【摘要】 5-氟-2-硝基苯甲醚经与哌嗪缩合、乙酰化、还原制得1-(3-甲氧基-4-氨基苯基)-4-乙酰基哌嗪(4);另用2,4-二氯-5-三氟甲基嘧啶经与3-硝基苯胺缩合、还原、酰胺化制得N-[3-(2-氯-5-三氟甲基嘧啶-4-氨基)苯基]丙烯酰胺(7)。4和7经缩合制得EGFR抑制剂类抗肿瘤药CO-1686,总收率约71%(以2,4-二氯-5-三氟甲基嘧啶计)。更多还原

【Abstract】 CO-1686 was synthesized from 2,4-dichloro-5-(trifluoromethyl)pyrimidine by condensation with 3-nitroaniline, reduction and amidation to afford N-[3-[[2-chloro-5-(trifluoromethyl)pyrimidin-4-yl]amino]phenyl]acrylamide(7), which was subjected to condensation with 1-(4-amino-3-methoxyphenyl)-4-acetylpiperazine(4) obtained from 4-fluoro-2-methoxy-1-nitrobenzene by condensation with piperazine, acetylation and reduction with an overall yield of approximately 71%(based on 2,4-dichloro-5-(trifl uoromethyl)pyrimidine).更多还原