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.
WANG Xian;SONG Fang;FENG Qingwei
. The Synthesis of Cancer Treatment Medicine Erlotinib[J]. Science & Technology Review, 2012
, 30(5)
: 49
-51
.
DOI: 10.3981/j.issn.1000-7857.2012.05.007