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Robustness Screen in Enantioselective Catalysis Enabled Generation of Enantioenriched Heterocyclic Scaffolds in One Pot

机译:在对映选择性催化中的鲁棒性筛选可在一锅中生成对映富集的杂环支架

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摘要

Enantioselective catalysis has emerged as a powerful synthetic paradigm and has accelerated the development of new methods to make diverse chiral molecules. Generally, these reactions are very sensitive to the steric and electronic environment present in the catalyst as well as the substrates. With this scenario, the presence of an additional component in the reaction mixture is expected to add complexity in achieving the enantioselective variants. Herein, we report that various enantioenriched molecules could be obtained from multiple starting materials in one pot. The reaction of aminoaromatics A with alkynols B-1, B-2, B-3...B-n with a Au-I/chiral BrOnsted acid catalyst afforded AB(1)*, AB(2)*, AB(3)*...AB(n)*; while, the reaction of alkynols B with aminoaromatics A(1), A(2), A(3)...A(n) under the same reaction conditions gave A(1)B*, A(2)B*, A(3)B*...A(n)B*.
机译:对映选择性催化已经成为一种强大的合成范例,并加速了制备多种手性分子的新方法的开发。通常,这些反应对催化剂以及底物中存在的空间和电子环境非常敏感。在这种情况下,预期反应混合物中存在额外的组分会增加实现对映选择性变体的复杂性。在本文中,我们报道可以从一锅中的多种原料中获得各种对映体富集的分子。氨基芳族化合物A与炔醇B-1,B-2,B-3 ... Bn与Au-1 /手性布朗斯台德酸催化剂的反应得到AB(1)*,AB(2)*,AB(3)* ... AB(n)*;同时,炔醇B与氨基芳烃A(1),A(2),A(3)... A(n)在相同的反应条件下反应,得到A(1)B *,A(2)B *, A(3)B * ... A(n)B *。

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