456-48-4 + 593-51-1 = 90389-84-7 反应条件:1.1 Reagents: Potassium Carbonate Solvents: Methanol; 30 Min,Rt1.2 1 H,Rt; Rt -> 0 °C1.3 Reagents: Sodium Borohydride; 0 °C; 1 H,0 °C; 0 °C -> Rt; 2 H,Rt 标题:Discovery Of A Highly Potent,Selective,And Metabolically Stable Inhibitor Of Receptor-Interacting Protein 1 (Rip1) For The Treatment Of Systemic Inflammatory Response Syndrome 作者:Ren,Yan; Et Al 参考文献:Journal Of Medicinal Chemistry 日期:2017 卷标:60(3) 页码:972-986]
456-48-4 = 90389-84-7 反应条件:1.1 Solvents: Methanol,Water; 20 Min,Rt1.2 Reagents: Sodium Borohydride Solvents: Methanol,Water; 2.5 H,0 °C -> Rt 标题:4-Phenyl Tetrahydroisoquinolines As Dual Norepinephrine And Dopamine Reuptake Inhibitors 作者:Pechulis,Anthony D.; Et Al 参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2012 卷标:22(23) 页码:7219-7222
1-(3-Fluorophenyl)-N-Methylmethanimine置于lithium Aluminium Tetrahydride体系中,用 乙醚 作为反应溶剂,化学反应 2.0H,反应生成 N-甲基-3-氟苄胺 参考文献:Benzylamines: Synthesis And Evaluation Of Antimycobacterial Properties 标题:Benzylamines: Synthesis And Evaluation Of Antimycobacterial Properties 摘要:The Synthesis Of Benzylamines With Various N-Alkyl Chains And Substituents In The Aromatic System As Well As Their Evaluation On Mycobacterium Tuberculosis H 37 Ra Are Described. The Most Active Compounds In This Test,N-Methyl-3-Chlorobenzylamine (19,Mic 10.2 Micrograms/ml),N-Methyl-3,5-Dichlorobenzylamine (93,Mic 10.2 Micrograms/ml),And N-Butyl-3,5-Difluorobenzylamine (103,Mic 6.4 Micrograms/ml),Also Exhibited A Marked Inhibitory Effect On Mycobacterium Marinum And Mycobacterium Lufu Used For The Determination Of Antileprotic Properties. The Combinations Of 93 With Aminosalicylic Acid,Streptomycin,Or Dapsone Exert Marked Supra-Additive Effects On M. Tuberculosis H 37 Ra. DOI:10.1021/jm00375A005
专利号:US-8981092-B2 优先权日:2008-09-19 标题 :Substituted 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-ones as modulators of protein kinase activity 发明人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO 权利人:MIRIZZI DANILO; CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; FERGUSON RON; CASUSCELLI FRANCESCO; NERVIANO MEDICAL SCIENCES SRL 摘要:Compounds which are 4,7-disubstituted derivatives of 3,4-dihydro-2H-pyrrolo[1,2-a]pyrazin-1-one compounds, n nor pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
专利号:US-10017481-B2 优先权日:2012-03-17 标 题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC 权利人:POLYPHOR AG 摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
专利号:US-10766863-B2 优先权日:2014-11-17 标 题 :Monocarboxylate transport modulators and uses thereof 发明人:SANDANAYAKA VINCENT; WU QIONG 权利人:NIROGYONE THERAPEUTICS INC 摘要:The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.
参考标题:One-Pot Synthesis Of 2-Aminobenzoxazole Derivatives Using Acetic Acid As An Electrolyte Under Electrochemical Conditions 作者:Tanay Ghoshal,Tarun M. Patel |发布日期:2021.9 摘要:Ammoniumbromide, Sodium Iodide And Lithium Perchlorate, But In This Conversion We Have Removed The Use Of All Supporting Electrolytes And We Have Used Acetic Acid, Which Plays A Dual Role Of Opening The Benzoxazole Moiety And Works As An Electrolyte. All These Electrochemical Conversions Were Done On A Electrochemical Reactor Prepared Through A 5V Mobile Charger Having A Output Current Density Of 0.35A.Cm−2. Various
合成参考文献
参考文献:10.1177/2472555219873068 摘要:Lee OW, Austin S, Gamma M, Cheff DM, Lee TD, Wilson KM, Johnson J, Travers J, Braisted JC, Guha R, Klumpp-Thomas C, Shen M, Hall MD. Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. SLAS Discov. 2020 Jan;25(1):9–20.