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发明公开
CN101921260A 一种伊马替尼的制备方法 有权 转让

一种伊马替尼的制备方法
摘要：
本发明涉及一种伊马替尼的制备方法。以如结构式(II)所示的化合物N-(5-氨基-2-甲基苯基)-4-(3-吡啶基)-2-氨基嘧啶(N-(5-Amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine)和如结构式(III)所示的化合物4-(4-甲基哌嗪甲基)苯甲酸(4-[(4-Methylpiperazin-l-yl)methyl]benzoic acid)为起始原料，在有机溶剂中在催化剂的作用下，在50～90℃滴加亚磷酸酯，1～2小时内滴加完，继续在50～90℃保温反应，制备如结构式(I)所示的化合物伊马替尼。有机溶剂是N，N-二甲基甲酰胺，N，N-二甲基乙酰胺或N-甲基吡咯烷酮。催化剂为吡啶；亚磷酸酯是亚磷酸三甲酯、亚磷酸三乙酯或亚磷酸三苯酯。本发明技术方案反应步骤简单，反应易于控制，生产周期短；所用原料为低毒性，对环境污染小；产品质量较好，收率能达到95％，纯度达到99.5％。
摘要（英）：

The invention relates to a method for preparing imatinib, which comprises the following steps of: with a compound N-(5-Amino-2-methylphenyl)-4-(3-pyridyl)-2-pyrimidineamine shown as the structural formula (II) and a compound 4-[(4-Methylpiperazin-l-yl)methyl]benzoic acid shown as the structural formula (III) as initial raw materials, dropwise adding phosphite ester at 50-90 DEG C for 1-2 hours inthe presence of a catalyst in an organic solvent; and continuously insulating and reacting at 50-90 DEG C to obtain the compound imatinib shown as the structural formula (I). The organic solvent is N,N-dimethylformamide, N,N-dimethylacetylamide or N-methylpyrrolidone. The catalyst is pyridine; and the phosphite ester is trimethyl phosphate, triethyl phosphate or triphenyl phosphate. The technical scheme of the invention has the advantages of simple reaction step, easy control of reaction, short production cycle, low toxicity of used raw materials, less pollution to the environment and higher product quality, and the yield can reach 95 percent, and the purity reaches 99.5 percent.

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