化学法合成RGD三肽的研究

Study on the synthesis of RGD tri-peptide by the chemical method

采用二环己基碳二亚胺法(DCC)合成了二肽Gly Asp(OBzl) 2 ,然后利用混合酸酐法得到全保护RGD三肽:Boc Arg(NO2 ) Gly Asp(OBzl) 2 三肽;最后在Pd/C的催化加氢下,将保护基一起脱掉而得到RGD三肽的粗品。具体研究了合成二肽及三肽的主要影响因素及其优化条件。在优化条件下,获得三肽的结晶干品,总得率为5 7 2 %。

Gly-Asp（ OBzl）2 dipeptide was synthesized by DCC method, then Boc-Arg（ NO2 ）-Gly-Asp （OBzl）2 was synthesized by the method of mixed anhydrides. De-protected RGD tri-peptide was obtained by hydrogenating with Pd/C catalyst under a mild condition. The influencing factors of several condensation reactions and optimum conditions in RGD synthesis were respectively investigated. Under the optimum conditions, the total yield of RGD crystal was 57.2 %.