Investigating a novel catalysis-based approach to access functionalised heterocyclic scaffolds

Lead Research Organisation: University of Birmingham
Department Name: School of Chemistry

Abstract

Heterocyclic motifs form the basis of many active pharmaceutical ingredients (API) and new hit/lead molecules against disease targets. A novel transition-metal based reactivity mode discovered by the Davies group (formal cycloadditions using nucleophilic nitrenoids) provides efficient and convergent access to heterocyclic motifs that are of particular import in the pharmaceutical sector. Efficient methods to access functionalised and diverse heterocyclic motifs result in substantial improvements in process efficiency for the manufacture of complex molecules [and the generation of less waste with reduced energy and chemical resource demands], and also provide the framework for the discovery of new medicines. This project will seek deeper understanding of the control factors in this new reactivity and explore the applicability of the method as a general tool for the preparation of high quality functionalised heterocyclic motifs to enable academic and pharmaceutical discovery and development activities. The project falls under the EPSRC research remit of: - Leading-edge healthcare and medicine - Manufacturing processes and materials of the future. This project will link the Davies group's expertise in the discovery of efficient new catalysis-based methods with Lilly scientists expertise in applying catalysis-based methods to drug discovery and scale-up synthesis of APIs.

Publications

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Studentship Projects

Project Reference Relationship Related To Start End Student Name
EP/R512436/1 01/10/2017 31/03/2022
1943894 Studentship EP/R512436/1 01/10/2017 24/12/2021 Peter Simm