WO2017081702A3 - A process for preparation of enzalutamide - Google Patents

A process for preparation of enzalutamide Download PDF

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Publication number
WO2017081702A3
WO2017081702A3 PCT/IN2016/050388 IN2016050388W WO2017081702A3 WO 2017081702 A3 WO2017081702 A3 WO 2017081702A3 IN 2016050388 W IN2016050388 W IN 2016050388W WO 2017081702 A3 WO2017081702 A3 WO 2017081702A3
Authority
WO
WIPO (PCT)
Prior art keywords
enzalutamide
preparation
fluoro
methyl
isothiocyanato
Prior art date
Application number
PCT/IN2016/050388
Other languages
French (fr)
Other versions
WO2017081702A2 (en
Inventor
Rajamannar Thennati
Shriprakash Dhar DWIVEDI
Arunkumar Gulabsingh Yadav
Nischalkumar Vinodbhai Patel
Sunil Rajaram KARANKE
Original Assignee
Sun Pharmaceutical Industries Limited
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 Sun Pharmaceutical Industries Limited filed Critical Sun Pharmaceutical Industries Limited
Publication of WO2017081702A2 publication Critical patent/WO2017081702A2/en
Publication of WO2017081702A3 publication Critical patent/WO2017081702A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/86—Oxygen and sulfur atoms, e.g. thiohydantoin

Abstract

The present invention relates to an improved process for preparation of enzalutamide which involves direct condensation of 2-(4-alkoxycarbonyl-3-fluoro-anilino)-2-methyl-propanoic acid and 4-isothiocyanato-2-(trifluoromethyl)benzonitrile to obtain alkyl 4-[3-(4-cyano-3- methyl-phenyl)-5,5-dimethyl-4-oxo-2-thioxo-imidazolidin-1-yl]-2-fluoro-benzoate, which is further converted to enzalutamide.
PCT/IN2016/050388 2015-11-09 2016-11-08 A process for preparation of enzalutamide WO2017081702A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN4279MU2015 2015-11-09
IN4279/MUM/2015 2015-11-09

Publications (2)

Publication Number Publication Date
WO2017081702A2 WO2017081702A2 (en) 2017-05-18
WO2017081702A3 true WO2017081702A3 (en) 2017-07-13

Family

ID=58694873

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2016/050388 WO2017081702A2 (en) 2015-11-09 2016-11-08 A process for preparation of enzalutamide

Country Status (1)

Country Link
WO (1) WO2017081702A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20220242829A1 (en) 2019-06-27 2022-08-04 Synthon B.V. Process for preparation of enzalutamide
CN114805327A (en) * 2021-01-29 2022-07-29 苏州开拓药业股份有限公司 Intermediate for thiohydantoin medicine and preparation method and application thereof

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015063720A1 (en) * 2013-10-31 2015-05-07 Ranbaxy Laboratories Limited Process for the preparation of enzalutamide
CN104803919A (en) * 2014-01-26 2015-07-29 上海医药工业研究院 Preparation method of enzalutamide intermediate F
CN104803918A (en) * 2014-01-26 2015-07-29 上海医药工业研究院 Preparation method of enzalutamide
US20150210649A1 (en) * 2014-01-27 2015-07-30 Cadila Healthcare Limited Process for preparation of androgen receptor antagonist
WO2015154730A1 (en) * 2014-04-07 2015-10-15 Zentiva, K.S. A process for producing enzalutamide

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015063720A1 (en) * 2013-10-31 2015-05-07 Ranbaxy Laboratories Limited Process for the preparation of enzalutamide
CN104803919A (en) * 2014-01-26 2015-07-29 上海医药工业研究院 Preparation method of enzalutamide intermediate F
CN104803918A (en) * 2014-01-26 2015-07-29 上海医药工业研究院 Preparation method of enzalutamide
US20150210649A1 (en) * 2014-01-27 2015-07-30 Cadila Healthcare Limited Process for preparation of androgen receptor antagonist
WO2015154730A1 (en) * 2014-04-07 2015-10-15 Zentiva, K.S. A process for producing enzalutamide

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
DATABASE CAPLUS [o] 2017, retrieved from STN Database accession no. 2015:1228940 *
DATABASE CAPLUS [o] 2017, retrieved from STN Database accession no. 2015:1228951 *
LI, JIANQI ET AL.: "Process for the preparation of enzalutamide", FAMING ZHUANLI SHENQING , CODEN: CNXXEV *
LI, JIANQI ET AL.: "Process for the preparation of intermediate of enzalutamide", FAMING ZHUANLI SHENQING , CODEN: CNXXEV *

Also Published As

Publication number Publication date
WO2017081702A2 (en) 2017-05-18

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