Application of Sequential Cu(I)/Pd(0)-Catalysis to Solution-Phase Parallel Synthesis of Combinatorial Libraries of Dihydroindeno[1,2-<i>c</i>]isoquinolines
作者:Sarvesh Kumar、Thomas O. Painter、Benoy K. Pal、Benjamin Neuenswander、Helena C. Malinakova
DOI:10.1021/co200027c
日期:2011.9.12
methodology is compatible with a wide-range of aliphatic linear, branched, and ester functionalized N-substituents. Unexpectedly, the formation of regioisomers featuring a 1,2,3-contiguous substitution pattern in the aromatic ring of the indene core was observed. Three distinct combinatorial libraries with a total of 111 of members were synthesized, and 80 highly substituted dihydroindenoisoquinolines structurally
实现了并行的溶液相合成二氢茚并异喹啉组合库的顺序Cu(I)/ Pd(0)催化的多组分耦合和环空协议。关于茚核的芳基环上的取代图案以及N-取代基的方案范围和局限性已经定义,这表明该方法与各种脂族直链,支链,和酯官能化氮-取代基。出乎意料的是,观察到在茚核的芳环中形成具有1,2,3-连续取代图案的区域异构体。合成了三个不同的组合文库,共有111个成员,并且提供了80种与已知药物结构相关的高度取代的二氢茚并异喹啉,包括一些由两种区域异构体的混合物组成的混合物,可用于生物活性测试。