合成β-(3,4-二氨基苯基)-α-氨基丙酸二盐酸盐的新路线

A New Synthetic Route for β-(3,4-Diaminophenyl)-Alanine Dihydrochloride

β-(3,4-二氨基苯基)-α-氨基丙酸二盐酸盐是合成药物的一个重要中间体。从文献中只见到苏联列宁格勒药物研究所等人^([1])在1966年报导的合成方法:以5-甲基苯并[2,1,3]硒二氮杂茂为原料依次与NBS、NaC(NHCOCH_(3))(COOC_(2)H_(5))_(2)、H_(2)S/NH_(4)OH及HCl,H_(2)O作用而制得。其中5-甲基苯并[2,1,3]硒二氮杂茂的制备需4—5步。该方法的路线较长,原料不易得到。

A new synthetic route for β-(3,4-diaminophenyl)-alaninc dihydrochloride by using P-nitrobenzaldehydc and N-benzoylglycine as starting substrates is reported. Some of the intermediates in this route are new compounds.Our method,compared with that of V.G.Pesin ct al.[1], has the advantages that the starting substrates are easily available, the reacting conditions are moderate and the operations are simple.