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比拉斯汀的合成 被引量：2

Synthesis of Bilastine
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摘要 α,α-二甲基苯乙酸甲酯（2）经傅-克酰基化和还原反应制得α,α-二甲基-4-（2-溴乙基）苯乙酸甲酯,依次与2-（4-哌啶基）-1H-苯并咪唑和2-氯乙基乙醚发生亲核取代反应后,水解得比拉斯汀,总收率约54%（以2计）。 Bilastine was prepared from methyl α,α-dimethylphenylacetate （2） via Friedel-Crafts acylation and reduction to give methyl α,α-dimethyl-4- （2-bromoethyl） phenylacetate, which was subjected to nucleophilic substitution with 2-（piperidin-4-yl）-1H-benzimidazole and 2-chloroethyl ether followed by hydrolysis with an overall yield about 54% （based on compound 2）.
作者 孔昊 耿海明 梅玉丹 朱晓琦 孙平华
机构地区 暨南大学药学院 远大医药(中国)有限公司
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2015年第7期677-679,共3页 Chinese Journal of Pharmaceuticals
基金 中山科技计划项目(2012cxy020) 中央高校基本科研基金项目(21615428)
关键词 比拉斯汀 组胺H1受体拮抗药 合成 bilastine histamine H1 receptor antagonist synthesis
分类号 R987 [医药卫生—药品]
  • 相关文献

参考文献9

  • 1Corc6stegui R, Labeaga L, Innerrity A, et al. Preclinical pharmacology of bilastine, a new selective histamine Hl receptor antagonist: receptor selectivity and in vitro anti- histaminic activity [J]. Drugs R D, 2005, 6 (6) : 371-384.
  • 2Carter NJ. Bilastine: in allergic rhinitis and urticaria [J]. Drugs, 2012, 72(9): 1257-1269.
  • 3Sadaba B, Azanza JR, Rodil R, et al. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria [J]. Ther Clin RiskManag, 2013, 9: 197-205.
  • 4Orjales A, Rubio V, Bordell M. Benzimidazole derivatives with antihistaminic activity: EP, 0818454 [P]. 1998-01-14.
  • 5Orjales-Venero A, Rubio-Royo V. New piperidine derivatives of benzimidazole as antihistaminic and antiallergic agents: EP, 0580541 [P]. 1994-01-26.
  • 6Collier S J, Wu X, Poh Z, et al. Alternative synthesis of bilastine [J]. Synth Commun, 2011, 41 (9) : 1394-1402.
  • 7Lee CH, Khoo JH, Kwon KC, et al. Process for preparation of 2-methyl-2-phenylpropionic acid derivatives and novel intermediate compounds: WO, 2009102155 [P]. 2009-02-12.
  • 8王蕾,李科,王倩,等.2-(4-卤乙基)苯基-2-甲基丙酸酯的制备方法及合成比拉斯汀的方法:中国.102675101[P].2012-09-19.
  • 9Matsumoto N, Kohno T, Uchida S, et al. Preparation of antibodies against a novel immunosuppressant FTY720, and development of an enzyme immunoassay for FTY720 [J]. Bioorg Med Chem, 2006, 14 (12) : 4182-4192.

同被引文献12

  • 1Corc6stegui R, Labeaga L, Inner_hrity A, et al. Preclinical pharmacology of bilastine, a new selective histamine H receptor antagonist: receptor selectivity and in vitro anti- histaminic activity [J]. Drugs R D, 2005, 6 (6) : 371--384.
  • 2Carter NJ. Bilastine: in allergic rhinitis and urticaria [J]. Drugs, 2012, 72(9): 1257--1269.
  • 3Sadaba B, Azanza JR, Gomez-Guiu A, et al. Critical appraisal of bilastine for the treatment of allergic rhinoconjunctivitis and urticaria [J]. Ther Clin Risk Manag, 2013, 9(4) : 197--205.
  • 4梅开忠,黄欣.比拉斯汀化合物及其制备方法:中国,104530002[P].2015-04.22.
  • 5Orjales A, Rubio V, Bordell M. Benzimidazole derivatives with antihistaminic activity: EP, 0818454 [P]. 1998-01-14.
  • 6Orjales-Venero A, Rubio-Royo V. New piperidine derivatives of benzimidazole as antihistaminic and antiaUergic agents: EP, 0580541 [P]. 1994-01-26.
  • 7Collier SJ, Wu X, Poh Z, et al. Alternative synthesis of bilastine [J]. Synth Commun, 2011, 41 (9): 1394--1402.
  • 8王蕾,李科,王倩,等.2-(4-卤乙基)苯基.2.甲基丙酸酯的制备方法及合成比拉斯汀的方法:中国,102675101[P].2012-09-19.
  • 9Lee CH, Khoo JH, Kwon KC, et al. Process for preparation of 2-methyl-2'-phenylpropionic acid derivatives and novel intermediate compounds: WO, 2009102155 [P]. 2009-08-20.
  • 10刘晓庆,邢爱敏.组胺H_1受体拮抗剂比拉斯汀[J].药学进展,2010,34(7):331-333. 被引量：4

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中国医药工业杂志
2015年 第7期

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