CAS: 549-84-8; .β.-Yohimbine

上下游产品

CAS号146-48-5 育亨宾

📜Methyl Endo/exo-3-(Bicyclo<2,2,1>Hept-5-En-2-yl)-3-Oxopropanoate置于palladium On Activated Charcoal 盐酸,Sodium Tetrahydroborate,1,4-Diazabicyclo[5.4.0]-7-Undecene,硫酸,氢气体系中,用 甲醇 作为反应溶剂,540.0 °C,101.33 Kpa 条件下,反应 44.33H,反应生成 Beta-育亨宾
参考文献:Total Syntheses Of Yohimbe Alkaloids,With Stereoselection For The Normal,Allo,And 3-Epiallo Series,Based On Annelations Of 4-Methoxy-1,2-Dihydropyridones
标题:Total Syntheses Of Yohimbe Alkaloids,With Stereoselection For The Normal,Allo,And 3-Epiallo Series,Based On Annelations Of 4-Methoxy-1,2-Dihydropyridones
摘要:N-[2-(1H-3-Indolyl)Ethyl]-2,3-Dihydro-4-Pyridone (31) Was Generated In Two Steps (77% Yield) From Tryptamine And N-Methyl-4-Piperidone Methiodide. Its Cyclization (90% Yield) And Oxidation (91% Yield) Provided The Tetracyclic Analogue 32. O-Methylation And Robinson-Type Annelation Of These Vinylogous Lactams (The Latter In Form Of Its N(A)-Carbamate) Furnished The Dienones 38 (64%) And 43 (90%). Further Elaboration By Cyclization And/or Reduction Reactions Selectively Provided The 15,16-Didehydroyohimbinones 7 Or 44. Their Reductions Then Led To Yohimbinone (52,20% Overall Yield From Tryptamine),Alloyohimbinone (11,19% Overall Yield),And 3-Epi-Alloyohimbinone (10,23% Overall Yield),Which Led To Yohimbine (3),Beta-Yohimbine (9),3-Epi-Alloyohimbine (53),And 3-Epi-17-Epi-Alloyohimbine (54).
DOI:10.1021/jo00008A025

专利信息

专利号:US-6469065-B1
优先权日:1996-02-02
标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use
发明人：GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.

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-2005187222-A1
优先权日:1996-02-02
标题:Nitrosated and nitrosylated alpha-adrenergic receptor antagonist compounds
发明人：GARVEY DAVID S; DE TEJADA INIGO S; GASTON RICKY D; KHANAPURE SUBHASH P; SHELEKHIN TATIANA E; WANG TIANSHENG
权利人:NITROMED INC
摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.