The Synthesis of Cancer Treatment Medicine Erlotinib
WANG Xian1, SONG Fang2, FENG Qingwei1
1. Chemistry Division of Patent Examination Cooperation Center, State Intellectual Property Office of the People's Republic of China, Beijing 100083, China;2. China Animal Husbandry Institute, Beijing 102206, China
Abstract：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.
王险;宋芳;冯清伟. 癌症治疗药物埃罗替尼的合成[J]. , 2012, 30(5): 49-51.
WANG Xian;SONG Fang;FENG Qingwei. The Synthesis of Cancer Treatment Medicine Erlotinib. , 2012, 30(5): 49-51.
2012, Vol. 30 
