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非布索坦合成路线图解 被引量：10

Graphical Synthetic Routes of Febuxostat
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摘要 非布索坦（febuxostat，1），化学名为2-[3-氰基-4-（2-甲基丙氧基）苯基]-4-甲基-5-噻唑甲酸，是日本Teijin公司研发的新型非嘌呤类黄嘌呤氧化酶选择性抑制剂，2008年5月在欧盟批准上市，商品名Adenuric；2009年2月由美国FDA批准上市，商品名Uloric。本品可降低体内的尿酸水平，临床主治高尿酸血症和痛风。
作者 孙运强 王玉玲 周辛波 李松 郑志兵
机构地区 沈阳药科大学制药工程学院 军事医学科学院毒物药物研究所
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2009年第12期954-956,共3页 Chinese Journal of Pharmaceuticals
关键词 合成路线图解 布索 黄嘌呤氧化酶 选择性抑制剂 批准上市 尿酸血症 美国FDA 商品名
分类号 TQ464.7 [化学工程—制药化工] TU323 [建筑科学—结构工程]
  • 相关文献

参考文献15

  • 1Pascual E, Sivera F, Yasothan U, et al. Febuxostat [J]. Nat Rev Drug Discov, 2009, 8(3): 191-192.
  • 2Perez-Ruiz F, Dalbeth N, Schlesinger N. Febuxostat, a novel drug for the treatment of hyperuricemia of gout [J]. Future Rheumatol, 2008, 3 (5) : 421-427.
  • 3Kondo S, Fukushima H, Hasegawa M, et al. 2-Arylthiazole derivative and pharmaceutical composition containing the same: WO, 9209279[P]. 1992-06-11. (CA 1993, 118: 38915).
  • 4Sorbera LA, Revel L, Rabasseda X, et al. TMX-67: treatment of gout and hyperuricemia xanthine oxidase inhibitor [J]. Drugs Future, 2001, 26 (1) : 32-38.
  • 5武瑊,王春辉,李松,郑志兵.抗痛风药物febuxostat的合成[J].中国药物化学杂志,2008,18(4):259-262. 被引量：12
  • 6冯明声,曹于平,韩爱霞,姚其正.2-(3-氰基-4-异丁氧基苯基)-4-甲基-5-噻唑甲酸的合成[J].中国新药杂志,2009,18(11):1066-1069. 被引量：10
  • 7Watanabe K, Tanaka T, Kondo S, et al. Preparation of phenylthiazoles as pharmaceuticals: JP, 06329647 EP]. 1994-11-29. (CA 1995, 122: 214062).
  • 8Watanabe K, Yarino T, Hiramatsu T. Preparation of 2-(4-alkoxy-3-cyanophenyl) thiazoles as xanthine oxidase inhibitors: JP, 10045733 [P]. 1998-02-17. (CA 1998, 128: 180409).
  • 9Hiramatsu T, Yarino T, Watanabe K. Preparation of formylhydroxyphenylthiazoles as intermediates for pharmaceuticals having xanthine oxidase inhibitory activity: JP, 09188670 [P]. 1997-07-22. (CA 1997, 127: 190732).
  • 10Minoshima T, Hiramatsu T. Preparation of 2-(3-cyanophenyl) thiazoles as pharmaceuticals for treatment of gout and hyperuricemia: JP, 10139770 [J]. 1998-05-26. (CA 1998, 129: 54365).

二级参考文献27

  • 1张媛.抗痛风药Febuxostat[J].药学进展,2005,29(3):141-142. 被引量：8
  • 2YAMAMOTO T. Development of antihyperuricemic candidates[J]. Nippon Rinsho, 2003, 61 ( S1 ) : 209 - 212.
  • 3TAKANO Y, HASE-AOKI K, HORIUCHI H, et al. Selectivity of febuxostat, a novel nonpurine inhibitor of xanthine oxldase/xanthine dehydyogenase[J]. Life Sci, 2005, 76(16) : 1835 - 1847.
  • 4BECKER M A, SCHUMACHER H R Jr, WORTMANN R L. Febuxostat compared with aUopurinol in patients with hyperurlcemia and gout [ J ]. N Engl J IVied, 2005, 353(23) :2450 - 2461.
  • 5BECKER M A, SCHUMACHER H R Jr, WORTMANN R L. Febuxostat, a novel nonpurine selective inhibitor of xanthine oxidase: a 28-day, multicenter, phase Ⅱ, randomized, double-blind, placebo controlled dose-response clinical trial examining safety and efficacy in patients with gout [ J ]. Arthritis Rheum, 2005, 52(3) :916 - 923.
  • 6POHAR S, MURPHY G. Febuxostat for prevention of gout attacks [ J ]. Issues Emerg Health Technol, 2006, 87(8) : 1 - 4.
  • 7TAYLOR W :j, SCHUMACHER H R :Jr. Assessment of outcome in clinical trials of gout-a review of current measures [ :J ]. Rheumatology, 2007, 46 ( 12 ) : 1751 - 1756.
  • 8BRYAN T, EMMERSON M D. The treatment of gout[J]. Drug Ther, 1996, 334(7) : 445 - 451.
  • 9VERGE J P, ROFFEY P. Antiprotozoal thiazoles. 2- (5-nitro-2-thienyl)-thiazoles[J] .J Med Chem, 1975, 18(8) :794.
  • 10HE H M, CUSHMAN M. A versatile synthesis of 2- methoxyestradiol, an endogenous metabolite of estradiol which inhibits tubulin polymerization by binding to the colchicine binding site [ J ]. Bioorg Med Chem Lett, 1994, 4 (14) : 1725 - 1728.

共引文献29

同被引文献55

  • 1张媛.抗痛风药Febuxostat[J].药学进展,2005,29(3):141-142. 被引量：8
  • 2聂淑芳,潘卫三,杨星钢,刘宏飞,刘志东.对大鼠在体肠单向灌流技术中重量法的评价[J].中国新药杂志,2005,14(10):1176-1179. 被引量：90
  • 3刘太明,蒋学华.黄芩苷和黄芩素大鼠在体胃、肠的吸收动力学研究[J].中国中药杂志,2006,31(12):999-1001. 被引量：79
  • 4Hasegawa M, Komoriya K. Cyano compound and its production: JP6345724[P]. 1994-12-20.
  • 5Kitamura M. Method of producing polymorphic crystal of 2-(3- cyanl-4- isobutyloxyphenyl) -4-methyl-5-thiazolecarboxylic acid: JP2003261548[P]. 2003-09-19.
  • 6Pascual E, Sivera F, Yasothan U, et al. Febuxostat. Nat Rev Drug Discov, 2009,8(3) : 191-192.
  • 7Vanderhoff J. Carrying out chemical reactionsusing microwaveenergy[P]. US:3432413,1969 -03 - 11.
  • 8Gedye R,Smith F,Westaway K,et al. The uses of microwave ovensfor rapid organic synthesis [J], Tetrahedron Letters,1986,27 ( 3 ):279 -282.
  • 9Castaldi G,A process for the preparation of febuxostat[P]. EP:2010142653,2010-12-16.
  • 10Ren Y,Liu Z,He Sfet al. Development of an open-air and robustmethod for large-scale palladium-catalyzed cyanation of arylhalides : the use of i-PrOH to prevent catalyst poisoning by oxygen[J]. Organic Process Research & Development,2009,13(4) :764-768.

引证文献10

二级引证文献20

中国医药工业杂志
2009年 第12期

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