One-pot tandem complexity-generating reaction based on Ugi four component condensation and intramolecular cyclization

A novel complexity-generating reaction is described, which can be used in a high-throughput parallel solution-phase combinatorial format. The synthetic pathway features the Ugi four component reaction followed by intramolecular cyclization via C–C bond formation. Starting from readily available initial reactants, the described approach leads to generation of novel 3-oxoisoindoline-1-carboxamides with four points of diversity around the core scaffold. The scope and limitations of the involved chemistry and some chemical transformations of the synthesized compounds are discussed.