精细与专用化学品
精細與專用化學品
정세여전용화학품
FINE AND SPECIALTY CHEMICALS
2011年
12期
36-38
,共3页
杜会茹%李丽娟%蒋翠岚%马东来
杜會茹%李麗娟%蔣翠嵐%馬東來
두회여%리려연%장취람%마동래
西洛他唑%5-(4-氯丁基)-1-环己基-1H-四氮唑%合成
西洛他唑%5-(4-氯丁基)-1-環己基-1H-四氮唑%閤成
서락타서%5-(4-록정기)-1-배기기-1H-사담서%합성
Cilostazol%5-（4-chlorobutyl）-l- cyclohexyl-1H-tetrazole%synthesis
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-氯丁基）-1-環己基-1H-四氮唑為閤成抗血小闆聚集藥物西洛他唑的重要中間體。以δ-環戊內酯和環己胺為原料,生成N-環己基-5-羥基戊酰胺,之後與PCl_5反應,以吡啶為相轉移催化劑,中間體不分離,直接與疊氮化鈉髮生反應,生成目標產物,總收率76.7%。對反應條件進行瞭探索和優化。
5-（4-록정기）-1-배기기-1H-사담서위합성항혈소판취집약물서락타서적중요중간체。이δ-배무내지화배기알위원료,생성N-배기기-5-간기무선알,지후여PCl_5반응,이필정위상전이최화제,중간체불분리,직접여첩담화납발생반응,생성목표산물,총수솔76.7%。대반응조건진행료탐색화우화。
5-（4-Chlorobutyl）-1-cyclohexyl-1H-tetrazole is a key intermediate compound for Cilostazol as blood platelet aggregation inhibitors.N-cyclohexy-5-hydroxy-pentanamide was obtained useing tetrahydro-2H-pyran -2-one and cyclohexylamine as starting materials,then PCl_5 was added and pyridine used as a phase transfer catalyst then react with NaN_3 directly to preparation the aimed compound.The total yield was 76.7%.The optimum reaction conditions were found in the experiment.
