Difluorocarbene enabled ester insertion/1,4-acyl rearrangement of 2-acetoxylpyridines: Modular access to gem-difluoromethylenated 2-pyridones
作者:Shi-Wei Li、Gang Wang、Zhi-Shi Ye
DOI:10.1016/j.tetlet.2023.154413
日期:2023.4
An efficient and simple protocol for the construction of gem-difluoromethylenated 2-pyridones via difluorocarbene enabled ester insertion/acyl rearrangement of 2-acetoxylpyridines and (bromodifluoromethyl)trimethylsilane has been documented. The reactions feature transition-metal free, mild reaction conditions and excellent functional group compatibility. The late-stage modification of bioactive molecules
已经记录了一种有效且简单的方案,用于通过二氟卡宾构建宝石- 二氟亚甲基化 2-吡啶酮,使 2-乙酰氧基吡啶和(溴二氟甲基)三甲基硅烷的酯插入/酰基重排成为可能。该反应不含过渡金属,反应条件温和,官能团相容性好。生物活性分子的后期修饰、放大反应和合成转化证明了该协议的实用性。