ES2127413T3 - Sintesis de esteroides 17-(3-piridilo). - Google Patents

Sintesis de esteroides 17-(3-piridilo).

Info

Publication number
ES2127413T3
ES2127413T3 ES94927003T ES94927003T ES2127413T3 ES 2127413 T3 ES2127413 T3 ES 2127413T3 ES 94927003 T ES94927003 T ES 94927003T ES 94927003 T ES94927003 T ES 94927003T ES 2127413 T3 ES2127413 T3 ES 2127413T3
Authority
ES
Spain
Prior art keywords
beta
steroid
hydroxy
group
substituted
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES94927003T
Other languages
English (en)
Inventor
Gerard Andrew Potter
Ian Robert Hardcastle
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
BTG International Ltd
Original Assignee
BTG International Ltd
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
Priority claimed from GB939320132A external-priority patent/GB9320132D0/en
Priority claimed from GB9414192A external-priority patent/GB9414192D0/en
Application filed by BTG International Ltd filed Critical BTG International Ltd
Application granted granted Critical
Publication of ES2127413T3 publication Critical patent/ES2127413T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005Normal 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)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)

Abstract

UN METODO PARA PREPARAR UN ESTEROIDE 3 BE -HIDROXI- O 3 BE}(ACILOXI BAJO) 16,17-ENO-17-(3-PIRIDILO)-SUSTITUIDO, DONDE EL GRUPO 3{BE}-(ACILOXI BAJO) DE LOS ESTEROIDES TIENE DE 2 A 4 ATOMOS DE CARBONO, QUE COMPRENDE SOMETER UN ESTEROIDE 3{BE}HIDROXI-16,17-ENO-17-IODO O BROMO A UNA REACCION DE ENLACE CRUZADO COMPLEJO-CATALIZADA DE PALADIO CON UN BORANO (3PIRIDILO)-SUSTITUIDO EN LA QUE EL ANILLO DE PIRIDINA ES SUSTITUIDO EN LA POSICION-5 POR UN GRUPO ALQUILO DE 1 A 4 ATOMOS DE CARBONO O ES INSUSTITUIDO EN ESE PUNTO, EN UNA PROPORCION DE AL MENOS 1.0 EQUIVALENTE DE BORANO POR EQUIVALENTE DE ESTEROIDE, EN UN LIQUIDO ORGANICO QUE ES UN SOLVENTE PARA EL PRODUCTO DE REACCION ESTEROIDAL 3{BE}-HIDROXI, Y OPCIONALMENTE ESTERIFICANDO EL PRODUCTO DE REACCION ESTEROIDAL 3{BE}-HIDROXI RESULTANTE CON UN AGENTE ESTERIFICANTE EFICAZ PARA REEMPLAZAR EL GRUPO HIDROXI POR UN GRUPO DE ACILOXI BAJO MENCIONADO; EL METODO INCLUYE (A) LLEVAR A CABO LA REACCION CON NO MAS DE 1.2 EQUIVALENTES DE BORANO POR EQUIVALENTEDE ESTEROIDE O (B) CRISTALIZAR EL PRODUCTO DE LA REACCION DE ENLACE CRUZADO MEDIANTE UNA MEZCLA DE ACETONITRILO Y METANOL.
ES94927003T 1993-09-30 1994-09-22 Sintesis de esteroides 17-(3-piridilo). Expired - Lifetime ES2127413T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB939320132A GB9320132D0 (en) 1993-09-30 1993-09-30 Synthesis of 17-(-3-pyridyl)steroids
GB9414192A GB9414192D0 (en) 1994-07-14 1994-07-14 Synthesis of 17-(3-pyridyl) steroids

Publications (1)

Publication Number Publication Date
ES2127413T3 true ES2127413T3 (es) 1999-04-16

Family

ID=26303602

Family Applications (1)

Application Number Title Priority Date Filing Date
ES94927003T Expired - Lifetime ES2127413T3 (es) 1993-09-30 1994-09-22 Sintesis de esteroides 17-(3-piridilo).

