5-(4-氯丁基)-1-环己基-1H-四氮唑为合成抗血小板聚集药物西洛他唑的重要中间体。以δ-环戊内酯和环己胺为原料,生成N-环己基-5-羟基戊酰胺,之后与PCl_5反应,以吡啶为相转移催化剂,中间体不分离,直接与叠氮化钠发生反应,生成目标产物,总收率76.7%。对反应条件进行了探索和优化。 5- (4-chlorobutyl) -1-cyclohexyl-1H-tetrazole is an important intermediate for the synthesis of anti-platelet aggregation drug cilostazol. Δ-cyclopentanolactone and cyclohexylamine as raw materials to generate N-cyclohexyl-5-hydroxy-pentanamide, followed by reaction with PCl_5 to pyridine as phase transfer catalyst, the intermediate does not separate directly with sodium azide occurred Reaction, generate the desired product, the total yield of 76.7%. The reaction conditions were explored and optimized.