The total synthesis of K-252c (staurosporinone) via a sequential C–H functionalisation strategy

Abstract

A synthesis of the bioactive indolocarbazole alkaloid K-252c (staurosporinone) <i>via</i> a sequential C-H functionalisation strategy is reported. The route exploits direct functionalisation reactions around a simple arene core and comprises of two highly-selective copper-catalysed C-H arylations, a copper-catalysed C-H amination and a palladium-catalysed C-H carbonylation, which build up the structural complexity of the natural product framework.