摘要
以左氧氟沙星中间体(S)-9,10-二氟-3-甲基-7-氧代-2,3-二氢-7-H吡啶[1,2,3-de][1,4]苯并噁嗪-6-羧酸乙酯为起始原料,经与氰乙酸乙酯进行亲核取代反应、水解脱羧、环合、水解、Hoffman降解,与甲磺酸成盐得甲磺酸帕珠沙星,总收率为38%,产品纯度符合药用标准。
Pazufloxacin mesilate was synthesized from (S)-9,10-difluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylate by nucleophilic substitution,hydrolysis and decarboxylation, cyclic addition ,hydrolysis,Hofmann degradation and salt formation.The overall yield was 38%.
出处
《安徽化工》
CAS
2006年第4期30-31,共2页
Anhui Chemical Industry
关键词
喹诺酮类抗菌药
帕珠沙星
合成
Fluoroquinolone antibacterial agent
Pazufloxacin mesilate
synthesis
