含丝氨酸残基手性肽核酸单体的合成

Synthesis of Chiral PNA Monomer Containing Serine Residue

对文献合成方法进行了改进.以N-Boc氨基酸与自制甲烷磺酸酯反应,制备N-Boc氨基酸丙烯酯,以混合酸酐法实现关键中间体与1-胸腺嘧啶乙酸的缩合,总收率为26.4%,比文献方法提高了12%,成本降低,制备了含丝氨酸残基碱基为胸腺嘧啶的手性肽核酸单体.

The allyl ester of N-Boc protected serine has been synthesized from allyl methanesulfonate prepared ourself and the condensation of key intermediate and thymin-1-yl-acetic acid have been sucessufully achieved in mixed anhyride in stead of the classic DCC method. Chiral PNA monomer containing serine residue and thymine has been prepared in total yield 26.4%, which is 12% higher than that of the literature method reported, and with low consumption.