Country Status (14)

Country Link
EP (1) EP0721461B1 (es)
JP (1) JP3722835B2 (es)
AT (1) ATE176481T1 (es)
AU (1) AU676088B2 (es)
CA (1) CA2170286C (es)
DE (1) DE69416419T2 (es)
DK (1) DK0721461T3 (es)
ES (1) ES2127413T3 (es)
GB (1) GB2282377B (es)
GR (1) GR3029601T3 (es)
HK (1) HK1002634A1 (es)
NZ (1) NZ273367A (es)
SG (1) SG49321A1 (es)
WO (1) WO1995009178A1 (es)

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US8569275B2 (en) 2002-08-28 2013-10-29 Harbor Therapeutics, Inc. Steroids having 7-oxgen and 17-heteroaryl substitution
US8236946B2 (en) 2004-08-24 2012-08-07 Btg International Limited Process for the preparation of 17-0-vinyl-triflates as intermediates
GB0418900D0 (en) * 2004-08-24 2004-09-29 Btg Int Ltd Novel salt forms
US20080051380A1 (en) 2006-08-25 2008-02-28 Auerbach Alan H Methods and compositions for treating cancer
CA2765983C (en) 2009-06-26 2017-11-14 Novartis Ag 1,3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
US8946260B2 (en) 2010-09-16 2015-02-03 Novartis Ag 17α-hydroxylase/C17,20-lyase inhibitors
CN102558274B (zh) * 2010-12-08 2014-10-15 深圳万乐药业有限公司 一种适合工业化生产醋酸阿比特龙的合成方法
CN102558275A (zh) * 2010-12-20 2012-07-11 天津药物研究院 α型多晶型醋酸阿比特龙结晶、其制备方法、用途和药物组合物
KR20140025492A (ko) 2011-04-28 2014-03-04 노파르티스 아게 17α-히드록실라제/C17,20-리아제 억제제
JP6091510B2 (ja) * 2011-10-10 2017-03-08 ザック システム 17−置換ステロイドの製造方法
CN103059090B (zh) * 2011-10-20 2016-06-22 连云港润众制药有限公司 醋酸阿比特龙草酸盐以及醋酸阿比特龙的纯化方法
CN102336801B (zh) * 2011-10-31 2013-05-15 南京卡文迪许生物工程技术有限公司 醋酸阿比特龙多晶型物和药用组合物
EP2607371A1 (en) 2011-12-23 2013-06-26 Crystal Pharma, S.A.U. Processes for the preparation of abiraterone and related compouds
CN103193849B (zh) * 2012-01-04 2016-05-04 连云港润众制药有限公司 一种高纯度醋酸阿比特龙的制备方法
CN103254265B (zh) 2012-02-21 2016-07-13 上海希迈医药科技有限公司 醋酸阿比特龙三氟乙酸盐及其制备方法和应用
CN102627681B (zh) * 2012-03-23 2016-04-13 山东新时代药业有限公司 一种醋酸阿比特龙的制备方法
EP2841444A4 (en) * 2012-04-23 2015-11-04 Alphora Res Inc PROCESS FOR PREPARING 17-SUBSTITUTED STEROIDS
CN102731605B (zh) * 2012-06-19 2016-04-13 鲁南制药集团股份有限公司 一种醋酸阿比特龙的纯化方法
WO2014009434A1 (en) 2012-07-11 2014-01-16 Sandoz Ag Self-microemulsifying drug delivery system of abiraterone or abiraterone acetate
WO2014009437A1 (en) 2012-07-11 2014-01-16 Sandoz Ag Oxidation stability of abiraterone acetate
WO2014009436A1 (en) 2012-07-11 2014-01-16 Sandoz Ag Nanosuspension of abiraterone acetate
CN102816199B (zh) * 2012-08-15 2015-04-08 武汉长联来福制药股份有限公司 醋酸阿比特龙二聚体化合物的制备及检测方法
CN102816200B (zh) * 2012-09-05 2015-04-15 中山大学 一种醋酸阿比特龙的制备方法
CN103665085B (zh) * 2012-09-24 2016-04-20 成都伊诺达博医药科技有限公司 一种改进的乙酸阿比特龙酯合成方法
CN102816201A (zh) * 2012-09-25 2012-12-12 成都伊诺达博医药科技有限公司 一种阿比特龙的纯化方法
WO2014058785A1 (en) 2012-10-10 2014-04-17 Novartis Ag Combination therapy
ITMI20121788A1 (it) 2012-10-22 2014-04-23 Olon Spa Procedimento per la purificazione di abiraterone acetato
WO2014071984A1 (en) 2012-11-09 2014-05-15 Synthon Bv Process for making abiraterone-3-acetate
EP2917226A1 (en) 2012-11-09 2015-09-16 Synthon BV Process for making the 17-triflate intermediate of abiraterone-3-acetate
