N-甲基-1,2-苯二胺置于二过氧壬二酸体系中,用 乙腈 作为反应溶剂,化学反应 0.5H,以89%的收率获得产物n-甲基-2-硝基苯胺 参考文献:Steric-Hindrance-Induced Regio-And Chemoselective Oxidation Of Aromatic Amines 标题:Steric-Hindrance-Induced Regio-And Chemoselective Oxidation Of Aromatic Amines 摘要:Unusual Regio-And Chemoselective Oxidation Of Aromatic Amines Hindered With Ortho Substituents (Except-Nh2,-Nhch3,And-Oh) To The Corresponding Nitro Compounds Is Described By Use Of Nonanebis(Peroxoic Acid). The Mechanistic Investigation For Selective Oxidation Of Amines Ortho-Substituted With-Nh2 Or-Oh Showed The Involvement Of H-Bonding Between The Ortho Hydrogen Of The Adjacent-Xh Group (Where X = Nh,Nr,Or O) And An Oxygen Atom From The Diperoxy Acid. Various Mono-And Diamines Are Oxidized Into Corresponding Mononitro Derivatives In High Yield And Purity Without Employing Any Protection Strategies. The Protocol Was Also Found To Successful On The Gram Scale. DOI:10.1021/acs.Joc.5B00582
专利信息
专利号:US-4269773-A 优先权日:1976-04-27 标 题:Fused oxazolidine compounds 发明人:MITSURU YOSHIOKA; TERUJI TSUJI; YASUHIRO NISHITANI; WATARU NAGATA 权利人:SHIONOGI & CO 摘要:Compounds represented by the following formula prepared from 6-aminopenicillanic acid are key intermediates in a stereo-specific synthesis of 1-oxadethiacephalosporins, highly active antibiotics: +TR [wherein COA and COB each is carboxy or protected carboxy; COX is carboxy, protected carboxy, or a group of the formula -COCQ=N2 or -COCHQ-Z (in which Q is hydrogen, lower alkyl or aryl; and Z is hydrogen or a nucleophilic group); Hal is halogen; R is lower alkyl or aralkyl; and Y is hydrogen or acyl].
专利号:US-8362019-B2 优先权日:2008-02-01 标 题:Synthesis and anti-proliferative effect of substituted imidazo[4,5-b]pyrazine compounds 发明人:WINFIELD LEYTE L 权利人:SPELMAN COLLEGE; WINFIELD LEYTE L 摘要:This invention provides for compounds, compositions, and methods that involve anti-proliferative and anti-neoplastic activity in cancer cells. In particular, a series of benzimidazole, purine, imidazopyridine, and imidazopyrizine compounds having selected substitution patterns are disclosed, and the activity of various subject compounds is demonstrated. In particular, the disclosure provides for substituted imidazo[4,5-b]pyrazine compounds having the general formula n ntheir salts, pharmaceutical compositions, and methods of treatment using the subject compounds and compositions.
专利号:US-8344010-B2 优先权日:2008-12-26 标 题 :Fused imidazole derivatives as TRPV3 antagonist 发明人:LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI 权利人:GLENMARK PHARMACEUTICALS SA; LINGAM V S PRASADARAO; THOMAS ABRAHAM; PHATANGARE SHANTARAM KASHINATH; MINDHE AJIT SHANKAR; KHATIK JAVED YUSUF; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI 摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.
专利号:US-2012095009-A1 优先权日:2008-02-01 标题 :Synthesis and anti-proliferative effect of benzimidazole derivatives
专利号:TW-201124411-A 优先权日:2009-11-26 标 题 :The manufacturing method of 6-substituted-1-methy-1H-benzimidazol derivatives and the synthesis intermediates thereof
专利号:US-9974779-B2 优先权日:2006-05-19 标 题:Piperidine derivatives as human papilloma virus inhibitors 发明人:BLUMENFELD MARTA; COMPERE DELPHINE; GAUTHIER JEAN-MICHEL 权利人:AVIRAGEN THERAPEUTICS INC; VAXART INC 摘要:The present disclosure is directed to antiviral compounds directed against the papilloma virus, to pharmaceutical compositions containing them, to their preparation method and synthesis intermediates, as well as to their use for treating or preventing an infection by the papilloma virus. The present method thus provides an efficient way of treating patients that have lesions associated with an infection by the papilloma virus.