Novel Bicyclo[1.1.1]pentane (BCP) Fragments, their Roles, Preparation and the Challenges in Synthesis at Scale

Bicyclo[1.1.1]pentane (BCP) is emerging as an interesting fragment in medicinal chemistry. It serves as a bioisostere for a phenyl or tert-butyl group. Due to the SP3 hybridization of the structures, it is considered to generate drug-like molecules with good passive permeability, high aqueous solubility, and improved metabolic stability.  BCP derivatives are already a pharmaceutically important scaffold. However, large scale preparation of BCP is still considered synthetically challenging. This webinar is going to review the medicinal application of the BCP in discovery new drug candidates, its metabolism and review new synthetic development to generate complex BCP derivatives in the recent literature.

This webinar was delivered by Dr Xiaoqi (Charles) Chen from Bellen Chem who kindly sponsored the session.