氟伐他汀钠的合成工艺研究
The Synthesis Process Research of Fluvastatin Sodium
摘要: 本文根据我国心脑血管疾病的增加和人口老龄化的到来,引出调血脂观念的重要性,从而介绍降血脂药物氟伐他汀钠,进而对氟伐他汀钠的合成工艺进行了全面的研究和探索。得出第四种合成工艺是最佳的,适合工业化大生产,可以开发出高效的内部合成工艺,值得推广,并给出了某些良好的建议。 According to the increasing of cardiovascular disease and the coming of aging population in our country, draws out the importance of lipid regulators, so as to introduce Fluvastatin sodium of lipid-lowering drugs, and carries on comprehensive research and exploration Fluvastatin sodium of synthesis routes. Because of it’s for industrial pro-duction and development of effective internal synthetic process, the fourth synthetic process is the best. And some good advice are be gived.
文章引用:李玉龙, 刘菊. 氟伐他汀钠的合成工艺研究[J]. 药物资讯, 2012, 1(1): 1-5. http://dx.doi.org/10.12677/PI.2012.11001

参考文献

[1] 陈宇瑛. 辛伐他汀的研究[J]. 精细与专用化学品, 2003, 10: 16-18.
[2] 陈碧珊, 苏丽华. 他汀类药物的研究进展[J]. 中国药房, 2005, 16(7): 545-546.
[3] 秦永忠. 辛伐他汀的研究[D]. 山东大学, 2005.
[4] 章飞风. 氟伐他汀的研究进展[J]. 中国实用医药, 2007, 2(34): 139-141.
[5] 蔡正艳, 宁奇, 周伟澄. HMG-CoA还原酶抑制剂的合成(上) [J]. 中国医药工业杂志, 2004, 35(10): 621-626.
[6] K. M. Chen, G. E. Hardtmann, G. T. Lee, et al. Preparation of olefinic compounds. EP: 244364, 1987. (CA 1987, 108: 131038)
[7] 蔡正艳, 宁奇, 周伟澄. HMG-CoA还原酶抑制剂的合成[J]. 中国医药工业杂志, 2004, 35(11): 687-691.
[8] P. K. Kapa. 6-substituted-4-hydroxytetrahydropyran-2-ones. US: 4571428, 1986. (CA 1986, 105: 60752)
[9] T. Honda, S. Ono, H. Mizutani, et al. Enantioselective synthesis of the lactone moiety of HMG-CoA reduc-tase inhibitors: Stereoselective synthesis of (+)-(4R,6R)-4-hydroxy-6-(2-phenylethyl)- tetrahydro-2H-pyran-2-one. Tetrahedron: Asymmetry, 1997, 8(2): 181-184.
[10] J. R. Wareing. (Tetrahydropyran-2-yl)aldehydes. US: 4474971, 1984. (CA 1984, 102: 95474)
[11] European Patent Application 1990: 363934. (CA 1990, 113: 131998)
[12] 杜鹃, 康宏杰. 氟伐他汀钠合成路线图解[J]. 中国医药工业杂志, 1996, 27(10): 478-480.
[13] 蔡正艳, 宁奇, 周伟澄. 氟伐他汀钠的合成[J]. 中国医药工业杂志, 2007, 38(2): 73-75.
[14] 金红日, 陈晓芳, 阎启东, 杨美玲. 氟伐他汀钠的合成[J]. 合成化学, 2008, 16(3): 358-361.
[15] 樊刚. 氟伐他汀钠的合成及中试工艺研究[D]. 华东理工大学, 2008.
[16] O. Repic, K. Prasad and G. T. Lee. The story of Lescol: From research to production. Or-ganic Process Research and Develop- ment, 2001, 5(5): 519-527.