α-取代的3-氨基丙烯酸酯的合成

Synthesis of α-substituted 3-amino acrylic acid derivatives

研究了3-氨基丙烯酸酯碳酰化制备α-取代的β-氨基酸脱氢衍生物的反应条件.实验以溶剂、碱、反应温度、反应时间和比例(底物/乙酰氯/吡啶)为反应参数对该反应的条件进行优化,发现当底物、乙酰氯、吡啶三者的比例为1∶2∶2至1∶4∶4,以环己烷作溶剂,以吡啶作碱,反应温度控制为0℃时,3-氨基丙烯酸酯的碳酰化反应得到较好的收率.

C-acylation of 3-amino acrylic acid derivatives to afford a-substituted β-dehydroamino acids. The best reaction condition was estabilished after optimizing the reaction conditions. A systematic study was carried out to evaluate parameters such as the solvent, base, temperature and the ratio of substrates/AcCl/Base. The most optimized reaction condition was afforded ： the ratio of substrates/ AcCl/Base is from 1：2：2 to 1：4： 4, cyclohexane as the reaction solvent, pyridine as the base, and the reaction temperature is 0 ℃.