摘要/Abstract

报道了一个通过β，γ-炔基α-亚胺酸酯的化学和对映选择性转移氢化反应来合成光学纯β，γ-炔基α-氨基酸酯的方法.该不对称还原反应所展示出的优秀的化学选择性是由手性磷酸作为催化剂以及苯并噻唑啉作为氢负供体实现的.反应展示出了良好的官能团兼容性，高对映选择性地合成了一系列光学活性的非天然氨基酸酯化合物.
关键词: β,γ-炔基α-氨基酸酯, 化学选择性, 对映选择性, 转移氢化, 苯并噻唑啉
An effective chemo- and enantioselective transfer hydrogenation of β,γ-alkynyl α-imino esters to prepare optically pure β,γ-alkynyl α-amino esters has been described. The excellent chemoselectivity was achieved by using chiral phosphoric acid catalyzed asymmetric reduction with benzothiazoline as hydride donor. The reaction exhibited good functional group tolerance, providing a range of optically active non-natural amino esters with excellent enantioselectivity.
Key words: β,γ-alkynyl α-amino ester, chemoselectivity, enantioselectivity, transfer hydrogenation, benzothiazoline


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