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MX2016004263A - Proceso industrial para la sintesis de acetato de ulipristal y su analogo 4'-acetil. - Google Patents

Proceso industrial para la sintesis de acetato de ulipristal y su analogo 4'-acetil.

Info

Publication number
MX2016004263A
MX2016004263A MX2016004263A MX2016004263A MX2016004263A MX 2016004263 A MX2016004263 A MX 2016004263A MX 2016004263 A MX2016004263 A MX 2016004263A MX 2016004263 A MX2016004263 A MX 2016004263A MX 2016004263 A MX2016004263 A MX 2016004263A
Authority
MX
Mexico
Prior art keywords
synthesis
industrial process
ulipristal acetate
acetyl
analogue
Prior art date
Application number
MX2016004263A
Other languages
English (en)
Other versions
MX355222B (es
Inventor
Mahó Sándor
Sánta Csaba
Csörgei János
Horváth János
Aranyi Antal
BÉNI Zoltán
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 MX2016004263A publication Critical patent/MX2016004263A/es
Publication of MX355222B publication Critical patent/MX355222B/es

Links

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
    • 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
    • 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
    • A61P5/30Oestrogens
    • 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
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J7/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/004Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa
    • C07J7/0045Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group substituted in position 17 alfa not substituted in position 16
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J75/00Processes for the preparation of steroids in general
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)

Abstract

La presente invención se refiere a un nuevo proceso para la síntesis de compuestos de fórmula (I) (en donde el significado de R es grupo dimetilamino o acetilo) (ver Fórmula) usando el compuesto de fórmula (II) (en donde el significado de R es grupo dimetilamino o 2-metil-1,3-dioxolan-2-ilo) como material de inicio, así como también con el intermediario del proceso.
MX2016004263A 2013-10-01 2014-10-01 Proceso industrial para la sintesis de acetato de ulipristal y su analogo 4'-acetil. MX355222B (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HU1300566A HU230319B1 (hu) 2013-10-01 2013-10-01 Ipari eljárás szteroid hatóanyagok előállítására
PCT/IB2014/064979 WO2015049637A1 (en) 2013-10-01 2014-10-01 Industrial process for the synthesis of ulipristal acetate and its 4'-acetyl analogue

Publications (2)

Publication Number Publication Date
MX2016004263A true MX2016004263A (es) 2016-10-12
MX355222B MX355222B (es) 2018-04-10

Family

ID=89991273

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016004263A MX355222B (es) 2013-10-01 2014-10-01 Proceso industrial para la sintesis de acetato de ulipristal y su analogo 4'-acetil.

Country Status (32)

Country Link
US (1) US9676814B2 (es)
EP (1) EP3052513B1 (es)
JP (1) JP6796366B2 (es)
KR (1) KR20160062046A (es)
CN (1) CN105593236B (es)
AR (1) AR097878A1 (es)
AU (1) AU2014330860B2 (es)
BR (1) BR112016006979B1 (es)
CA (1) CA2924553C (es)
CY (1) CY1121286T1 (es)
DK (1) DK3052513T3 (es)
EA (1) EA030905B1 (es)
ES (1) ES2713325T3 (es)
GE (1) GEP20186827B (es)
HR (1) HRP20190414T1 (es)
HU (2) HU230319B1 (es)
IL (1) IL244501A0 (es)
LT (1) LT3052513T (es)
ME (1) ME03337B (es)
MX (1) MX355222B (es)
MY (1) MY176613A (es)
PL (1) PL3052513T3 (es)
PT (1) PT3052513T (es)
RS (1) RS58252B1 (es)
SG (1) SG11201601683SA (es)
SI (1) SI3052513T1 (es)
SM (1) SMT201900125T1 (es)
TR (1) TR201901381T4 (es)
UA (1) UA118269C2 (es)
UY (1) UY35766A (es)
WO (1) WO2015049637A1 (es)
ZA (1) ZA201601589B (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU230381B1 (hu) * 2014-02-17 2016-03-29 Richter Gedeon Nyrt Ipari eljárás szteroid intermedier előállítására
CN105237607B (zh) * 2015-10-29 2018-10-02 国家卫生计生委科学技术研究所 醋酸乌利司他晶k型物质及制备方法和其组合物与用途
CN112578037A (zh) * 2020-11-12 2021-03-30 湖南新合新生物医药有限公司 一种检测醋酸乌利司他中间体ⅰ中乌双缩酮含量的方法
CN112461957B (zh) * 2020-11-12 2022-02-22 湖南新合新生物医药有限公司 一种检测醋酸乌利司他中间体ii中杂质含量的方法

