Boc-苯丙氨酸叔丁酯选择性脱保护工艺研究

Study on Selective Deprotection Process of Boc-Phenylalanine Tert-Butyl Ester

被保护的氨基酸化合物作为药物分子中间体和功能材料中间体得到广泛使用。Boc保护的氨基酸酯类化合物在脱除Boc保护时的高效性,可为其在整条工艺中的后续转化提供重要的先决条件。以Boc-苯丙氨酸叔丁酯为原料,对其选择性脱除Boc保护基而保留叔丁酯保护基生成苯丙氨酸叔丁酯盐酸盐的工艺进行了研究。结果表明,在室温或低温条件下,采用酸性条件脱保护的方式,收率可达到82%左右;反应条件简单、温和,工艺设备成本低廉,此工艺具有操作简单、经济实惠和绿色环保的特点。

Protected amino acid compounds are often widely used as intermediates of drug molecules and functional material intermediates.The high efficiency of Boc-protected amino acid esters provides an important prerequisite for their subsequent conversion in the entire process.Boc-tert-butyl phenylalanine was selected as the raw material,and the process of selectively removing the Boc protecting group while retaining the protecting group of tert-butyl ester to generate tert-butyl phenylalanine hydrochloride was studied.Under room temperature or low temperature conditions,the yield of about 82%can be achieved by deprotection under acidic conditions,and the reaction conditions are simple and mild,and the cost of process equipment is low,which realizes simple operation,economical benefits and environmental protection.