L-高丝氨酸内酯盐酸盐的氨基保护

L-高丝氨酸内酯盐酸盐的氨基保护 Amino Protection of L-Homoserine Lactone Hydrochloride 滕汉兵 TENG Hanbing 1 first-author 黄进 HUANG Jin 1 武汉理工大学化学工程学院 武汉理工大学化学工程学院 College of Chemical Engineering,Wuhan University of Technology College of Chemical Engineering,Wuhan University of Technology 以氯甲酸苄酯（CbzCl）为氨基保护试剂,研究了它对L-高丝氨酸内酯盐酸盐的氨基保护.实验表明,以水为溶剂,NaHCO3为碱的无机反应体系,制备N-Cbz-L-高丝氨酸内酯的产率可高达93%,显著优于以CH2Cl2为溶剂,Et3N或吡啶（Py）为碱的有机反应体系.以氯甲酸乙酯（EocCl）和氯甲酸甲酯（MocCl）为氨基保护试剂时,无机反应体系也明显优于有机反应体系.同时发现,氯甲酸甲酯为保护试剂,NaHCO3为碱时,组合溶剂（THF/H2O或丙酮/H2O）形成的均相溶剂体系可获得比仅使用水作溶剂时更高的产率. The N-protection of L-Homoserine lactone hydrochloride has been researched with benzyl chloroformate （CbzCl） as amino protecting agent. The yield reached 93% when the solvent was H2O and the base was NaHCO3. This inorganic reaction system excels the organic reaction system remarkably which the solvent is CH2Cl2 and the base is Et3N or pyridine. The result shows that the inorganic reaction system is also better than the organic reaction system when the amino protecting agent is ethyl chloroformate （EocCl） or methyl chloroformate （MocCl）. However for MocCl,if the base is NaHCO3,the yield is higher using homogeneous solvent system such as THF/H2O or acetone/H2O than only using H2O as solvent. 氨基保护 N-Cbz-L-高丝氨酸内酯 L-高丝氨酸内酯盐酸盐 amino protection N-Cbz-L-homoserine lactone L-homoserine lactone hydrochloride 10.14188/j.1671-8836.2010.01.007 O626 国家“211”工程专项经费资助项目（38650219） 2010-01-01 2021-04-01 1 56