CAS: 57475-17-9; Brovincamine

该化合物是一种合成化合物,被归类为一种代孕,主要用于增进认知性,以其改善大脑血液流动和增强认知功能的能力著称,使它对治疗痴呆症和认知下降等状况感兴趣;该物质作为血管止血器,促进大脑血液循环的增加,从而可以改善向...

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    methanol (+)-11-bromo-14-epivincamine vincamin

    合成工艺路线路线简述

      📜(+)-3(S),17(S)-11-Bromo-14-Oxo-15-Hydroxyimino-E-Homo-Eburnane Hydrochloride置于聚合甲醛,Potassium Tert-Butylate,对甲苯磺酸体系中,用 溶剂黄146 作为反应溶剂,化学反应 5.0H,反应生成 溴长春胺
      参考文献:长春花生物碱及相关化合物的合成,Xxxiv 通过区域选择性溴化合成(3S,14S,16S)-溴长春胺和溴亚春胺
      标题:长春花生物碱及相关化合物的合成,Xxxiv 通过区域选择性溴化合成(3S,14S,16S)-溴长春胺和溴亚春胺
      摘要:通过亚胺盐 2A (X-Cl) 的溴化,得到无异构体状态的 9-溴衍生物 2C (X = Clo4).内酰胺 8D 的溴化导致 11-溴 (8C) 和 9-溴 (8A) 内酰胺的约 7.5:1 混合物.这些前体已被用于合成 9-,10-和 11-溴春胺 (11A-C) 以及 9-,10-和 11-溴春胺 (12A-C).
      DOI:10.1002/ardp.19873200904

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      专利信息


      专利号:US-2008287407-A1
      优先权日:2003-12-10
      标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
      发明人:GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
      权利人:NITROMED INC
      摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

      专利号:US-4314939-A
      优先权日:1979-07-13
      标题 :Process for the preparation of 15-hydroxyimino-E-homoeburnane and intermediates therefor
      发明人:SZANTAY CSABA; SZABO LAJOS; KALAUS GYOERGY; DANCSI LAJOS; KEVE TIBOR; DREXLER FERENC
      权利人:RICHTER GEDEON VEGYESZET
      摘要:A process for the preparation of 15-hydroxyimino-E-homoeburnane derivatives of the formula (I), ##STR1## wherein X 1 stands for hydrogen or halogen and n R is a C 1-6 alkyl group, n or acid addition salts and optically active derivatives thereof. These compounds are valuable intermediates of the synthesis of compounds with outstanding biological effects. According to the invention a racemic or optically active 15-hydroxy-E-homoeburnane derivative of the formula (II), ##STR2## is treated, optionally after separating the 15-epimers and/or resolution, with a halogenating agent. The resulting 15-halo-E-homoeburnane derivative of the formula (III), ##STR3## wherein X 2 stands for halogen, is reacted, optionally after separating the 15 epimers and/or resolution, with an alkali nitrite in the presence of an acid, and, if desired, the resulting 15-hydroxyimino-E-homoeburnane derivative of the formula (I) is converted into its acid addition salt and/or resolved. The compounds of the formula (III) formed as intermediates in the above process are new and biologically active.

      专利号:US-4343738-A
      优先权日:1979-08-06
      标题 :Halogenated 15-hydroxy-E-homoeburane derivatives
      发明人:SZANTAY CSABA; SZABO LAJOS; KALAUS GYOERGY; DANCSI LAJOS; KEVE TIBOR; DREXLER FERENC
      权利人:RICHTER GEDEON VEGYESZET
      摘要:The invention relates to new, racemic or optically active, halogenated 15-hydroxy-E-homoeburnane derivatives of the formulae (Ia) and/or (Ib), ##STR1## wherein R is a C 1-6 alkyl group and X is halogen, and acid addition salts thereof. These compounds are biologically active, furthermore they can be applied as intermediates in the synthesis of other pharmaceutically active substances.

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      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Araie M, Mayama C. Use of calcium channel blockers for glaucoma. Prog Retin Eye Res. 2011 Jan;30(1):54-71. doi: 10.1016/j.preteyeres.2010.09.002. Epub 2010 Oct 8. (2):CD002222. doi: 10.1002/14651858.CD002222.pub2. (4):CD002222. doi: 10.1002/14651858.CD002222. Update in: Cochrane Database Syst Rev. 2010;(2):CD002222. 105(12):828-42. Japanese. 8(2):117-23. 102(10):654-61. Japanese. 100(2):118-25. Japanese. 103(2):283-8. doi: 10.1016/s0161-6420(96)30703-3. 27(1):3-32. doi: 10.1016/0306-3623(95)00113-1. 26(6):1419-24. doi: 10.1016/0306-3623(94)00306-8. 44(7):803-8. 32(6):314-7. doi: 10.1159/000116851. 42(1):190-2. doi: 10.1016/0006-2952(91)90700-f. 11(1):39-46. doi: 10.1016/0197-4580(90)90060-d. Erratum in: Neurobiol Aging 1990 Nov- Dec;11(6):675. 184(2):175-80. French. 107(5-6):413-6. doi: 10.3109/00016488909127532. 37(3):298-307. doi: 10.1016/0026-2862(89)90048-4. 4(4):131-5. 39(12):1117-24. Japanese. 40(10):943-9. doi: 10.1016/0024-3205(87)90313-4.

      合成参考文献


      参考文献:10.1007/s004170050202
      摘要:Vainio-Jylhä E, Vuori M. The favorable effect of topical betaxolol and timolol on glaucomatous visual fields: a 2-year follow-up study. Graefe's Archive for Clinical and Experimental Ophthalmology. 1999 Jan 15;237(2):100–4. doi: 10.1007/s004170050202.
      参考文献:10.1007/s004170050203
      摘要:Daugeliene L, Kitazawa Y, Yamamoto T. Risk factors for visual field damage progression in normal-tension glaucoma eyes. Graefe's Archive for Clinical and Experimental Ophthalmology. 1999 Jan 15;237(2):105–8. doi: 10.1007/s004170050203.
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