左氟沙星的微波催化合成

Synthesis of Levofloxacin

以2,3,4,5-四氟苯甲酰乙酸乙酯为原料,在微波辐射下,经N,N-二甲基甲酰胺二甲缩醛缩合,S-(+)-2-氨基丙醇置换,环合和水解后再与N-甲基哌嗪缩合制得左氟沙星(1),总收率48.1%。1和中间体的结构经1H NMR和MS表征。

Levofloxacin（ 1 ） in total yield of 48.1% was synthesized from ethyl（ 2,3,4,5-tetrafluoro- benzoyl） acetate under microwave irradiation by N, N-dimethylformamide dimethylacetal condensation, S-（ ＋ ）-2-aminopropanol displacement, cyclization, hydrolysis, and finally N-methylpiperazine condensation. The structures of 1 and intermediates were determined by 1H NMR and MS.