5-氧代-1,2,4-噁二唑化合物的合成工艺改进  

Improved Synthesis of 5-Oxo-1,2,4-oxadiazole Compounds

作　　者：王建国[1] 陈志龙[1] 李玥[1] 王莉清[1] 

机构地区：[1]第二军医大学海医系毒物药物研究室,上海200433

出　　处：《中国医药工业杂志》2004年第11期646-647,共2页Chinese Journal of Pharmaceuticals

摘　　要：氰基化合物在盐酸羟胺和三乙胺作用下于85～90℃反应20～24h得到N-羟基脒化合物,收率由文献的26%～68%提高到90%以上。再与氯甲酸异丁酯反应后脱醇环合即可得到5-氧代-1,2,4-噁二唑化合物。以TAK-536甲酯为例总收率可达49%。Oxo-1,2,4-oxadiazole group was synthesized from cyano compound by reaction with NH2OH·HCland Et3N for 20～24h at 85～90℃ to give 90% yield of N-hydroxyamidino compound, which subjected to reaction withisobutyl chloroformate and followed by cyclization to afford TAK-536 methyl ester in an overall yield of 49%.

关 键 词：5-氧代-1 2 4-噁二唑 中间体 合成 

分 类 号：O626.2[理学—有机化学]