一种手性β-氨基膦酸酯的合成方法研究  

Study on the synthesis of a chiral β-amino phosphonate

作　　者：张鹏 杨丽娟 钏永明 李宏利 ZHANG Peng;YANG Li-juan;CHUAN Yong-ming;LI Hong-li(School of Chemistry&Environment,Yunnan Minzu University,Kunming 650500,Yunnan,China)

机构地区：[1]云南民族大学化学与环境学院,云南昆明650500

出　　处：《云南大学学报（自然科学版）》2023年第5期1099-1104,共6页Journal of Yunnan University(Natural Sciences Edition)

基　　金：云南民族大学化学博士点培育青年项目(BSD-HX-2022-01);云南省万人计划—青年拔尖人才计划(YNWR-QNBJ-2019-094).

摘　　要：合成了4种金鸡纳碱衍生的手性相转移催化剂,用于催化(2-氧代丙基)膦酸二甲酯与α-氨基砜的不对称Mannich反应制备β-氨基膦酸酯.经过反应条件的优化,确定了-40℃,以化合物D为催化剂,甲苯为溶剂,6%LiOH水溶剂为碱的最佳反应条件,手性β-氨基膦酸酯衍生物的收率达到90%,ee值达到60%.Four cinchona-derived chiral phase transfer catalysts were synthesized to catalytic asymmetric Mannich reaction of dimethyl(2-oxopropyl)phosphonate with α-aminosulfones to prepare β-aminophosphonates.After the optimization of the reaction conditions,the optimal reaction conditions were determined at-40℃,using compound D as the catalyst,toluene as the solvent,and 6%LiOH water solvent as the base,and the yield of chiral β-aminophosphonate derivatives reached 90%,the ee reached 60%.

关 键 词：相转移催化 手性β-氨基膦酸酯衍生物 MANNICH反应 

分 类 号：O621.3[理学—有机化学]