CAS: 5638-76-6; Betahistine

该化合物是一种类同类类胺,主要用于治疗甲状腺病,它作为血管调节器发挥作用,改善内耳的血液流,有助于缓解脊椎和等症状.乙酸丁作为H1受体的选择性激动剂和H3受体的对抗剂,影响...

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2-vinylpyridine methylamine hydr°Chloride 2-(2-Hydroxyethyl)pyridine methylamine acetate -1,2-cyclohexanediaminetrans-(+/-)-N,N'-Dimethyl-N-2-(2-pyridyl)ethyl-1,2-cyclohexanediamine -(2-pyridyl)ethylamineN-Methyl-N-2-(4-pyridyl)ethyl-(2-pyridyl)ethylamine carbonyl>propionatebenzyl (2R)-2-benzyl-3-(2-pyridin-2-ylethyl)methylamin°Carbonylpropionate sulfonyl>propionatemethyl 2-benzyl-3-(2-pyridin-2-ylethyl)methylaminosulfonylpropionate

合成工艺路线路线简述

  • 合成目标产物 Betahistine 主要起始原料 2-Vinylpyridine And Methylamine Hydrochloride
  • (文献来源)合成步骤主要原料 2-Vinylpyridine 和 Methylamine Hydrochloride
📜Magnesium Stearate 反应生成 2-(2-甲基氨基乙基)吡啶
参考文献:Pharmaceutical Combination Of Betahistine And Trimetazidine
标题:Pharmaceutical Combination Of Betahistine And Trimetazidine
摘要:这项发明涉及贝他组胺或其药用可接受盐和三甲嗪或其药用可接受盐的药物组合.

海关参考信息

专利信息


专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-10865390-B2
优先权日:2018-02-12
标 题 :Alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols
发明人:NI YE; ZHOU JIEYU; XU GUOCHAO; WANG YUE
权利人:UNIV JIANGNAN
摘要:The present disclosure discloses an alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant of the present disclosure has excellent catalytic activity and stereoselectivity, and may efficiently catalyze the preparation of a series of chiral diaryl alcohols in R- and S-configurations. By coupling alcohol dehydrogenase of the present disclosure to glucose dehydrogenase or formate dehydrogenase, the synthesis of chiral diaryl alcohol intermediates of various antihistamines may be achieved. Compared with the prior art, a method for preparing diaryl chiral alcohols through asymmetric catalytic reduction using the alcohol dehydrogenase of the present disclosure has the advantages of simple and convenient operation, high substrate concentration, complete reaction and high product purity, and has great industrial application prospects.

专利号:US-10822593-B2
优先权日:2018-02-12
标 题:Alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols
发明人:NI YE; ZHOU JIEYU; XU GUOCHAO; WANG YUE
权利人:UNIV JIANGNAN
摘要:The present disclosure discloses an alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant of the present disclosure has excellent catalytic activity and stereoselectivity, and may efficiently catalyze the preparation of a series of chiral diaryl alcohols in R- and S-configurations. By coupling alcohol dehydrogenase of the present disclosure to glucose dehydrogenase or formate dehydrogenase, the synthesis of chiral diaryl alcohol intermediates of various antihistamines may be achieved. Compared with the prior art, a method for preparing diaryl chiral alcohols through asymmetric catalytic reduction using the alcohol dehydrogenase of the present disclosure has the advantages of simple and convenient operation, high substrate concentration, complete reaction and high product purity, and has great industrial application prospects.

专利号:US-11078465-B2
优先权日:2018-02-12
标题:Alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols
发明人:NI YE; WANG YUE; DAI WEI; XU GUOCHAO; ZHOU JIEYU
权利人:UNIV JIANGNAN
摘要:The present disclosure discloses an alcohol dehydrogenase mutant and application thereof in synthesis of diaryl chiral alcohols, and belongs to the technical field of bioengineering. The alcohol dehydrogenase mutant of the present disclosure has excellent catalytic activity and stereoselectivity, and may efficiently catalyze the preparation of a series of chiral diaryl alcohols in R- and S-configurations. By coupling alcohol dehydrogenase of the present disclosure to glucose dehydrogenase or formate dehydrogenase, the synthesis of chiral diaryl alcohol intermediates of various antihistamines may be achieved. Compared with the prior art, a method for preparing diaryl chiral alcohols through asymmetric catalytic reduction using the alcohol dehydrogenase of the present disclosure has the advantages of simple and convenient operation, high substrate concentration, complete reaction and high product purity, and has great industrial application prospects.

专利号:US-11912647-B2
优先权日:2020-05-22
标 题:Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation
发明人:CRICH DAVID; HETTIKANKANAMALAGE ASIRI; HILL JARVIS
权利人:UNIV GEORGIA
摘要:In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

专利号:US-8735586-B2
优先权日:2007-06-26
标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles
发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR
权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA
摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.

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主要参考文献


1: Albu S, Nagy A, Doros C, Marceanu L, Cozma S, Musat G, Trabalzini F. Treatment of Meniere's disease with intratympanic dexamethazone plus high dosage of betahistine. Am J Otolaryngol. 2016 May-Jun;37(3):225-30. doi: 10.1016/j.amjoto.2015.12.007. Epub 2015 Dec 30. doi: 10.1097/JCP.0000000000000489. Epub 2016 Jan 18.
5: Lian J, Huang XF, Pai N, Deng C. Ameliorating antipsychotic-induced weight gain by betahistine: Mechanisms and clinical implications. Pharmacol Res. 2016 Apr;106:51-63. doi: 10.1016/j.phrs.2016.02.011. Epub 2016 Feb 15. Review. doi: 10.1177/0269881115626349. Epub 2016 Feb 2. Efficacy and safety of betahistine treatment in patients with Meniere's disease: primary results of a long term, multicentre, double blind, randomised, placebo controlled, dose defining trial (BEMED trial). BMJ. 2016 Jan 21;352:h6816. doi: 10.1136/bmj.h6816.
9: Harcourt J, Cosentino S. Betahistine for Meniere's disease. BMJ. 2016 Jan 21;352:i46. doi: 10.1136/bmj.i46. doi: 10.3109/00016489.2015.1072873. Epub 2015 Aug 6. doi: 10.5152/iao.2015.368. doi: 10.1016/j.phrs.2015.07.023. Epub 2015 Jul 26. doi: 10.1159/000368293. Epub 2015 Jun 27. doi: 10.1185/03007995.2015.1067193. Epub 2015 Sep 16. doi: 10.1002/bdd.1955. Epub 2015 May 22. Review.

合成参考文献


参考文献:10.2165/11530130-000000000-00000
摘要:Hasnain M, Vieweg WV, Fredrickson SK. Metformin for atypical antipsychotic-induced weight gain and glucose metabolism dysregulation: review of the literature and clinical suggestions. CNS Drugs. 2010 Mar;24(3):193–206. doi: 10.2165/11530130-000000000-00000.
参考文献:10.3109/10837450.2011.557730
摘要:Shamma RN, Basalious EB, Shoukri R. Development of novel sustained release matrix pellets of betahistine dihydrochloride: effect of lipophilic surfactants and co-surfactants. Pharmaceutical Development and Technology. 2011 Jul 19;17(5):583–93. doi: 10.3109/10837450.2011.557730.
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