比卡鲁胺的合成

Synthesis of Bicalutamide

以环氧化合物1,2-环氧-2-甲基-N-[4-氰基-3-(三氟甲基)苯基]丙酰胺为起始原料,经缩合、氧化两步反应制得非甾体类抗雄激素药物比卡鲁胺。对中间体的合成工艺进行了改进。以二甲基甲酰胺为溶剂、四丁基溴化铵为相转移催化剂、碳酸钾为缚酸剂,使反应无需控制水分,并可在温和条件下进行,反应收率由文献的67.8%提高到88.9%。

A nonsteroidal antiandrogen drug,bicalutamide,was synthesized starting from N-[4-cyano3-（trifluoromethyl）phenyl]-1,2-epoxy-2-methylpropionamide via two steps of condensation and oxidation.The synthetic process of the intermediate was improved.The condensation reaction needed not control moisture,and could take place under a mild condition by using DMF as solvents,TBAB as a phase transfer catalyst,and K2CO3 as an acid binding agent.The yield was up to 88.9% from 67.8%.