The indole flamework is one of the ubiquitous heterocycles in natural products and pharmaceuticals. Thus, various methods have been developed to afford functionalized indoles. Recently, direct functionalization of indoles at the C7 position has been emerged. Introduction of directing groups such as hydrosilyl, phosphinoyl, and pivaloyl group at the N1 position enables site-selective functionalization via coordination to metal catalysts. In these cases, bulkiness of the directing group is found to be crucial for high reactivity and C7-selectivity.
2017 社団法人 有機合成化学協会