摘要
2-氨基吡啶与4-溴乙酰乙酸乙酯在碳酸氢钠和二噁烷中环合制得2-(咪唑并[1,2-a]吡啶-3-基)乙酸乙酯,再经浓盐酸水解、与三氯氧磷/亚磷酸反应、浓盐酸水解后用水重结晶,制得高纯度抗骨质疏松药米诺膦酸,总收率约23%(以2-氨基吡啶计)。
Ethyl 2-（imidazopyridin-3-yl）acetate（5） was synthesized by cyclization of 2-aminopyridine and ethyl 4-bromo-3-oxobutanoate in the presence of NaHCO3 in hot dioxane,and subsequently hydrolysis with concentrated HCl to yield 2-（imidazopyridin-3-yl）acetic acid hydrochloride（6）.Compound 6 was treated with phosphorous acid and phosphorus oxychloride,followed by hydrolysis with HCl and then recrystallization from H2O to afford the highly purified anti-osteoporosis agent minodronic acid（1） in 23% overall yield（based on 2-aminopyridine）.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2012年第5期321-323,共3页
Chinese Journal of Pharmaceuticals
关键词
米诺膦酸
抗骨质疏松药
合成
minodronic acid
anti-osteoporosis agent
synthesis
