甲磺酸伊马替尼的合成

Synthesis of Imatinib Mesylate

用3-乙酰吡啶(2)和N,N-二甲基甲酰胺二甲缩醛(3)反应得3-二甲胺基-1-(3-吡啶基)-2-丙烯-1-酮(4),4与2-甲基-5-硝基苯基胍硝酸盐(6)经成环、还原、由4-氯甲基苯甲酰氯酰化后与N-甲基哌嗪反应,所得伊马替尼再成盐即得甲磺酸伊马替尼,总收率约58%(以2计)。

Imatinib mesylate was synthesized by reaction from 3-acetylpyridine（2） and N,N-dimethylformamide dimethyl acetal（3） to give 3-dimethylamino-1-（3-pyridinyl）-2-propylene-1-one（4）, which was subjected to cyclization, reduction, acylation with 4-chloromethylbenzoyl chloride and reaction with N-methylpiperazine, followed by salt formation with an overall yield of about 58%（based on 2）.