摘要
目的研究雷尼酸锶的化学合成。方法以枸橼酸为起始原料,经过脱羧、酯化、环合、烷基化、水解成盐等多步反应生成终产物雷尼酸锶。结果雷尼酸锶的结构经IR,1H-NMR,13C-NMR得到证实,总产率约为42.6%。结论本合成路线操作简单、成本低,适合工业化生产。
Abstract
OBJECTIVE To study the synthesis route of strontium ranelate,an antiosteoporosis drug.METHODS Strontium ranelate was synthesized from citric acid via decarboxylation,esterification,cyclization,alkylation,hydrolysis and salification.RESULTS The structure of strontium ranelate was confirmed by IR,1H-NMR,13C-NMR,the total yield was 42.6% approximately.CONCLUSION The synthesis route was simple,low cost and could be used in industry.
关键词
雷尼酸锶 /
合成 /
骨质疏松
{{custom_keyword}} /
Key words
strontium ranelate /
synthesis /
osteoporosis
{{custom_keyword}} /
丁翔宇;蒋晔;贾湘曼;刘丰华.
抗骨质疏松药雷尼酸锶的合成[J]. 中国药学杂志, 2008, 43(11): 874-876
DING Xing-yu;JING Ye;JI Xing-mn;LIU Feng-hu.
Synthesis of Strontium Ranelate,an Antiosteoporosis Drug [J]. Chinese Pharmaceutical Journal, 2008, 43(11): 874-876
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
参考文献
[1] IMANISHI Y，NISHIZAWA Y. Strontium ranelate as new therapeutic agent for osteoporosis[J] .Clin Calcium，2005，15(1)：25-33.
[2] WIERZBICKI M，BONNET J，BRISSET M，et al. Bivalent metal salts of 2-[N，N-di(carboxymethyl)aminol] -3-cyano-4-carboxymethylthiophene-5-carbox-ythiopheneacidprocess for their preparation and pharmaceutical compsns： US 5128367[P] . 1990-8-31.
[3] MICHEL W，DENISE C，PAUL C. Appliationla synth se de quelques thiéno [2，3-b] pyrroles [J] .Bull Soc Chim Fr，1975(7-8)：1786-1792.
[4] VAYSSE L L，LECOUVE J P，LANGLOIS P. New process for industrial synthesis of strontium ranelate and its hydrates： FR 200211763[P] .2002-09-24.
[5] FANG N T. Events of Organic Synthesis(有机合成事典)[M] . Beijing： Institute of Technology Press，1992：341-342.
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}
