比卡鲁胺的合成

Synthesis of Bicalutamide

以 2 -甲基丙烯酸甲酯为起始原料 ,经氧化、与 4-氟苯硫酚缩合、水解成α-羟基酸 ( )、 再与 2 -三氟甲基-4-氨基苯腈在亚硫酰氯作用下缩合、最后经间氯过氧化苯甲酸氧化而合成比卡鲁胺。总收率为 1 1 .2 %。

Bicalutamide was synthesized from methyl methacrylate via oxidation, condensation with 4 fluorothiophenol and hydrolysis to give α hydroxy acid which was first reacted with 2 trifluoromethyl 4 aminobenzonitrile and then oxidized with m chloroperoxybenzoic acid. The overall yield was about 11.2%.