Catalytic Desulfonylative Alkylation of Unactivated Olefins as a Vehicle to Forge sp3-architectures

• Applicant: Dr. Liangliang Zhang
• Subject Area: Organic Molecular Chemistry - Synthesis and Characterisation
• Term: since 2023
• Project identifier: Deutsche Forschungsgemeinschaft (DFG) - Project number 520709125

An increase of sp3 character in drug candidates has shown to improve several molecular attributes that ultimately contribute to clinical success. Despite the advances realized, our chemical industry is hesitant to apply the know-how of the existing methods for sp3-sp3 bond-formation due to the accessibility of the starting precursors, the utilization of well-defined organometallics and/or the lack of generality, particularly in late-stage functionalization. This project offers new vistas for accessing sp3 architectures by the development of a catalytic site-selective desulfonylative alkylation of readily available unactivated olefins, compounds derived from the petroleum processing. The utilization of alkyl sulfones as nucleophilic handles via C-S bond-functionalization offers versatility in terms of the coupling products that can be accessed, and the opportunity for late-stage diversification given the wide number of advanced sulfones currently available in the medicinal chemistry portfolio.

• DFG Programme: WBP Fellowship
• International Connection: Spain
• Host: Professor Dr. Ruben Martin