论文部分内容阅读
1-甲基-1H-吲哚和2,4-二氯嘧啶通过偶联得3-(2-氯嘧啶-4-基)-1-甲基吲哚,与4-氟-2-甲氧基-5-硝基苯胺-(由4-氟-2-甲氧基苯胺经硝化制得)发生取代反应后,再与N,N,N’-三甲基乙二胺缩合得N-(2-二甲胺基-乙基)-2-甲氧基-N-甲基-N-[4-(1-甲基-1H-吲哚-3-基)-嘧啶-2-基]-5-硝基-苯-1,4-二胺,经还原、酰胺化和成盐得抗肿瘤药物奥默替尼。总收率38%(以4-氟-2-甲氧基苯胺计),纯度99.5%。
1-methyl-1H-indole and 2,4-dichloropyrimidine were coupled by coupling with 3- (2-chloropyrimidin-4-yl) 5-nitroaniline - (by 4-fluoro-2-methoxyaniline by nitration system) substitution reaction, and then N, N, N’- trimethyl ethylenediamine condensation N- ( Dimethylamino-ethyl) -2-methoxy-N-methyl-N- [4- (1 -methyl- 1 H-indol-3 -yl) -pyrimidin-2-yl] - 5-nitro-benzene-1,4-diamine, after reduction, amidation and salt into the antitumor drug ometettinib. The total yield of 38% (4-fluoro-2-methoxyaniline dollars), the purity of 99.5%.