WO2014075978A1 (en) 2012-11-16 2014-05-22 Synthon B.V. Process for the production of abiraterone-3-acetate involving an enol trliflation reaction in the presence of an alkoxy-pyridine compound
CN103059091B (zh) * 2012-11-22 2017-04-19 常州靶点医药科技有限公司 一种避免重金属残留的醋酸阿比特龙的制备方法
WO2014083512A1 (en) * 2012-11-28 2014-06-05 Dr. Reddy's Laboratories Limited Process for preparation of abiraterone acetate
HUE033085T2 (en) 2013-04-19 2017-11-28 Zach System A method of producing solid abiraterone acetate
WO2014188445A1 (en) * 2013-04-26 2014-11-27 Srinivasan Thirumalai Rajan PROCESS FOR THE PREPARATION OF (3β)-17-(3-PYRIDINYL)ANDROSTA-5,16-DIEN-3-YL ACETATE AND POLYMORPH THEREOF
CN103387597B (zh) * 2013-08-21 2015-03-25 苏州明锐医药科技有限公司 阿比特龙醋酸酯的制备方法
CN104558090A (zh) * 2013-10-28 2015-04-29 重庆医药工业研究院有限责任公司 醋酸阿比特龙杂质及其测定方法
WO2015102022A2 (en) * 2013-12-31 2015-07-09 Laurus Labs Private Limited An improved process for the preparation of abiraterone acetate
CA2938023C (en) 2014-01-28 2022-03-08 Olon S.P.A. Procedure for the preparation of abiraterone acetate and intermediates thereof
CN103965282B (zh) 2014-04-21 2016-01-20 武汉百科药物开发有限公司 一种醋酸阿比特龙的制备方法
EP3160450A1 (en) 2014-06-30 2017-05-03 Galenicum Health S.L. Stable pharmaceutical compositions in the form of immediate release tablets
CZ2014475A3 (cs) 2014-07-09 2016-01-20 Zentiva, K.S. Způsob přípravy Abirateron acetátu o vysoké čistotě aplikovatelný v průmyslovém měřítku
CN105622703B (zh) * 2014-11-05 2019-09-27 兰州大学 一种制备醋酸阿比特龙的方法
US20180028521A1 (en) 2016-07-29 2018-02-01 Janssen Pharmaceutica Nv Methods of Treating Prostate Cancer
CN107056871A (zh) * 2017-06-28 2017-08-18 李建恒 一种阿比特龙醋酸酯的合成方法
HU231297B1 (hu) 2018-07-31 2022-09-28 Richter Gedeon Nyrt Stabil gyógyszerkészítmények és eljárás az előállításukra
CN109134571B (zh) * 2018-09-13 2020-10-02 浙江工业大学 一种17-碘-雄甾-5,16-二烯-3β-醇的制备方法
EP3944860A1 (en) 2020-07-30 2022-02-02 Galenicum Health S.L.U. Abiraterone for use in a method of treating cancer
CN112125942B (zh) * 2020-09-28 2021-12-14 湖南新合新生物医药有限公司 醋酸阿比特龙及其中间体的合成方法
CN112940065A (zh) * 2021-02-03 2021-06-11 山东大学 三氟甲磺酸盐在制备醋酸阿比特龙中的应用及合成方法
CN114709557B (zh) * 2022-04-13 2023-10-27 南京工业大学 一种后修饰碳硼烷的共价有机框架材料的设计合成及其在锂硫电池隔膜中的应用

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ249911A (en) * 1992-03-31 1996-06-25 British Tech Group 17-(3-pyridyl) substituted steroids and use in pharmaceutical compositions

Also Published As

Publication number Publication date
ATE176481T1 (de) 1999-02-15
AU676088B2 (en) 1997-02-27
DE69416419D1 (de) 1999-03-18
EP0721461B1 (en) 1999-02-03
JPH09502994A (ja) 1997-03-25
SG49321A1 (en) 1998-05-18
HK1002634A1 (en) 1998-09-04
GR3029601T3 (en) 1999-06-30
NZ273367A (en) 1997-07-27
GB2282377A (en) 1995-04-05
JP3722835B2 (ja) 2005-11-30
GB9419139D0 (en) 1994-11-09
WO1995009178A1 (en) 1995-04-06
AU7661894A (en) 1995-04-18
CA2170286C (en) 2005-04-05
EP0721461A1 (en) 1996-07-17
GB2282377B (en) 1997-09-03
DE69416419T2 (de) 1999-06-10
CA2170286A1 (en) 1995-04-06
DK0721461T3 (da) 1999-09-20

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