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目的研究酪氨酸激酶c-Met受体抑制剂LY-2801653的合成方法。方法以3-羟基苯甲醛为起始原料,经过溴化、亲核取代、成席夫碱、取代、环化、Suzuki反应、氢化还原、酰胺化等8步反应制得目标化合物LY-2801653。结果与结论目标化合物和中间体的结构通过~1H-NMR、MS谱确证。该合成方法具有原料易得、安全高效、成本较低、操作简便等特点,适于工业化放大制备。
Objective To study the synthesis of tyrosine kinase c-Met receptor inhibitor LY-2801653. Methods The target compound LY-2801653 was obtained from 3-hydroxybenzaldehyde through 8 steps, such as bromination, nucleophilic substitution, Schiff base, substitution, cyclization, Suzuki reaction, hydrogenation reduction and amidation. Results and Conclusion The structures of target compounds and intermediates were confirmed by ~ 1H-NMR and MS spectra. The synthesis method has the advantages of easy availability of raw materials, safety and high efficiency, low cost, easy operation and the like, and is suitable for industrialized amplification and preparation.