他洛沙酯(1,Talosalate,2-乙酰氧基苯甲酸3-羟基苯酞酯)是一种新的乙酰水杨酸类消炎镇痛药,属较理想的前体药物。有关1的合成方法较多,国内尚未见报道。我们以邻苯二甲酰亚胺为原料,经还原、溴化、酯化而得。其合成路线见下页。改变最后一步的部分反应条件,乙酰水杨酸-溴苯酞-三乙胺摩尔比为1∶1∶1.2,控温65～70℃,并延长反应时间,以乙醇重结晶,敢率可较文献报道有所提高。 Talosalate (1, 3-hydroxyphthalidyl 2-acetoxybenzoate) is a new anti-inflammatory analgesic acetylsalicylic acid, which is an ideal prodrug. More about the synthesis method of 1, has not been reported in China. We phthalimide as raw material, the reduction, bromination, esterification derived. The synthetic route see next page. Part of the reaction conditions to change the last step, acetylsalicylic acid - bromophthalide - triethylamine molar ratio of 1: 1: 1.2, temperature 65 ~ 70 ℃, and extend the reaction time, ethanol recrystallization, dare to compare Literature reports have increased.