提供了一种埃罗替尼的制备方法,该方法以3,4-二羟基苯甲酸乙酯为起始原料,经过与乙二醇单甲醚的醚化反应,再经硝化、还原、缩合成环,然后经卤化与间氨基苯乙炔反应,最后通入干燥的氯化氢气体后生成埃罗替尼。其中,硝化工艺相比于以前的工艺有较大的改进。本合成路线具有反应条件温和、总收率好、后处理简便易行和易于进行工业化生产等优点。

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.