Synthesis of erlotinib hydrochloride from 4-chloro-6,7 bis- (2-methoxyethoxy)- quinazoline

Abstract

A highly efficient and economical process in synthesizing Erlotinib Hydrochloride, as a useful drug in treatment of non-small-cell lung cancer. Erlotinib hyrochloride was synthesized in seven steps. In this study, I focus on synthesis of product at last step which Erlotinib Hydrochloride is synthesized from 4-chloro-6,7 bis-(methoxyethoxy)-quinazoline with water solvent and cytotoxicity of Erlotinib with lung cancer cell. The final product was characterized by 1H and 13 C nuclear magnetic resonance (NMR), mass spectra (MS), and thin layer chromatography,and purities of final product were determined by high performance liquid chromatogram (HPLC). Then the final product was also conducted to Evaluate its activityagainst lung cancer cell.This proposed method obtained erlotinib with 98.2% purity.And in 10 μg/ml surveyed concentration, Erlotinib exhibited a high cytotoxicity with NCI-H460 lung cancer cells which inhibited 84% growth of the cell. Keywords: Erlotinib Tyrosine kinase Nonsmall cell lung cancer Cytotoxicity