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。