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE194358T1 (de) * 1996-05-01 2000-07-15 Us Gov Health & Human Serv 21-substituierte progesteron derivate als antigestagene
US6020328A (en) * 1998-03-06 2000-02-01 Research Triangle Institute 20-keto-11β-arylsteroids and their derivatives having agonist or antagonist hormonal properties
AU4584901A (en) 2000-03-17 2001-10-15 Us Gov Health & Human Serv Structural modification of 19-norprogesterone i: 17-alpha-substituted-11-beta-substituted-4-aryl and 21-substituted 19-norpregnadienedione as new antiprogestational agents
US20060111577A1 (en) * 2003-02-28 2006-05-25 Kim Hyun K Method for preparing 17 alpha-acetoxy-11beta-(4-n,n-dimethylaminophenyl)-19-norpregna-4,9-diene-3,20-dione, intermediates thereof, and methods for the preparation of such intermediates
HU227112B1 (hu) 2006-06-14 2010-07-28 Richter Gedeon Nyrt 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
HU228636B1 (en) * 2007-06-27 2013-04-29 Richter Gedeon Nyrt Industrial method for the synthesis of 17-acetoxy-11betha-4[-(dimethylamino)-phenyl]-21-methoxy-19-norpregna-4,9-dien-3,20-dione and the key intermediates of the process
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
CN103601785A (zh) 2013-11-25 2014-02-26 四川大学 一种醋酸优力斯特新的合成方法

Also Published As

Publication number Publication date
JP6796366B2 (ja) 2020-12-09
MX355222B (es) 2018-04-10
AU2014330860A1 (en) 2016-03-24
BR112016006979A2 (pt) 2017-08-01
MY176613A (en) 2020-08-18
SI3052513T1 (sl) 2019-03-29
CA2924553A1 (en) 2015-04-09
GEP20186827B (en) 2018-02-26
CN105593236A (zh) 2016-05-18
HUP1300566A2 (en) 2015-04-28
KR20160062046A (ko) 2016-06-01
HU230319B1 (hu) 2016-01-28
RS58252B1 (sr) 2019-03-29
EP3052513B1 (en) 2018-12-05
DK3052513T3 (en) 2019-03-25
CY1121286T1 (el) 2020-05-29
UY35766A (es) 2015-04-30
JP2016533347A (ja) 2016-10-27
HRP20190414T1 (hr) 2019-04-19
ZA201601589B (en) 2017-07-26
BR112016006979B1 (pt) 2022-05-03
AU2014330860B2 (en) 2018-10-18
PL3052513T3 (pl) 2019-05-31
US9676814B2 (en) 2017-06-13
IL244501A0 (en) 2016-04-21
SMT201900125T1 (it) 2019-05-10
CN105593236B (zh) 2017-11-28
US20160311849A1 (en) 2016-10-27
WO2015049637A1 (en) 2015-04-09
AR097878A1 (es) 2016-04-20
UA118269C2 (uk) 2018-12-26
NZ717638A (en) 2021-05-28
HUE043002T2 (hu) 2019-07-29
LT3052513T (lt) 2019-02-25
EA201690467A1 (ru) 2016-07-29
TR201901381T4 (tr) 2019-02-21
ES2713325T3 (es) 2019-05-21
CA2924553C (en) 2021-10-19
HK1223105A1 (en) 2017-07-21
EA030905B1 (ru) 2018-10-31
EP3052513A1 (en) 2016-08-10
ME03337B (me) 2019-10-20
SG11201601683SA (en) 2016-04-28
PT3052513T (pt) 2019-03-01

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