Identification and synthesis of novel medicinal chemistry relevant heterocycles

Replacing high throughput biochemical screening for drug targets, with high throughput fragment screening (e.g. XChem methodology) followed by enhanced computational approaches to optimise fragment hits into leads, could accelerate projects and reduce costs and the requirement for large compound libraries. To achieve this high quality fragment libraries covering a broad chemical space must be developed. Fortunately, thousands of possible medicinal chemistry relevant heterocycles that would enrich fragment screening sets and be useful building blocks for medicinal chemistry campaigns are unreported.

These novel heterocycles, knowledge of workable synthetic routes and the establishment of new synthetic methodology will facilitate the delivery of medicinal chemistry programmes.