摘要
替比培南侧链是合成目前世界上唯一的口服型碳青霉烯类抗生素替比培南酯的关键中间体。以苄胺和和环氧氯丙烷为起始原料,经开环、分子内环合、甲磺酰化、催化氢化、缩合、S_N2取代、碱性水解和酸化等8步反应合成了替比培南侧链,工艺总收率52.6%,其结构得到~1H-NMR和IR确认。该方法原料廉价易得、反应条件温和、操作简单、收率高、成本低,适合工业化生产。
Tebipenem pivoxil is the only oral carbapenem antibiotic in the world. The key intermidiate of tebipenem pivoxil,tebipenem side chain,was synthesized from benzylamine and epichlorohydrin by ring opening,cyclization,mesylation,catalytic hydrogenation,condensation,S_N2 substitution,hydrolysis and acidification. The overall yield was56%. The structure was confirmed by ~1H-NMR and IR. The method has merits of cheap raw materials,mild conditions,simple operation,high yield,low cost and suitability for industrialization.
出处
《广州化工》
CAS
2018年第1期60-61,共2页
GuangZhou Chemical Industry
