2019-06-21 2022-03-18 河南利华制药有限公司 一种氯倍他索丙酸酯的制备方法
CN113480593A (zh) * 2021-07-05 2021-10-08 山东泰华生物科技股份有限公司 一种曲安奈德的制备方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU75903A1 (es) 1976-09-29 1978-05-16
US4036831A (en) 1975-10-28 1977-07-19 Steroid Development Company Establishment Trimethyl siloxane steroid intermediates
DE2655570A1 (de) 1975-12-12 1977-06-16 Ciba Geigy Ag Neue polyhalogensteroide und verfahren zu ihrer herstellung
CH631185A5 (en) 1978-01-01 1982-07-30 Ciba Geigy Ag Multiply halogenated steroids
NL187577C (nl) * 1978-04-05 1991-11-18 Sibla Srl 3-acetoxy-9beta,11beta-epoxy-pregna-1,3,5-trienen, werkwijze voor de bereiding daarvan en werkwijze voor de bereiding van 6alfa-halogeen-pregna-1,4-dieen-3-onen.
DE3071122D1 (en) 1979-11-16 1985-10-31 Sterosynt Ltd 6-alpha-fluoro-9-alpha-chloro-prednisolone-17,21 diesters, pharmaceutical compositions containing them and intermediates
JPS606700A (ja) * 1983-06-23 1985-01-14 Mitsubishi Chem Ind Ltd 含フツ素ステロイド化合物の製法
US5086178A (en) 1990-09-20 1992-02-04 Air Products And Chemicals, Inc. Fluorinated diazabicycloalkane derivatives
FR2701262B1 (fr) * 1993-02-05 1995-03-24 Roussel Uclaf Nouveau procédé de préparation de stéroïdes 6 alpa, 9 alpha-difluorés et nouveaus intermédiaires.
GB0026010D0 (en) 2000-10-24 2000-12-13 Air Prod & Chem N-fluorotriazinium fluorinating agents
IT1319663B1 (it) * 2000-11-17 2003-10-23 Farmabios Srl Processo per la preparazione di fluoro-steroidi.
PT102628B (pt) * 2001-06-12 2010-09-09 Hovione Farmaciencia S A Novo processo de preparação de flumetasona e do seu análogo 17-carboxilo androsteno
WO2003047329A2 (en) 2001-11-29 2003-06-12 Taro Pharmaceuticals U.S.A., Inc. Method for the preparation of 6-alpha-fluoro corticosteroids
CA2509366C (en) 2002-12-09 2008-04-15 Sicor Inc. Process for the preparation of pregnanes

Also Published As

Publication number Publication date
IL162140A0 (en) 2005-11-20
US7718793B2 (en) 2010-05-18
CA2473471A1 (en) 2003-06-12
BR0214520A (pt) 2006-05-30
US7098328B2 (en) 2006-08-29
EP1465855A2 (en) 2004-10-13
WO2003047329A3 (en) 2003-12-31
US20030162959A1 (en) 2003-08-28
CN1596241A (zh) 2005-03-16
AU2002359523A1 (en) 2003-06-17
WO2003047329A8 (en) 2003-10-30
WO2003047329A2 (en) 2003-06-12
JP2005530679A (ja) 2005-10-13
US20060247434A1 (en) 2006-11-02

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