报告题目：后期修饰中看似简单却非显而易见的转化反应（Simple-Looking but Non-Obvious Transformations for Late-Stage Modification）
报告人：董广斌(Guangbin Dong）教授 美国芝加哥大学
报告时间：2026年8月15日10:00-12:00
报告地点：中国–东盟艺术学院 A 栋 A1018 学术报告厅（东盟小礼堂）
报告内容简介：后期官能化已成为药物发现中增加类药性分子结构多样性的重要策略，但目前可用的后期官能化手段仍相对有限，且多集中于C−H键官能化。本报告将介绍三种看似简单、实则非显而易见的转化反应，这些反应可对复杂分子实现非常规的后期修饰。第一种转化实现未活化芳烃的导向性加氢饱和，能够在复杂分子中实现苯环向环己烷环的位点选择性转化。第二种转化可在常规芳基三氟甲磺酸酯或芳基氯化物上同时并排引入两个化学性质迥异的硼基，从而获得具有发散性区域选择性的双官能化产物。第三种转化则代表一种“原子置换”策略，即用硫或氮等杂原子替换羰基。该方法可由易得的环状酮高效构建饱和杂环，其应用实例包括将常见甾体骨架快速转化为相应的硫杂甾体和氮杂甾体。
Abstract：Late-stage functionalization has become an increasingly important strategy for increasing structural diversity of analogues in drug discovery. However, the current late-stage functionalization tactics remain limited, mostly centered on C-H functionalization. In this talk, three simple-looking but non-obvious transformations will be discussed, which allow for unusual late-stage modifications of complex molecules. The first transformation promotes directed saturation of unactivated arenes, leading to site-selective conversion of a benzene ring into a cyclohexane ring in complex molecules. The second transformation enables simultaneous installation of two chemically different boryl groups side-by-side into common aryl triflates or chlorides, resulting in divergent regioselective difunctionalization. The third one represents an “atom swap” strategy, which replaces a carbonyl group with a heteroatom, such as sulfur or nitrogen. This method can efficiently introduce saturated heterocycles from readily available cyclic ketones, and the application includes rapid conversion of readily available steroids into the corresponding thia- and azasteroids.
