Synthesis Of Novel Thiophene-Bipyrimidine EGFR Inhibitors

Pyrimidine is a prevalent component in numerous antineoplastic medications. Herein, starting with Olmutinib, by applying the concept of skeleton transition, the thiopheno [3,2-d] pyrimidines were categorized into a thiophene bipyrimidine framework as the foundation, leading to the creation of a novel thiophene bipyrimidine compound. The target product was synthesized through nucleophilic substitution, Suzuki coupling, and reduction reactions employing 2-pyrrolidine-4-trichloropyrimidine as the raw material and triethylamine as the base, leading to the efficient synthesis of compound 7.The structure of compound 7 was confirmed by MS and 1H NMR spectrum and the total yield was high up to 65.7%.