精氨酰甘氨酰天门冬氨酸三肽的合成

Synthesis of Tripeptide-RGD

以L-精氨酸、L-甘氨酸、L-天门氨酸为原料,采用二环己基碳二亚胺(DCC)法合成了Arg-Gly-Asp(RGD)。Z-Arg(NO2)-OH经偶联剂活化与H-Gly-OMe.HCl缩合,水解后得到Z-Arg(NO2)-Gly-OH;产物与H-Asp(OBzl)-OBzl.TosOH偶联得到全保护多肽,经Pd-C/H2还原为Arg-Gly-Asp。

Takintg L-Arginine, L-Glycine and L-Aspartate as a raw material, used DCC couplingmethod to synthesize Arg-Gly-Asp （RGD）. Activating by coupling reagent, Z-Arg（NO2）-OH wascoupled with H-Gly-OMe· HCl, after the hydrolysis Z-Arg（NO2）-Gly-OH was obtained; and then itwas reacted with H-Asp（OBzl）-OBzl·TosOH to get complete protected tripeptide, at last using Pd-C/H2 as reducing reagent, the final product Arg-Gly-Asp was obtained.