ZA200809799B - Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process - Google Patents

Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

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Publication number
ZA200809799B
ZA200809799B ZA200809799A ZA200809799A ZA200809799B ZA 200809799 B ZA200809799 B ZA 200809799B ZA 200809799 A ZA200809799 A ZA 200809799A ZA 200809799 A ZA200809799 A ZA 200809799A ZA 200809799 B ZA200809799 B ZA 200809799B
Authority
ZA
South Africa
Prior art keywords
norpregna
acetoxy
dione
diene
dimethyl
Prior art date
Application number
ZA200809799A
Other languages
English (en)
Inventor
Dancsi Lajosne
Visky Gyoergy
Tuba Zoltan
Csoergei Janos
Molnar Csaba
Magyari Endrene
Original Assignee
Richter Gedeon Nyrt
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 Richter Gedeon Nyrt filed Critical Richter Gedeon Nyrt
Publication of ZA200809799B publication Critical patent/ZA200809799B/xx

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/006Ketals at position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • 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
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
ZA200809799A 2006-06-14 2008-11-17 Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process ZA200809799B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
HU0600491A HU227112B1 (hu) 2006-06-14 2006-06-14 Ipari eljárás 17-alfa-acetoxi-11-béta-[4-(N,N-dimetil-amino)-fenil]-19-norpregna-4,9-dién-3,20-dion elõállítására és új intermedierek az eljáráshoz

Publications (1)

Publication Number Publication Date
ZA200809799B true ZA200809799B (en) 2009-11-25

Family

ID=89986843

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200809799A ZA200809799B (en) 2006-06-14 2008-11-17 Industrial process for the synthesis of 17α-acetoxy-11β-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

Country Status (22)

Country Link
US (1) US8110691B2 (pl)
EP (1) EP2027140B1 (pl)
JP (1) JP5274453B2 (pl)
CN (1) CN101466723B (pl)
AR (1) AR061052A1 (pl)
AU (1) AU2007258955B2 (pl)
BR (1) BRPI0713157A2 (pl)
CA (1) CA2653552C (pl)
DK (1) DK2027140T3 (pl)
EA (1) EA015302B1 (pl)
ES (1) ES2409841T3 (pl)
HU (1) HU227112B1 (pl)
IL (1) IL195253A (pl)
MX (1) MX2008015972A (pl)
NO (1) NO341620B1 (pl)
PL (1) PL2027140T3 (pl)
PT (1) PT2027140E (pl)
RS (1) RS52758B (pl)
SI (1) SI2027140T1 (pl)
UA (1) UA94269C2 (pl)
WO (1) WO2007144674A1 (pl)
ZA (1) ZA200809799B (pl)

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CN102241722B (zh) * 2010-05-12 2015-11-25 杭州容立医药科技有限公司 一种合成孕酮受体调节剂优力司特的纯化方法
CN102372760A (zh) * 2010-08-12 2012-03-14 杭州容立医药科技有限公司 一种合成孕酮受体调节剂优力司特的合成方法
CN102477060B (zh) * 2010-11-22 2014-08-13 华润紫竹药业有限公司 甾体化合物及其制备方法和用途
CN102516345B (zh) 2011-11-01 2014-11-26 上海优拓医药科技有限公司 醋酸乌利司他及其关键中间体的制备方法
CN102295674B (zh) * 2011-07-14 2013-04-10 四川大学 获得高纯度17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的方法
CN102321141B (zh) * 2011-07-22 2013-05-15 上海希迈医药科技有限公司 一种17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的无定形物及其制备方法
CN102344478B (zh) * 2011-07-22 2013-08-07 上海希迈医药科技有限公司 一种17α-乙酰氧基-11β-(4-N,N-二甲氨基苯基)-19-去甲孕甾-4,9-二烯-3,20-二酮的结晶物及其制备方法
CN103193850A (zh) * 2012-01-04 2013-07-10 北京紫竹药业有限公司 甾体化合物的新晶型及其制备方法
CN106046099B (zh) * 2012-01-19 2018-03-16 华润紫竹药业有限公司 甾体化合物及其制备方法和用途
CN104628806A (zh) * 2012-01-19 2015-05-20 华润紫竹药业有限公司 甾体化合物及其制备方法和用途
CN103755765B (zh) * 2012-04-17 2018-01-02 常州市第四制药厂有限公司 醋酸乌利司他的多晶型及其制备方法
CN102675395B (zh) * 2012-04-17 2014-04-30 常州市第四制药厂有限公司 醋酸乌利司他的多晶型及其制备方法
CN102702296B (zh) * 2012-06-19 2014-09-03 山东诚创医药技术开发有限公司 环-3,20-双(1,2-亚乙基缩醛)-17α-羟基-17β-乙酰基-雌甾-5(10),9(11)-二烯-3-酮的制备方法
JP6474722B2 (ja) 2012-09-28 2019-02-27 あすか製薬株式会社 ウリプリスタール酢酸エステルの結晶多形
CA2885798A1 (en) 2012-09-28 2014-04-03 Aska Pharmaceutical Co., Ltd. Crystalline polymorphic form of ulipristal acetate
JP6200493B2 (ja) 2012-09-28 2017-09-20 あすか製薬株式会社 無定形ウリプリスタール酢酸エステル
CN102875629B (zh) * 2012-10-10 2014-11-19 苏州康润医药有限公司 醋酸乌利司他的合成方法
WO2014060888A1 (en) * 2012-10-18 2014-04-24 Lupin Limited Novel process and intermediate for preparation of ulipristal
CN102942612A (zh) * 2012-10-30 2013-02-27 四川大学 一种合成醋酸乌利司他的新方法
CN103804456B (zh) * 2012-11-15 2017-08-04 上海创诺医药集团有限公司 醋酸乌利司他中间体及其制备方法
CN103145787B (zh) * 2012-12-25 2017-02-22 常州市亚邦医药研究所有限公司 制备醋酸优力司特关键中间体的新方法
CN103087140A (zh) * 2013-03-04 2013-05-08 四川尚锐生物医药有限公司 一种醋酸优力司特多晶型的制备方法
CN103145788B (zh) * 2013-03-25 2015-08-19 浙江仙琚制药股份有限公司 醋酸优力司特关键中间体的制备方法
HU230319B1 (hu) * 2013-10-01 2016-01-28 Richter Gedeon Nyrt. Ipari eljárás szteroid hatóanyagok előállítására
CN103755763A (zh) * 2013-12-30 2014-04-30 烟台东诚生化股份有限公司 17α-乙酰氧基-11β-[4-(N,N-二甲基氨基)-苯基]-19-去甲孕甾-4,9-二烯-3,20-二酮的制备方法
CN104530169B (zh) * 2014-12-12 2017-09-12 成都化润药业有限公司 一种醋酸乌利司他及其中间体的制备方法
CN106986908B (zh) * 2017-03-23 2019-05-10 湖南玉新药业有限公司 倍他米松的制备方法
CN106986911B (zh) * 2017-03-23 2019-05-10 湖南玉新药业有限公司 地塞米松关键中间体联烯亚砜物的制备方法
CN108558982A (zh) * 2018-05-21 2018-09-21 郑州泰丰制药有限公司 一种新型醋酸乌利司他以及其生产制造方法
CN109053846B (zh) * 2018-08-14 2020-01-07 台州仙琚药业有限公司 制备醋酸优力司特双缩酮的方法
CN111349137A (zh) * 2018-12-21 2020-06-30 北京启慧生物医药有限公司 一种绿色合成醋酸乌利司他中间体及醋酸乌利司他的方法
CN110256519B (zh) * 2019-05-23 2021-06-08 江苏联环药业股份有限公司 一锅法制备醋酸乌利司他的方法

