合成目标产物 N-Methylpropargylamine 主要起始原料 Propargyl Bromide And Methylamine
(文献来源)合成步骤主要原料 Propargyl Bromide 和 Methylamine
N-Methyl N-Propargyl Bis-Dimethylphosphoramide置于oxonium体系中,用58%的收率获得产物n-甲基炔丙基胺 参考文献:Thermal Oxidative Deamination Of Aliphatic Amines To Aldehydes With Bis(Diphenylphosphinyl) Peroxide 标题:Thermal Oxidative Deamination Of Aliphatic Amines To Aldehydes With Bis(Diphenylphosphinyl) Peroxide 摘要:将在 1-亚甲基上具有假酸性氢的 N-取代烷基胺与过氧化双(二苯基膦)反应,通过热消除中间 O-二苯基膦羟基胺中的二苯基膦酸,得到脱氨基产物. DOI:10.1055/s-1988-27750
专利号:US-2013267680-A1 优先权日:2010-09-15 标题:Total chemical synthesis of ubiquitin, ubiquitin mutants and derivatives thereof 发明人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL 权利人:OVAA HUIB; EL OUALID FARID; MERKX REMCO NICOLAAS SEBASTIAAN MICHEL; STICHTING HET NL KANKERINST 摘要:The present invention relates to the field of total chemical synthesis of ubiquitin and related peptides. More in particular, a method is provided of solid phase synthesis of ubiquitin, ubiquitin mutants and derivatives thereof. It was the object of the present invention to provide an approach for the total chemical synthesis of ubuiqitin, which allows for the chemical synthesis of virtually any Ub mutant and giving high overall efficiency and purity. The present inventors have surprisingly found that this object can be realized with a method relying on incorporation of special amino acid building blocks. This approach was found to allow for exceptionally high yields of up to 14% and to provide an synthetic entry into virtually any ubiquitin derivative.
专利号:US-2003050305-A1 优先权日:2000-05-22 标题:Thromboxane inhibitors, compositions and methods of use 发明人:TEJADA INIGO SAENZ DE 摘要:The present invention describes methods for treating or preventing sexual dysfunctions in males and females, and for enhancing sexual responses in males and females by administering a therapeutically effective amount of at least one thromboxane inhibitor, and, optionally, 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 vasoactive agent. The male or female may preferably be diabetic. The present invention also provides novel compositions comprising at least one thromboxane inhibitor, 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, optionally, at least one therapeutic agent, such as, vasoactive agents, nonsteroidal antiinflanmmatory compounds (NSAIDs), selective cyclooxygenase-2 (COX-2) inhibitors, anticoagulants, angiotensin converting enzymes (ACE) inhibitors, angiotensin II receptor antagonists, renin inhibitors, and mixtures thereof. The present invention also provides methods for treating or preventing ischemic heart disorders, myocardial infarction, angina pectoris, stroke, migraine, cerebral hemorrhage, cardiac fatalities, transient ischaemic attacks, complications following organ transplants, coronary artery bypasses, angioplasty, endarterectomy, atherosclerosis, pulmonary embolism, bronchial asthma, bronchitis, pneumonia, circulatory shock of various organs, nephritis, graft rejection, cancerous metastases, pregnancy-induced hypertension, preeclampsia, eclampsia, thrombotic and thromboembolic disorders, intrauterine growth, gastrointestinal disorders, renal diseases and disorders, disorders resulting from elevated uric acid levels and dysmenorrhea, and for inhibiting platelet aggregation or platelet adhesion or relaxing smooth muscles.
专利号:US-7211590-B2 优先权日:2002-08-01 标 题:Nitrosated proton pump inhibitors, compositions and methods of use 发明人:FANG XINQIN; GARVEY DAVID S; LETTS L GORDON 权利人:NITROMED INC 摘要:The invention describes novel nitrosated proton pump inhibitor compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated proton pump inhibitor 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 nitrosated proton pump inhibitor 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 nitrosated proton pump inhibitor compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating gastrointestinal disorders; facilitating ulcer healing; decreasing the recurrence of ulcers; improving gastroprotective properties, anti-Helicobacter pylori properties or antacid properties of proton pump inhibitors; decreasing or reducing the gastrointestinal toxicity associated with the use of nonsteroidal antiinflammatory compounds; treating bacterial infections and/or viral infections.
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-12180182-B2 优先权日:2021-12-01 标题 :(Di)amination of activated allene compounds, derivatives thereof, and methods for synthesis of the same 发明人:DAI MINGJI 权利人:PURDUE RESEARCH FOUNDATION 摘要:One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.
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.
摘要:Huy, P.; Czekelius, C., Science of Synthesis Knowledge Updates, (2019) 2, 162. 摘要:Arndtsen, B. A.; Tjutrins, J., Science of Synthesis: Multicomponent Reactions, (2013) 2, 478. 参考文献:10.1007/s11030-005-9009-x 摘要:Roy DR, Sarkar U, Chattaraj PK, Mitra A, Padmanabhan J, Parthasarathi R, Subramanian V, Van Damme S, Bultinck P. Analyzing toxicity through electrophilicity. Mol Divers. 2006 May;10(2):119–31. doi: 10.1007/s11030-005-9009-x. 参考文献:10.1023/b:neur.0000011327.23739.1b 摘要:Sharma SK, Carlson EC, Ebadi M. Neuroprotective actions of Selegiline in inhibiting 1-methyl, 4-phenyl, pyridinium ion (MPP+)-induced apoptosis in SK-N-SH neurons. J Neurocytol. 2003 May;32(4):329–43. doi: 10.1023/b:neur.0000011327.23739.1b. 参考文献:10.1007/s007020200050 摘要:Naoi M, Maruyama W, Akao Y, Yi H. Mitochondria determine the survival and death in apoptosis by an endogenous neurotoxin, N-methyl(R)salsolinol, and neuroprotection by propargylamines. J Neural Transm (Vienna). 2002 May;109(5-6):607–21. doi: 10.1007/s007020200050.