2-(咪唑并[1,2-a]吡啶-3-基)乙酸的制备

Synthesis of 2-(imidazopyridin-3-yl)acetic acid

研究了一种用于治疗骨质疏松症药物的关键中间体米诺膦酸的制备方法。实验以二乙氧基膦酰乙酸乙酯和2,2-二甲氧基乙醛为起始原料,经维蒂希-霍纳反应、水解、环合、水解4步制备得到标题化合物。其熔点与1HNMR和文献报道的结果一致,总收率87.5%(以2-氨基吡啶计)。该方法克服了文献报道的工艺缺陷,与现有技术相比,后处理更简单,更适合工业化生产。

To study the preparation of the key intermediate of minnodronic acid,a drug which was used to the treatment of osteoporosis. The target compound was synthesized from tri- ethyl phosphonoaeetate and 2, 2-dimethoxyacetaldehyde via four steps through wittig-horner reaction, hydrolysis, cycliza- tion and hydrolysis. The melting point and I HNMR of final compound was in accordance with the literature, and the over- all yield of was 87.5%. Some drawbacks in the literature were improved and the method was easy for synthesis and suitable for industrial manufacturing.