氨基二元酸的Boc化研究

Study on the preparation of Boc-protected acidic amino acids

提出了制备Boc 氨基二元酸的适用溶剂系统 :亚氨基二乙酸和天冬氨酸在碱性 1 ,4 二氧六环 水溶剂系统中与(Boc) 2 O反应及谷氨酸在碱性 1 ,4 二氧六环和四氢呋喃 水溶剂系统中与 (Boc) 2 O反应的收率均明显高于以叔丁醇 水为溶剂系统的反应收率。

Improved solvent systems for the preparation of Boc protected acidic amino acids were tested.Iminodiacetic acid and aspartic acid reacting with t-butyloxycarbonyl anhydride in the basic solvent system of 1,4-dioxane-water gave better yields than those from conventional t-BuOH/H 2O system method,while glutamic acid in both solvent systems of 1,4-dioxane-water and tetrahydrofuran-water also gave better yield.