帕珠沙星的合成研究

Synthesis of Pazufloxacin

以左氟沙星中间体 (S) - 9,10 -二氟 - 3-甲基 - 7-氧代 - 2 ,3-二氢 - 7H-吡啶 [1,2 ,3- de][1,4]苯并嗪 - 6 -羧酸乙酯为原料 ,经与氰乙酸乙酯缩合、脱羧、环合、水解及 Hoffm an降解制得帕珠沙星 ,总收率 43%。

Pazulfloxacin was synthesized by condensation of ethyl (S)-9,10-difluoro-3-methyl-7-oxo-2,3-dihydro-pyrido[1,2,3-de][1,4] benzoxazine-6-carboxylate with ethyl cyanoacetate, decarboxylation, cyclization, hydrolysis and Hoffman reaction in an overall yield of 43%.