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目的改进抗骨质疏松药米诺膦酸的关键中间体2-(咪唑并[1,2-a]吡啶-3-基)乙酸的制备方法。方法以2-氧代戊二酸二乙酯为起始原料,经溴代、环合、水解和脱羧4步反应制得目标产物。结果目标化合物的熔点1、H-NMR谱数据与文献报道相符,总收率为40.5%(以2-氧代戊二酸二乙酯计)。结论与文献报道的方法相比,改进后的工艺路线后处理简单,更有利于工业化生产。
OBJECTIVE To improve the preparation of 2- (imidazo [1,2-a] pyridin-3-yl) acetic acid, a key intermediate of minodronic acid against osteoporosis. Methods Starting from 2-oxopentanedioic acid diethyl ester, the target product was obtained through 4 steps of bromination, cyclization, hydrolysis and decarboxylation. Results Melting point 1 of the target compound. The H-NMR spectrum was consistent with that reported in the literature. The overall yield was 40.5% (as diethyl 2-oxopentanedioate). Conclusion Compared with the methods reported in the literature, the improved postprocessing process is simple and more conducive to industrial production.