A palladium-catalyzed, amine-directed C(sp2)–H carbonylation of α,α-disubstituted benzylamine under 1 atm of CO for the facile synthesis of sterically hindered benzolactam has been developed. The key to success is the use of 2,2,6,6-tetramethyl-1-piperidinyloxy as the crucial sole oxidant. The synthetic utility of this transformation has been demonstrated by the first concise synthesis of the natural
已开发了在1 atm的CO下
钯催化的,胺导向的α,α-二取代的
苄胺的C(sp 2)-H羰基化反应,可轻松合成位阻苯并内酰胺。成功的关键是使用2,2,6,6-四甲基-1-
哌啶基氧基作为关键的唯一氧化剂。
天然产物spiropachysin-20-one的第一个简明合成证明了这种转化的合成效用。