专利号:US-7199257-B1 优先权日:1999-06-10 标题 :Process for the synthesis of N-(4-cyano-3-trifluoromethylphenyl)-3-(4-fluorophenylsulfonyl)-2-hydroxy-2-methylpropionamide 发明人:SOEROES BELA; TUBA ZOLTAN; GALIK GYOERGY; BOR ADAM; DEMETER ADAM; TRISCHLER FERENC; HORVATH JANOS; BRLIK JANOS 权利人:RICHTER GEDEON VEGYESZET 摘要:A new process is disclosed for the synthesis of racemic or optically pure N-[4-cyano-3-trifluoro-methyl-phenyl]-3[4-fluorophenyl-sulfonyl]-2-hydroxy-2-methylpropionamide. The process includes the formation of several novel intermediates in the synthesis.
专利号:US-9174943-B2 优先权日:2010-02-24 标 题 :Processes for the synthesis of diarylthiohydantoin and diarylhydantoin compounds 发明人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT 权利人:JAIN RAJENDRA PARASMAL; ANGELAUD REMY; THOMPSON ANDREW; LAMBERSON CAROL; GREENFIELD SCOTT; MEDIVATION PROSTATE THERAPEUTICS INC 摘要:Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.
专利号:EP-1614677-B1 优先权日:2004-06-17 标 题 :Improved procedure for the synthesis of bicalutamide 发明人:PIZZATTI ENRICA; VIGANO' ENRICO; LUSSANA MASSIMILIANO; LANDONIO ERNESTO 权利人:COSMA S P A 摘要:The object of the invention is an improved procedure for the synthesis of bicalutamide, characterised in that the 2-hydroxy-2-methyl-3-(4-fluorophenylthio) propionic acid initially produced undergoes a step to acylate the hydroxyl group in position 2 to give an intermediate 2-acyloxy-2-methyl-3-(4-fluorophenylthio) propionic acid, which allows the formation of a successive N-[4-cyano-3-(trifluoromethyl)-phenyl-]-3-[4-fluorophenylthio]-2-acyloxy-2-methyl-propionamide intermediate.
专利号:US-10626091-B2 优先权日:2014-10-01 标 题 :Process for the preparation of enzalutamide 发明人:CHIVUKULA KAMESWAR RAO; KARUTURI VEERA VENKATESWARA RAO; BENDA SRINIVAS; ANKE RAMACHANDRA; GAJULA DHARMAPURI; MOTURU VENKATA RAMA KRISHNA MURTHY; INDUKURI VENKATA SUNIL KUMAR; GORANTLA SEETA RAMA ANJANEYULU; CHAVA SATYANARAYANA 权利人:LAURUS LABS LTD 摘要:The present invention relates to an improved process for the preparation of enzalutamide by conventional synthesis, which avoids utilization of microwave irradiation and noxious reagents. The present invention also relates to an improved process for preparation of 4-isothiocyanato-2-(trifluoromethyl) benzonitrile, which is an intermediate in the synthesis of Enzalutamide.
专利号:US-2008177109-A1 优先权日:2005-03-29 标 题:Novel Process for Preparation of Bicalutamide 发明人:TARUR VENKATASUBRAMANIAN RADHA; KADAM SURESH MAHADEV; JOSHI ANIL PURUSHOTTAM; GAVHANE SACHIN BABAN 权利人:USV LTD 摘要:The present invention discloses a process for the synthesis of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide (Form I). The invention discloses a reagent for oxidation of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)thio]-2-hydroxy-2-methyl propanamide to N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide. More particularly, the invention discloses a method of purification of N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulphonyl]-2-hydroxy-2-methyl propanamide in a mixture of methylethyl ketone and hexane giving form (I). This form (I) is useful as an active pharmaceutical and has antiandrogenic activity.
专利号:US-2017190670-A1 优先权日:2014-07-11 标题:Improved process for the preparation of enzalutamide 发明人:HIRPARA SANJAY; SHRAWAT VIMAL KUMAR; POTHURAJU RAJU; TRIPATHI CHANDRESH KUMAR; AKSHAYKANT CHATURVEDI 权利人:SHILPA MEDICARE LTD 摘要:The present application relates to an improved process for preparation of Enzalutamide (I). n n n n n n n n n n The present application also relates to an improved process for the preparation of substantially pure Enzalutamide (I) having purity of greater than 99.5%. n The present application also relates to a novel process for the preparation of Enzalutamide intermediate useful in the industrially viable synthesis of Enzalutamide.