The ability to functionalize complex compounds at a late-stage in synthesis opens up the capacity to rapidly build libraries of functionalized drug-like compounds. This enables fast access to diverse structures from a single late-stage compound, facilitating structure-activity relationship (SAR) exploration, as well as modulation of physicochemical properties in the search of new drugs. Here we describe the application of late-stage functionalization techniques, including modern synthetic methodology, classical chemistry transformations and biocatalysis, in the synthesis of a novel kinase inhibitor. Through late-stage modification of an early <i>in vivo</i> probe, we were able to rapidly explore structure-activity and structure-property relationships, far quicker than by conventional step-wise synthetic approaches. This allowed us to identify key architectural features to enhance potency, stability and physicochemical properties and ultimately access improved compounds.<br/>

Application of late-stage functionalization techniques in the identification of novel kinase inhibitors

ACS Fall 2020 Virtual Meeting

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.