近日，南昌大学熊小东团队报道了使用手性磷酸催化剂通过硫烯酰胺的不对称胺化反应实现手性亚磺酰脒的对映选择性合成。相关论文于2025年12月9日发表在《德国应用化学》杂志上。

尽管手性硫化合物在药物科学与有机化学中具有重要应用，但精确构建有价值的手性亚磺酰脒的高效方法仍较为有限。

研究组报道了一种手性磷酸催化的不对称策略，通过直接胺化硫烯酰胺来合成手性亚磺酰脒。该方法在多种亚磺酰脒化合物中展现出优异的底物普适性、出色的收率和立体选择性。通过克级规模反应、产物衍生化以及天然产物和药物的后期官能团化，进一步彰显了这一稳健方案的合成实用性与应用潜力。

附：英文原文

Title: Enantioselective Synthesis of Chiral Sulfinamidines via Asymmetric Amination of Sulfenamides Using a Chiral Phosphoric Acid Catalyst

Author: Qi Chen, Chaoxiang Ning, Xuhao Ren, Xiaodong Xiong

Issue&Volume: 2025-12-09

Abstract: Despite the significant applications of stereogenic-at-sulfur compounds in pharmaceutical sciences and organic chemistry, efficient methods for precise construction of valuable chiral sulfinamidines remain limited. Herein, we disclosed a chiral phosphoric acid-catalyzed asymmetric strategy for the synthesis of chiral sulfinamidines through the direct amination of sulfenamides. This method demonstrated remarkable substrate scope and excellent yields and stereoselectivities across a diverse array of sulfinamidine compounds. The synthetic utility and practicability of this robust protocol were further highlighted through gram-scale reactions, product derivatization and late-stage functionalization of natural products and drugs.

DOI: 10.1002/anie.202524073

Source: https://onlinelibrary.wiley.com/doi/10.1002/anie.202524073