Synthesis of diversely functionalised 2,2-disubstituted oxetanes: fragment motifs in new chemical space

Abstract

Di-, tri- and tetra-substituted oxetane derivatives with combinations of ester, amide, nitrile, aryl, sulfone and phosphonate substituents are prepared as fragments or building blocks for drug discovery. The synthesis of these novel oxetane functional groups, in new chemical space, is achieved via rhodium-catalysed O–H insertion and C–C bond forming cyclisation.