摘要
对头孢布烯的关键中间体2-(2-苄氧羰基氨基噻唑-4-基)-5-(3-甲基-2-丁烯氧羰基)-2-戊烯酸(1)的合成工艺进行了研究。选用国内易得的(2-氨基噻唑-4-基)乙酸甲酯(2)作为起始原料,经过氨基保护、M ichae l加成-消除和选择性酯化三步反应制得目标化合物1,反应总收率63.0%。该工艺操作简单,生产成本低,适合工业化生产。
2-（2-Benzyloxycarbonylaminothiazol-4-yl）-5-（3-methyl-2-butenyloxycarbonyl） pent-2-enoic acid （1）, the key intermediate of ceftibuten, was prepared from methyl （2-aminothiazol-4-yl）acetate which could be easily bought in China through a three-step reaction of amino group protection, Michael additionelimination and selective esterification with an overall yield of 63.0%. This facile and lower-cost process was suitable for industrial production.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2007年第10期604-607,635,共5页
Chinese Journal of Antibiotics
