CAS: 90356-78-8; N-(4-Cyano-3-(Trifluoromethyl)Phenyl)-3-((4-Fluorophenyl)Thio)-2-Hydroxy-2-Methylpropanamide

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CAS号371-42-6 4-氟苯硫酚 | CAS号90357-51-0 2-羟基-2-甲基-N-[4-... | CAS号339530-91-5 3-(4-氟苯巯基)-2-羟基... | CAS号654-70-6 4-氨基-2-三氟甲基苯甲腈 | CAS号3887-61-4 sodium salt of ... | CAS号7440-44-0 活性炭 | CAS号90357-53-2 N-(4-氰基-3-三氟甲基苯... | CAS号873014-32-5 N-[4-cyano-3-(t... | CAS号194853-86-6 4-氟-2-三氟甲基苯甲腈 | CAS号90357-06-5 比卡鲁胺 | CAS号945419-64-7 比卡鲁胺砜

4-Amino-2-Iodobenzonitrile置于双氧水,四丁基碘化铵,Sodium Hydride,Potassium Carbonate体系中,用 二氯甲烷,N,N-二甲基甲酰胺,丙酮,Mineral Oil 作为反应溶剂,化学反应 5.5H,反应生成 N-[4-氰基-3-(三氟甲基)苯基]-3-[(4-氟苯基)硫基]-2-羟基-2-甲基丙酰胺
参考文献:Chemical Degradation Of Androgen Receptor (Ar) Using Bicalutamide Analog-thalidomide Protacs
标题:Chemical Degradation Of Androgen Receptor (Ar) Using Bicalutamide Analog-thalidomide Protacs
摘要:一系列由比卡鲁胺类似物和沙利度胺组成的protacs(proteolysis-Targeting Chimeras)被设计,合成并在生物学上评估,作为新型雄激素受体(ar)降解剂.特别地,我们发现protac化合物13B能够成功地在ar阳性癌细胞中展示对ar的有针对性降解,并可能是一种用于研究ar依赖性癌细胞的有用化学探针,同时也是前列腺癌的潜在治疗候选药物.
DOI:10.3390/molecules26092525

专利信息

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: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-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:EP-1383735-A4
优先权日:2001-05-02
标题 :PROCESSES FOR THE SYNTHESIS OF ACYLANILIDES COMPRISING BICALUTAMIDE AND DERIVATIVES THEREOF

专利号:EP-1614677-A2
优先权日:2004-06-17
标 题:Improved procedure for the synthesis of bicalutamide

专利号:US-2006041161-A1
优先权日:2004-06-17
标 题:Procedure for the synthesis of bicalutamide