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阿立哌唑的合成 被引量：5

Synthesis of Aripiprazole
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摘要 4-(2,3-二氯苯基)-1-哌嗪盐酸盐与1,4-二溴丁烷缩合得到1-(4-溴丁基)-4-(2,3-二氯苯基)哌嗪,再与3-氯-N-(3-羟基苯基)丙酰胺反应得3-氯-N-[3-[4-[4-(2,3-二氯苯基)]-1-哌嗪基]丁氧基]苯丙酰胺,最后经闭环制得阿立哌唑,总收率25%。 Aripiprazole was synthesized from 4- （2,3-dichlorophenyl） - 1-piperazine hydrochloride and 1,4-dibrombutane by condensation to give 1- （4-brombutyl） -4 （2,3-dichlorophenyl） piperazine, which was subjected to condensation with 3- chloro-N- （3-hydroxyphenyl） propionamide to give 3-chloro-N- [3- [4- [4- （2,3-dichlorophenyl） ] - 1-piperazinyl] butoxy] - phenylpropionamide followed by cyclization with an overall yield of 25 %.
作者 张桂森 朱永超 马彦琴
机构地区 江苏徐州恩华药业集团技术中心 天津大学化工学院
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2006年第10期655-656,共2页 Chinese Journal of Pharmaceuticals
关键词 阿立哌唑 抗精神病药 合成 aripiprazole antipsychosis synthesis
分类号 R971.43 [医药卫生—药品]
  • 相关文献

参考文献9

  • 1张璞,李中东,焦正.第二代非典型抗精神病药——阿立哌唑[J].中国药学杂志,2005,40(3):238-240. 被引量：59
  • 2Yasuo O,Seiji S.Carbostyril derivatives[P].US:5006528,1991-04-09.(CA 1990,113:152468)
  • 3Tsujimori H,Takaoka K,Fujioka T,et al.Benzenesulfonate compounds[P].JP:2002193915,2002-07-10.(CA 2002,137:78764)
  • 4Yasuo O,Seiji S,Kurahashi N,et al.Novel antipsychotic agents with dopamine autoreceptor agonist properties:synthesis and pharmacology of 7-[4-(4-phenyl-l-piperazinyl) butoxy] -3,4-dihydro-2 (1 H) -quinolinone derivatives[J].J Med Chem,1998,41 (5):658-667.
  • 5Salama P,Meunier JF,Lafreniere J.Process for the preparation of carbostyril derivatives,such as aripiprazole and its intermediates[P].WO:2004099152,2004-11-18.(CA 2004,141:424212)
  • 6张庆文,许艳艳,时惠麟.1H-喹啉-2-酮化合物的制备方法[P].CN:02150807,2002-11-28.
  • 7王军玲,贾湘曼,鲍春和,陈子明,蒋晔.阿立哌唑的合成[J].中国医药工业杂志,2004,35(12):707-708. 被引量：10
  • 8Allen CFH,Gates JW.Organic Sytheses[M].vol 25,New York:John Wiley,1945.9.
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二级参考文献14

  • 1Butini S, Campiani G, Angelis MD, et al. Novel antipsychotic agents:recent advances in the drug treatment of schizophrenia [J].Expert Opinion on Therapeutic Patents, 2003, 13(4): 425.
  • 2Marder SR, McQuade RD, Stock E, et al. Aripiprazole in the treatment of schizophrenia: safety and tolerability in short-term, placebocontrolled trials [J]. Schizophr Res, 2003, 61 (2～3):123.
  • 3Bowles TM, Levin GM. Aripiprazole: a new atypical antipsychotic drug[J]. Ann Pharmacother, 2003, 37(5): 687.
  • 4Bristol-Myers Squibb Company. ABILIFY (aripiprazole) Tablets[EB/OL]. http://www.bms.com/cgi-bin/anybin.pl? sql = select％20PPI％ 20from％ 20TB_PRODUCT_PPI％ 20where％ 20PPI_SEQ =101&key = PPI, 2002-11-15/2003-07-17.
  • 5Keck Jr, McElroy SL. Aripiprazole: a partial dopamine D2 receptor agonist antipsychotic[J]. Expert Opin Investig Drugs, 2003, 12 (4):655.
  • 6Goodnick PJ, Jerry JM. Aripiprazole: profile on efficacy and safety [J]. Expert Opin Pharmacother, 2002, 3(12): 1773.
  • 7Marcus R, Gharbia NA, Kujawa MJ, et al. Aripiprazole for longterm maintenance treatment of schizophrenia [A]. The 2002 annual meeting of the American College of Clinical Pharmacy [C], Albuquerque, New Mexico, Sage Science press, October 20～ 23, 2002.
  • 8Carson W, Pigott T, Saha A, et al. Aripiprazole vs placebo in the treatment of stable, chronic schizophrenia [A] . The 42nd annual meeting of the New Clinical Drug Evaluation Unit[C], Boca Raton,Florida, The National Institute of Mental Health,June 10 ～ 13, 2002.
  • 9Petrias JM, McQuade RD, Cassey DE, et al. Switch to aripiprazole monotherapy[A]. The 2002 annual meeting of the American College of Clinical Pharmacy[C], Albuquerque, New Mexico, Sage Science Press, October 20～23, 2002.
  • 10Kern RS, Cornblatt B, Carson WH, et al. An open-label comparison of the neurocognitive effects of aripiprazole vs. olanzapine in patients with stable psychosis [J]. Schizophr Res, 2001, 49 (Suppl 1～2):S234.

共引文献64

同被引文献38

引证文献5

二级引证文献8

中国医药工业杂志
2006年 第10期

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