5-HT_3受体拮抗剂阿扎西隆的合成

Synthesis of the 5-HT_3 Receptor Antagonist Azasetron

以水杨酸甲酯为起始原料 ,经氯代、硝化等 8步反应合成 5 HT3 受体拮抗剂阿扎西隆 ,以化合物 (2 )计总收率为 45 % (文献〔6〕收率为 34 % ) ,其结构经IR ,1H

The 5 HT 3 receptor antagonist azasetron was synthesized from methyl salicylate through an eight step synthetic route with chlorination,nitration,etc.The total yield was 45%(calculated on 2).The yield reported in literature 〔6〕 was 34%.It was characterized by IR, 1H NMR and MS.