【摘要】 头孢他啶侧链酸在碱性条件下与DM缩合生成头孢他啶侧链酸活性硫酯时,用价格低廉的亚磷酸三乙酯代替价格昂贵的三苯基膦,通过设计正交实验优选出的较佳反应条件为:固定头孢他啶侧链酸19.8 g,反应物料n(头孢他啶侧链酸)∶n(DM)∶n(亚磷酸三乙酯)∶n(三乙胺)=1∶1.2∶1.2∶1.2,反应溶剂乙腈150 mL,于5℃反应5 h,收率86.8%.更多还原

【Abstract】 The condensate(Z)-2-(2-aminothiazol-4-yl)2-(tert.-butyoxycarbonylprop-2-oxyimino) acetic acid forms 2-(2-amino-4-thiazolyl)-(Z)-2-[(1-tert-butoxycarbonyl-1-methyl-ethoxy)-imino]with DM,in alkali conditions,acetic acid benzothiazolyl thioester,by triethyl phosphate instead of the expensive triphenylphosphine.The optimum conditions were studied through the orthogonal experiment:(Z)2-(2-aminothiazol-4-yl)-2-(tert.-butyoxycarbonylprop-2-oxyimino)acetic acid 19.8 g,n((Z)-2-(2-aminothiazol-4-yl)-2-(tert.-butyoxycarbonylprop-2-oxyimino)aceticacid)∶n(DM)∶n(triethyl phosphite)∶n(triethylamine)=1∶1.2∶1.2∶1.2,with reaction solvent acetonitrile of 150 ml;reaction temperature of 5 ℃ and reaction time of 5 h.The yield of product is up to 86.8%.更多还原