改进的“一锅煮”法合成3-氨基-3-芳基丙酸

Improved one-pot synthesis of 3-amino-3-arylpropionic acids

目的 :改进 3 氨基 3 芳基丙酸的合成方法 ,提高化学产率 .方法 :以甲醇为反应溶剂 ,芳香醛和 3当量醋酸铵反应生成希夫碱 ,再加入丙二酸 ,反应混合物剧烈回流 1 6h得目标产物 .将产物用核磁共振仪进行光谱学鉴定 .结果 :合成出 1 0种 3 氨基 3 芳基丙酸 ,其中 5种为新的β 氨基酸 ,产率为 2 5 %～ 79% ,比文献报道产率提高约 1 0 % .结论 :该合成法简单、易行 ,降低了反应成本 。

AIM: To improve the synthetic method of 3 Amino 3 arylpropionic acid and obtain high yield. METHODS: Aromatic aldehyde and 3 equivalents of ammonium acetate were refluxed in methanol for 10 min to form Shiff base. Malonic acid was added and reaction mixture refluxed intensely for 16 h. The product was obtained and then characterized by NMR spectrum. RESULTS: Ten 3 Amino 3 arylpropionic acids were prepared, of which 5 kinds wee new. The yields were 25%～79%, which were respectively higher than the values reported by literature. CONCLUSION: Our improved method, simple and easy, reduces the cost, and is of high value for industrial appliation.