Hemmasi B, Stüber W, Bayer E
Hoppe Seylers Z Physiol Chem. 1982 Jul;363(7):701-8. doi: 10.1515/bchm2.1982.363.2.701.
The syntheses of 4-(Boc-aminoacyloxymethyl)-3-nitrobenzoic acids are described. These compounds are suitable reagents for coupling to polyethylene glycol or its derivatives by the dicyclohexylcarbodiimide method to obtain 4-(Boc-aminoacyloxymethyl)-3-nitrobenzoyl-polyethylene glycol support. This is demonstrated by the reaction of the 4-carboxy-2-nitrobenzyl ester of Boc-alanine with glycylpolyethylene glycol in excellent yield. This synthetic route produces a much better coupling yield and an easier purification procedure in comparison with the original method in which Boc-amino acid cesium salts are allowed to react with 4-(bromomethyl)-3-nitrobenzoyl-polyethylene glycol.
描述了4-(Boc-氨基酰氧基甲基)-3-硝基苯甲酸的合成方法。这些化合物是通过二环己基碳二亚胺法与聚乙二醇或其衍生物偶联以获得4-(Boc-氨基酰氧基甲基)-3-硝基苯甲酰基聚乙二醇载体的合适试剂。Boc-丙氨酸的4-羧基-2-硝基苄酯与甘氨酰聚乙二醇的反应以优异的产率证明了这一点。与使Boc-氨基酸铯盐与4-(溴甲基)-3-硝基苯甲酰基聚乙二醇反应的原始方法相比，该合成路线产生了更好的偶联产率和更简便的纯化程序。
