The Synthesis of Cancer Treatment Medicine Erlotinib

The concise synthesis of Erlotinib was described.Treatment of Ethyl 3,4-dihydroxybenzoate with 2-methoxyethyl methanesulfonate followed by nitration,reduction,cyclization and chloration to afford 4-chloro-6,7-bis(2-methoxyethoxy)-1,4-dihydroquinazoline,which was treated with 3-ethynylaniline and then with dry hydrochloride to give Erlotinib.In this synthesis,the nitration process has greatly been improved.The advantages of this synthetic route include short reaction time,good total yield,and simple work-up.