CAJ | 학술논문

描述了以乙腈为溶剂,在亚磷酸三乙酯和三乙胺存在下,使MICA和DM进行反应, 合成第三代头孢菌素类抗生素头孢克肟(cefixime)、卡芦莫南(Carumonam)关键中间体,( Z )-2-(2-氨基噻唑-4-基)-2-甲氧羰基甲氧亚氨基硫代乙酸(S-2-苯并噻唑)酯的方法.最高收率为60.5%,最佳原料摩尔比为1∶1.2∶1.2∶1.2.所得目标化合物经过与样品化合物红外光谱数据、核磁共振光谱数据比对得到确认.
묘술료이을정위용제,재아린산삼을지화삼을알존재하,사MICA화DM진행반응, 합성제삼대두포균소류항생소두포극우(cefixime)、잡호막남(Carumonam)관건중간체,( Z )-2-(2-안기새서-4-기)-2-갑양탄기갑양아안기류대을산(S-2-분병새서)지적방법.최고수솔위60.5%,최가원료마이비위1∶1.2∶1.2∶1.2.소득목표화합물경과여양품화합물홍외광보수거、핵자공진광보수거비대득도학인.
S-2-Benzothiazolyl (Z) -2-(2-Aminothiazol-4-yl)-2-methoxycarbonyl methoxy imino thioacetate (MICA activated thioester),a key intermediate for Cefixime and Carumonam,is synthesized by the esterification reaction of (Z)-2-(methoxycar-bonyl methoxyimino)-2- (2-Aminothiazol-4-yl) acetic acid (1) with dibenzothiazolyl disulfide (2) in acetonitrile in presence of P (OEt)_3 instead of Ph_3 P and Et_3N with 60.5% yield.The best molar ratio of (1),(2),(P(OEt)_3) and Et_3N is 1: 1.2 :1.2 1.2.The structure of the target compound is confirmed by the its IR and 1HNMR data with that of the standard sample.