Pazulfloxacin was synthesized by condensation of ethyl (S)-9,0-difluoro- -methyl-7-oxo-, -dihydro-pyrido[,, -de][,] benzoxazine--carboxylate with ethyl cyanoacetate, decarboxylation, cyclization, hydrolysis and Hoffman reaction in an overall yield of %.
Pazulfloxacin was synthesized by condensation of ethyl (S)-9,0-difluoro- -methyl-7-oxo-, -dihydro-pyrido[,, -de][,] benzoxazine--carboxylate with ethyl cyanoacetate, decarboxylation, cyclization, hydrolysis and Hoffman reaction in an overall yield of %.
以左氟沙星中间体 (S) - 9,0 -二氟 - -甲基 - 7-氧代 - , -二氢 - 7H-吡啶 [, , - de][,]苯并嗪 - -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 %。