Synthesis of risedronate sodium

ZHANG Xiu-li; ZHANG Yu-jia; WANG Lu-lu; FANG Xia-qin; CHEN Shao-hua; XIANG Li; LIU Meng-meng; ZHENG Wen-sheng

doi:10.3969/j.issn.1006-0111.2013.06.014

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Volume 31 Issue 6

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Article Navigation > Journal of Pharmaceutical Practice and Service > 2013 > 31(6): 448-450

ZHANG Xiu-li, ZHANG Yu-jia, WANG Lu-lu, FANG Xia-qin, CHEN Shao-hua, XIANG Li, LIU Meng-meng, ZHENG Wen-sheng. Synthesis of risedronate sodium[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(6): 448-450. doi: 10.3969/j.issn.1006-0111.2013.06.014

Citation:

ZHANG Xiu-li, ZHANG Yu-jia, WANG Lu-lu, FANG Xia-qin, CHEN Shao-hua, XIANG Li, LIU Meng-meng, ZHENG Wen-sheng. Synthesis of risedronate sodium[J]. Journal of Pharmaceutical Practice and Service, 2013, 31(6): 448-450. doi: 10.3969/j.issn.1006-0111.2013.06.014

Synthesis of risedronate sodium

doi: 10.3969/j.issn.1006-0111.2013.06.014

Institute of Materia Medica, Chinese Academy of Medical Sciences, Beijing City Key Laboratory of Drug Delivery Technology and Novel Formulations, Beijing 100050, China

Received Date: 2012-12-27
Rev Recd Date: 2013-05-20

Abstract

Objective To synthesis the new anti-osteoporotic risedronate sodium. Methods Nicotinic acid was used as raw material, by esterification, condensation, Willgerodt reaction and hydrolysis steps to get the key intermediate 3-pyridine acetic acid hydrochloride.Then 3-pyridine acetic acid hydrochloride and phosphorous acid reacted to obtain the risedronate sodium. Results The reaction time, reaction conditions and the yield of Willgerodt reaction were explored. The synthetic route was optimized and the total yield of the reactions was increased. Conclusion This synthetic route of risedronate sodium could be applied to industrial production.
- risedronate sodium,
- anti-osteoporotic,
- chemical synthesis

References

[1]	杜蕾, 马培奇. 第三代双磷酸盐类药物利塞膦酸钠[J]. 中国医药情报, 2000, 6(3):1.
[2]	郑珩. 治疗骨质疏松症新药Risedronate Sodium[J]. 药学进展, 1999, 23(3):181.
[3]	Soc Pour Lind Chim àB1e. Heterocyclic substituted fatty acids and their amide[P]. BP, 558774, 1944-01-20.
[4]	王华, 李云, 尤启冬, 等. 3-吡啶乙酸盐酸盐的合成[J]. 中国新药杂志, 2004, 13(3):245.
[5]	Wieczorek M, Stawinski T, Chrulski K. A process for the preparation of risedronic acid[P]. EP, 1243592, 2002-09-25.

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通讯作者: 陈斌, [email protected]

1.
沈阳化工大学材料科学与工程学院沈阳 110142

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