近日，美国威斯康星大学麦迪逊分校Jennifer M. Schomaker团队报道了手性硫（VI）平台整合了复杂分子和烷烃原料的选择性C-H胺化。相关论文发表在2026年4月23日出版的《科学》杂志上。

复杂分子与简单烷烃对催化剂控制的碳-氢（C-H）键官能团化提出了截然不同的挑战。密集官能团化的骨架需要在多个反应位点中实现精准靶向，同时耐受敏感官能团；而缺乏导向基团的未活化底物则需选择性激活那些极其惰性、几乎相同的C-H键。

研究组通过将一个经典手性辅助基重新利用，构建了一个由银催化与手性硫（VI）氮宾前体介导的统一、选择性强且可预测的C-H胺化平台。该系统不仅能够对活化C-H键进行立体发散性的后期胺化，具有广泛的官能团耐受性和水性环境兼容性，还能介导化学原料的温和、选择性胺化。硫（VI）基序功能作为一个模块化、立体构型明确且具有药物相关性的合成枢纽，可快速实现化合物库的多样化，既支持靶向合成，也支持多样性导向合成。

附：英文原文

Title: Chiral S(VI) platform unifies selective C–H amination of complex molecules and alkane feedstocks

Author: Tuan Anh Trinh, Derek B. Hu, Anna J. Kenny, Ethan M. Warrington, Stanislav Cherempei, Ilia A. Guzei, Jennifer M. Schomaker

Issue&Volume: 2026-04-23

Abstract: Complex molecules and simple alkanes pose distinct challenges for catalyst-controlled carbon-hydrogen (C–H) functionalizations. Whereas densely functionalized scaffolds require precise targeting among multiple reactive sites while tolerating sensitive functionalities, unactivated substrates that lack directing groups require selective activation of exceptionally inert, nearly identical C–H bonds. In this work, we addressed both challenges by repurposing a classic chiral auxiliary into a unified, selective, and predictable C–H amination platform mediated by silver catalysis and chiral sulfur(VI) nitrene precursors. This system enables stereodivergent, late-stage aminations of activated C–H bonds with broad functional group tolerance and compatibility with aqueous conditions while also mediating mild, selective aminations of chemical feedstocks. The sulfur(VI) motif functions as a modular, stereodefined, and medicinally relevant synthetic linchpin for rapid library diversification, enabling both target- and diversity-oriented synthesis.

DOI: aee3321

Source: https://www.science.org/doi/10.1126/science.aee3321