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目的以硅胶作为催化剂,高效合成Naftopidil(Naf)及其光学异构体。方法在室温氮气保护和无溶剂条件下,使用60～100目硅胶催化萘氧基缩水甘油醚与邻甲氧基苯基哌嗪进行反应,得到Naf及其光学异构体。通过筛选催化剂的用量及循环使用次数优化反应。结果用20%的硅胶催化得到Naf,最佳收率为87%;硅胶循环5次,催化活性未见明显降低;对光学异构体的Naf的最佳收率为77%,ee值最高达98.2%。结论所用方法反应条件温和、收率高、产物与催化剂容易分离、催化剂可循环使用、活性未见明显降低,基本符合绿色化学反应的要求,具有良好的工业应用前景。
Objective To synthesize Naftopidil (Naf) and its optical isomers efficiently using silica gel as a catalyst. Methods The Naf and its optical isomers were obtained by reaction of naphthyloxy glycidyl ether and o-methoxyphenylpiperazine with 60-100 mesh silica gel under nitrogen atmosphere and without solvent at room temperature. The reaction was optimized by screening the amount of catalyst and the number of cycles. Results Naf was obtained with 20% silica gel and the best yield was 87%. The silica gel was recycled 5 times without any significant decrease in the catalytic activity. The optimum yield of Naf for optical isomers was 77% 98.2%. Conclusion The reaction conditions are mild, the yield is high, the product and catalyst are easily separated, the catalyst can be reused, the activity is not obviously reduced, basically meet the requirements of green chemical reaction, and have good industrial application prospects.