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US4041055A (en) * 1975-11-17 1977-08-09 The Upjohn Company Process for the preparation of 17α-hydroxyprogesterones and corticoids from androstenes
US4954490A (en) 1988-06-23 1990-09-04 Research Triangle Institute 11 β-substituted progesterone analogs
US5929262A (en) * 1995-03-30 1999-07-27 The United States Of America As Represented By The Department Of Health And Human Services Method for preparing 17α-acetoxy-11β-(4-N, N-dimethylaminophyl)-19-Norpregna-4,9-diene-3, 20-dione, intermediates useful in the method, and methods for the preparation of such intermediates
AU775831B2 (en) * 1999-12-29 2004-08-19 Government Of The United States Of America, As Represented By The Secretary Of The Department Of Health And Human Services, The Process for preparing 17alpha-acetoxy-11beta-(4-N,N-(dimethylamino)phenyl)-21- methoxy-19-norpregna-4,9-diene-3,20-dione, intermediates useful in the process, and processes for preparing such intermediates
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EP1613640A4 (en) 2003-02-28 2010-05-19 Us Gov Health & Human Serv PROCESS FOR PREPARING 17 ALPHA-ACETOXY-11 BETA- (4-N, N-DIMETHYLAMINOPHENYL) -19-NORPREGNA-4,9-DIENE-3,20-DION, INTERMEDIATE PRODUCTS AND METHOD OF MANUFACTURING THESE INTERMEDIATE PRODUCTS
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Also Published As

Publication number Publication date
US8110691B2 (en) 2012-02-07
EP2027140A1 (en) 2009-02-25
JP5274453B2 (ja) 2013-08-28
DK2027140T3 (da) 2013-06-03
AU2007258955B2 (en) 2012-09-20
RS52758B (en) 2013-08-30
HU0600491D0 (en) 2006-08-28
WO2007144674A1 (en) 2007-12-21
IL195253A0 (en) 2009-08-03
ES2409841T3 (es) 2013-06-28
UA94269C2 (en) 2011-04-26
EA200900015A1 (ru) 2009-04-28
CA2653552A1 (en) 2007-12-21
CA2653552C (en) 2013-04-23
NO341620B1 (no) 2017-12-11
CN101466723A (zh) 2009-06-24
HU227112B1 (hu) 2010-07-28
AR061052A1 (es) 2008-07-30
BRPI0713157A2 (pt) 2012-04-03
US20090187032A1 (en) 2009-07-23
PL2027140T3 (pl) 2013-09-30
NO20090196L (no) 2009-03-10
JP2009539964A (ja) 2009-11-19
IL195253A (en) 2011-11-30
EA015302B1 (ru) 2011-06-30
PT2027140E (pt) 2013-06-04
CN101466723B (zh) 2011-11-02
HUP0600491A2 (en) 2008-02-28
EP2027140B1 (en) 2013-03-13
SI2027140T1 (sl) 2013-07-31
MX2008015972A (es) 2009-01-12
AU2007258955A1 (en) 2007-12-21

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