以乙醛酸一水合物为起始原料通过芳环上的胺烷基化反应合成了3种苯环上带有易离去官能团的保护苯甘氨酸衍生物:N-苯甲酰基-4-溴苯甘氨酸甲酯、N-苄氧酰基-4-对甲苯磺酰氧基苯甘氨酸苄酯和N-苄氧酰基-4-三氟甲磺酰氧基苯甘氨酸苄酯,合成的3种化合物的总收率分别为39.3%、67.4%和66.7%。产物结构采用IR,1H NMR和13C NMR进行了鉴定。
Three protected phenylglycine derivatives with easy leaving groups, methyl 4- bromo-N-benzoylphenylglycinate, benzyl N-benzyloxycarbonyl-4-( p-toluenesulfonyloxy) phenylglycinate and benzyl N-benzyloxycarbonyl-4-trifluoromethanesulfonyloxy- phenylglycinate, were synthesized by amidoalkylation of aromatic compounds using glyoxylic acid monohydrate as starting material. Effects of some factors on reaction yield were discussed. The yields of compounds were 39.3%, 67.4% and 66.7% ,respectively. The structures of the products were identified by IR, 1H NMR and 13C NMR.