Synthesis of 5-Aryl-Pyrrolo[2,3-d]pyrimidines and Their Bioactivity

Abstract

The epidermal growth factor receptor tyrosine kinase is one of the more important targets in targeted cancer therapy. However, on prolonged administration of EGFR inhibitors, resistance emerge, which in 50% of the cases is due to a second mutant, EGFR-T790M. This renders the first class of drugs inefficient. The goal of the master project is to synthesise new pyrrolopyrimidines as potential EGFR T790M inhibitors and as EGFR inhibitors, and optimise route selection and key coupling steps.