氨基酸酰胺类化合物的简便合成

A simple way to prepare amino acid amide compounds

报道一种氨基酸酰胺类化合物的简便合成方法。以带芴甲氧羰基(Fmoc)保护基团的氨基酸为原料,经过酰氯化后,选择可以溶解酰氯但不溶解酰胺的溶剂溶解,然后直接与简单胺类反应沉淀出产物,得到高产率的氨基酸酰胺类化合物。产物结构经元素分析、1H-NMR、13C-NMR、IR等手段证实。

A simple and effective way to prepare amino acid amide compounds is pat forward. By this method amino acid amide compounds are directly prepared in suitable solvent at high yields by the reaction between simple amine and Fmoc-amino acid chloride, which is initially synthesized from Fmoc-amino acid and acid chloride reagents. The solvent employed must be a good solvent for Fmoc-amino acid chloride but not for Fmoc-amino acid amide,by this the product can be quickly precipitated out and de-protection of Fmoc and other by-reaction can be avoided. The structures of the products are confirmed by ^1H-NMR, ^13C-NMR, IR spectra and elemental analysis as well.