Abstract:
Herein we describe a sustainable and efficient photocatalytic method for the stereoselective radical alkylation of chiral sulfinyl imines. By employing readily available non-prefunctionalized radical precursors and the cost-effective TBADT as a direct HAT photocatalyst, we successfully obtain diverse chiral amines with high yields and excellent diastereoselectivity under mild conditions. This method provides an efficient approach for accessing a diverse array of medicinally relevant compounds, including both natural and synthetic α-amino acids, aryl ethyl amines, and other structural motifs commonly found in approved pharmaceuticals and natural product.
摘要:
在此,我们描述了一种可持续且有效的光催化方法,用于手性亚磺酰基亚胺的立体选择性自由基烷基化。通过使用容易获得的非预官能化自由基前体和低负载的TBADT作为直接HAT光催化剂,我们成功地获得了不同的手性胺,在温和的条件下,高产率和优异的非对映选择性。这种方法提供了一种有效的方法来获取不同的药物相关化合物,包括天然和合成的α-氨基酸,芳基乙基胺,以及批准的药物和天然产品中常见的其他结构图案。