90356-78-8

基本信息
N-[4-氰基-3-(三氟甲基)苯基]-3-[(4-氟苯基)硫基]-2-羥基-2-甲基丙酰胺
N-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-3-[(4-FLUOROPHENYL)THIO]-2-HYDROXY-2-METHYL PROPANAMIDE
N-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-3-[(4-FLUOROPHENYL)THIO]-2-HYDROXY-2-METHYLPROPIONAMIDE
(S)-N-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-3-(4-FLUOROPHENYLTHIO)-2-HYDROXY-2-METHYLPROPANAMIDE
Bicalutamide Intermediate
BICALUTAMIDE-SULFIDE (BICALUTAMIDE ASH)
N-[4-Cyano-3-(Trifluoromethyl)Phenyl]-3-[(4-Fluorophenyl)thio]-2-Hydroxy-2-Methy
N-[4-CYANO-3-(TRIFLUOROMETHYL)PHENYL]-3-[(4-FLUOROPHENYL)THIO] -2- HYDROXY-2-MET
4-OYANO-3-TRIFLUOROMETHYL-N-[3-(4-FLUOROPHENYLTHIO)-2-HYDROXYL-2-METHYLPROPIONYL]ANILINE
H-(4-CYANO-3-TRIFLUOROMTHYLPHENYL)-3-(4-FLOUROPHENYLSULFANYL)-2-HYDROXY-2-METHYLPROPIONAMIDE
4-Cyano-3-(trifluoromethyl)phenyl-3-(4-fluorophenyl)thio)-2-methylpropanamide
N-[4-Cyano-3-(trifluoromethyl)
4-cyano-3-trifluoromethyl-N-[3-(4-fluorophenylthio)-2-hydroxyl-2-methylpropionyl]aniline (intermediate of bicalutamide)
INTERMEDIATE OF BICALUTAMIDE
物理化學(xué)性質(zhì)
制備方法

371-42-6
![N-[4-氰基-3-(三氟甲基)苯基]甲基環(huán)氧丙烯酰胺](/CAS/GIF/90357-51-0.gif)
90357-51-0
![N-[4-氰基-3-(三氟甲基)苯基]-3-(4-氟苯巰基)-2-羥基-2-甲基丙酰胺](/CAS/GIF/90356-78-8.gif)
90356-78-8
實施例1 N-[4-氰基-3-(三氟甲基)苯基]-3-[(4-氟苯基)硫代]-2-羥基-2-甲基丙酰胺的制備:將4-氟苯硫酚(21g)溶于甲醇(65ml)中,冷卻至0℃。在攪拌下分批加入50%氫氧化鈉水溶液(14g)。反應(yīng)混合物在0℃下攪拌30分鐘,隨后在25℃下繼續(xù)攪拌1小時。向反應(yīng)體系中加入N-[4-氰基-3-(三氟甲基)苯基]-2-甲基環(huán)氧乙烷酰胺(40g),室溫下攪拌反應(yīng)2小時。通過薄層色譜(TLC)監(jiān)測反應(yīng)進(jìn)度。反應(yīng)完成后,向混合物中加入水(100ml),并用濃鹽酸調(diào)節(jié)pH至7以下。在減壓下蒸餾除去甲醇,直至無甲醇餾出。將所得懸浮液在5℃下攪拌3小時,過濾收集固體產(chǎn)物,并用水(2×40ml)洗滌。最后,將固體在50-60℃下真空干燥,得到目標(biāo)產(chǎn)物N-[4-氰基-3-(三氟甲基)苯基]-3-[(4-氟苯基)硫代]-2-羥基-2-甲基丙酰胺58g,收率98%。
參考文獻(xiàn):
[1] Patent: US2007/27211, 2007, A1. Location in patent: Page/Page column 2; 4
[2] Patent: US2003/191337, 2003, A1. Location in patent: Page/Page column 5; 11
[3] Patent: US2013/274501, 2013, A1. Location in patent: Paragraph 0107; 0108; 0109
[4] Patent: US2003/191337, 2003, A1. Location in patent: Page/Page column 5; 11
[5] Patent: US2003/191337, 2003, A1. Location in patent: Page/Page column 12; 13