以(S)-4-(4-氨基苄基)噁唑烷-2-酮为起始原料,经重氮化、还原制得(S)-4-(4-肼基苄基)噁唑烷-2-酮。再和4,4-二乙氧基-N,N-二甲基丁胺缩合后经回流环合制得选择性5-HT1B/1D激动剂佐米曲坦。通过比较不同的环合条件,确定在pH3～4、回流温度下、反应5h的条件下环合效果较好,总收率达45.3%。改进后的工艺操作简便易行。 Starting from (S) -4- (4-aminobenzyl) oxazolidin-2-one, diazotization and reduction of (S) -4- (4-hydrazinobenzyl) 2-one. And then 4, 4-diethoxy-N, N-dimethyl butylamine condensed by reflux cyclization prepared a selective 5-HT1B / 1D agonist Zolmitriptan. By comparing different cyclization conditions, it was confirmed that the cyclization was better under the conditions of pH3 ~ 4, reflux temperature and reaction for 5h, and the total yield was 45.3%. The improved process operation is simple and easy.