Building C(sp³)-rich complexity by combining cycloaddition and C-C cross-coupling reactions.

ABSTRACT: Prized for their ability to rapidly generate chemical complexity by building new ring systems and stereocentres¹, cycloaddition reactions have featured in numerous total syntheses² and are a key component in the education of chemistry students³. Similarly, carbon-carbon (C-C) cross-coupling methods are integral to synthesis because of their programmability, modularity and reliability⁴. Within the area of drug discovery, an overreliance on cross-coupling has led to a disproportionate representation of flat architectures that are rich in carbon atoms with orbitals hybridized in an sp² manner⁵. Despite the ability of cycloadditions to introduce multiple carbon sp³ centres in a single step, they are less used⁶

SUBMITTER: Chen TG 

PROVIDER: S-EPMC6126906 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature