Abstract：
The first Ficini reaction between ynamides and acrylates is reported herein. The reaction is catalyzed by B(C6F5)3 acting as a Lewis acid and is giving access to stable tri-substituted aminocyclobutenes in high yield. The resulting products can be hydrogenated and epimerized under basic conditions or in presence of a Lewis acid, providing two distinct trans- aminocyclobutane monoester stereoisomers in high yield and diastereoisomeric ratio (up to quantitative yield and >99:1 dr).
摘要：
本文报道了炔烃和丙烯酸酯之间的第一Ficini反应。该反应由作为路易斯酸的B(C6F5)3催化,并以高产率获得稳定的三取代氨基环丁烯。所得产物可以在碱性条件下或在路易斯酸存在下进行氢化和差向异构化，以高产率和非对映异构体比例(高达定量产率和>99:1dr)提供两种不同的转氨基环丁烷单酯立体异构体。
