化学
对映选择合成
亚胺
磷酸
催化作用
组合化学
曼尼希反应
有机化学
作者
Congcong Zhang,Lijun Chen,Baochun Shen,Hua Xie,Wei Li,Zhong‐Wen Sun
摘要
The chiral keto-substituted propargylamines are an essential class of multifunctional compounds in the field of organic and pharmaceutical synthesis and have attracted considerable attention, but the related synthetic approaches remain limited. Therefore, a concise and efficient method for the enantioselective synthesis of β-keto propargylamines via chiral phosphoric acid-catalyzed asymmetric Mannich reaction between β-keto acids and C-alkynyl N-Boc N,O-acetals as easily available C-alkynyl imine precursors has been demonstrated here, affording a broad scope of β-keto N-Boc-propargylamines in high yields (up to 97%) with generally high enantioselectivities (up to 97 : 3 er).
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