Study On The Synthesis Of Gefitinib And Erlotinib

The introduction of epidermal growth factor receptor and the therapeutical function, research development of epidermal growth factor receptor inhibitor were reviewed briefly in this paper. The therapeutical function and research development of Gefitinib and Erlotinib, which were tyrosine kinase inhibitors, were introduced in detail.The synthetic methods for Gefitinib and Erlotinib were investigated and an economical and reasonable synthetic route was studied. Gefitinib was synthesized with a total yield of 49.5% from 3-hydroxy-4-methoxybenzaldehyde via six steps of reaction. Erlotinib was synthesized with a total yield of 53.9% from 3,4-dihydroxybenzaldehyde via six steps of reaction.The synthetic procedure of the intermediates was studied intensively and optimized. The operation was simplified and could be practical in a large scale. All the materials are available domestically.The structures of Gefitinib, Erlotinib and the intermediates were confirmed by ’H-NMR and mass spectrum detection.