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(6S)2,6-二氨基-4,5,6,7-四氢苯并噻唑的制备 被引量:1

Preparation of(6S)2,6-Diamino-4,5,6,7-tetrahydrobenzothiazole
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摘要 以2-氨基-6-乙酰氨基-4,5,6,7-四氢苯并噻唑氢溴酸盐为原料,经过水解反应除去乙酰基,然后用L(+)酒石酸成盐、解析拆分后合成了制备普拉克索的重要中间体-(-)-(6S)2,6-二氨基-4,5,6,7-四氢苯并噻唑,总收率>75%,并对合成产物进行1H NMR、IR表征分析。 (-)-(6S)2,6-Diamino-4,5,6,7-tetrahydrobenzothiazole,an important chiral intermediate for Pramipexole which is a non-ergoline dopamine agonist,was prepared from 2-amino-6-acetamido-4,5,6,7-tetrahydrobenzothiazole hydrobromide and resolved with L(+)tartaric acid.The title compound was obtained in an overall yield of 75% and its structure was confirmed with 1H NMR and IR.
出处 《精细化工中间体》 CAS 2011年第6期21-23,共3页 Fine Chemical Intermediates
基金 湖北省高校产学研合作重点项目[鄂教科2009(6)]
关键词 四氢苯并噻唑 手性化合物 水解反应 合成工艺 tetrahydrobenzothiazole chiral compound hydrolysis synthesis process
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  • 1Maggio R, Scarselli M, Novi F, et al. Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole [J]. J Neurochem, 2003,87 (3) :631-641.
  • 2Okura T, Ito T, Ishiguro N, et al. Blood-brain barrier transport of pramipexole, a dopamine D2 agonist [J]. Life Sciences, 2007,80 (17) : 1564-1571.
  • 3Parkison Study Group. Pramipexole vs levodopa as initial treatment for Parkinson disease: a randomized controlled trial. Parkinson Study Group [J]. JAMA, 2000,284(15):1931-198.
  • 4Noyes K, Dick A W, Holloway R G. Pramipexole versus levodopa in patients with early Parkinson's disease: effect on generic and disease-specific quality of life [ J ]. Value Health, 2006,9 ( 1 ) : 28- 38.
  • 5Constantinescu R, Romer M, McDermott M P, et al. Impact of pramipexole on the onset of levodopa-related dyskinesias[J]. Mov Disord, 2007,22(9) : 1317-1319.
  • 6Parkison Study Group. Pramipexole in levodopa-treated Parkinson disease patients of African, Asian, and Hispanic heritage[J]. Clin Neuropharmacol, 2007,30(2) :72-85.
  • 7Moller J C, Oertel W H, Koster J, et al. Long-term efficacy and safety of pramipexole in advanced Parkinson's disease: results from a European multicenter trial [ J ]. Mov Disord, 2005,20 (5) : 602- 610.
  • 8Weiner W J, Factor S A, Jankovic J, et al. The long-term safety and efficacy of pramipexole in advanced Parkinson's disease [J]. Parkinsonism Relat Disord, 2001,7(2) : 115-120.
  • 9Zanettini R, Antonini A, Gatto G, et al. Valvular Heart Disease and the Use of Dopamine Agonists for Parkiuson's Disease [J]. N Engl J Med, 2007,356( 1 ) : 39-46.
  • 10Linazasoro G. Conversion from dopamine agonists to pramipexole. An open-label trial in 227 patients with advanced Parkinson's disease [ J ]. J Neurol, 2004,251 (3) : 335-339.

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  • 1詹静.抗帕金森氏症药物普拉克索的合成[D].上海:华东理工大学.2006.
  • 2Bennett J P, Piercey M F. Pramipexole: a new dopamine agonist for the treatment of parkinson's disease[J]. J N eurol Sci,1999,163( 1 ):25 -26.
  • 3J GerhartGriss, RudoffHumaus, et al. Tetrahydro- benzthlazoles, the preparation Thereof and their use as intermediate Products or as Pharmaceuticals[P]. US, 4886812, 1989 - 12 - 12.
  • 4Pospisilik Karel, Hoorn Hansjanetal. Process for preparation of 2 - amino - 6 - (alkyl) ajmino - 4, 5,6,7 - tetrahydobenzothiazole and compounds therefor[ P] : US, 0103240, 2001 -9 -1.
  • 5Claus S, Schneider, et al. Dopamine Autoreceptor Agonists:Resolution and Pharmacological Activity of 2, 6 -Dlaminotetrahy- drobenzothiazole and an Alninothiazole Analogue of Apo - morphine [J]. J. Med. Chem. 1987,30:494 -498.
  • 6宫庆创,司志现.一种普拉克索及其二盐酸盐-水合物的工业化制备方法[P].中国,1024429-72A,2012-5-9.
  • 7Balicki R, Ciesielska A. A new method for preparing (S) - ( - ) - 2 - amino - 6 - n - propylamino - 4, 5,6, 7 - tetrahydrobenzothiazofe (pramipexal) dihydrochloride monohydrate [ J ]. Przemysl chemiczny, 2006,85 ( 5 ) : 344 - 346.
  • 8杨宇.普拉克索治疗帕金森病的疗效分析与评价[J].临床合理用药杂志,2011,4(05X):37-38. 被引量:23
  • 9金华,李建其.盐酸普拉克索的合成研究[J].中国药物化学杂志,2011,21(6):430-432. 被引量:8

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