CAJ | 학술논문

2-氨基-5-噻唑甲酸乙酯经N-Boc保护、水解,经酰氯成酰胺、脱保护和与2-甲基-4,6-二氯嘧啶进行亲核取代等反应制得N-(2-氯-6-甲基苯基)-2-[(6-氯-2-甲基-4-嘧啶基)氨基]-5-噻唑甲酰胺,然后再与N-(2-羟乙基)哌嗪缩合制得抗肿瘤药达沙替尼,总收率约46%.
2-안기-5-새서갑산을지경N-Boc보호、수해,경선록성선알、탈보호화여2-갑기-4,6-이록밀정진행친핵취대등반응제득N-(2-록-6-갑기분기)-2-[(6-록-2-갑기-4-밀정기)안기]-5-새서갑선알,연후재여N-(2-간을기)고진축합제득항종류약체사체니,총수솔약46%.
Dasatinib was synthesized by condensation of N-(2-chloro-6-methylphenyl)-2-[(6-chloro-2-methylpyrimidin-4-yl)amino]-5-thiazolecarboxamide(10) with N-(2-hydroxyethyl) piperazine with an overall yield of about 46%. Compound 10 was obtained from 2-amino-5-thiazolecarboxylic acid ethyl ester by iV-Boc protection, hydrolysis, chlorination, amidation, deprotection and nucleophilic substitution with 2-methyl-4,6-dichloropyrimidine.