合成目标产物 Methyl 6-Methylnicotinate 主要起始原料 Methanol And 6-Methylnicotinic Acid
(文献来源)合成步骤主要原料 Methanol 和 6-Methylnicotinic Acid
5-乙基-2-甲基-吡啶置于硫酸,硝酸体系中,化学反应生成 6-甲基烟酸甲酯 参考文献:Synthesis,Characterization And Molecular Docking Studies Of Some New 1,3,4-Oxadiazolines Bearing 6-Methylpyridine Moiety For Antimicrobial Property 标题:Synthesis,Characterization And Molecular Docking Studies Of Some New 1,3,4-Oxadiazolines Bearing 6-Methylpyridine Moiety For Antimicrobial Property 摘要:A New Series Of 3-Acetyl-2-Aryl-2H/methy1-5[3-(6-Methylpyridinyl)]-2,3-Dihydro-[1,3,4]-Oxadiazole Derivatives Were Synthesized From 6-Methyl Nicotinate Through A Multistep Reaction Sequence. The Structures Of Newly Synthesized Compounds Were Established On The Basis Of Elemental Analysis,Ir,H-1 NMR,C-13 NMR And Mass Spectral Data. Three Dimensional Structure Of The Compound 5F Was Further Confirmed By Single Crystal X-Ray Analysis. All The Synthesized Compounds Were Screened For Their Antimicrobial Activity And Antioxidant Activity. The Final Compounds Were Subjected To Molecular Docking Studies For The Inhibition Of Enzyme L-Glutamine: D-Fructose-6-Phosphate Amidotransferase [glcn-6-P] (Ec 2.6.1.16). The In Silico Molecular Docking Results Are Matching With The In Vitro Studies And They May Be Considered As Good Inhibitor Of Glcn-6-P Synthase.6-Methylpyridine. (C) 2013 Elsevier Masson Sas. All Rights Reserved. DOI:10.1016/j.Ejmech.2013.07.019
专利号:EP-1404682-B1 优先权日:2001-06-29 标题:Method of inhibiting ptp 1b and/or t-cell ptp and/or other ptpases with an asp residue at position 48 发明人:HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL 权利人:NOVO NORDISK AS 摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al., Proc. Natl. Acad. Sci. USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1. This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
专利号:US-2003064979-A1 优先权日:2001-06-29 标题 :Method of inhibiting PTP 1B and /or T-cell PTP and/or other PTPases with an Asp residue at position 48 发明人:HANSEN THOMAS KRUSE; OLSEN OLE HVILSTED; PETERSEN ANDERS KLARSKOV; LAU JESPER; ANDERSEN HENRIK SUNE; MOLLER NIELS PETER HUNDAHL 摘要:This invention relates to oxalylamide inhibitors of Protein Tyrosine Phosphatase 1B (PTP1B) and/or T-cell Protein Tyrosine Phosphatase (TC-PTP) and/or Protein Tyrosine Phosphatases (PTPases) having an aspartic acid (Asp) in position 48 (PTP1B numbering, Chernoff et al, Proc Natl Acad Sci USA 87: 2735-2789 (1989)) and a method of inhibiting such PTPases by exposing the enzyme to inhibitor compounds of formula 1 n n n This invention also relates to (I) the design and selection of inhibitors, which bind to the active site of PTP1B and/or TC-PTP and/or PTPases having an aspartic acid (Asp) in position 48 (II) the synthesis of said inhibitors, methods for their preparation and (III) to compositions comprising the inhibitor compounds.
专利号:US-8012972-B2 优先权日:2007-03-28 标 题:Pyridinecarboxylic acid (2-aminophenyl) amide derivative having urea structure 发明人:MOGI HIROYUKI; TAJIMA HISASHI; MISHINA NORIKO; YAMAZAKI YUSUKE; YONEDA SHINJI; WATANABE KATSUHIKO; FUJIKAWA JUNKO; YAMAMOTO MINORU 权利人:SANTEN PHARMACEUTICAL CO LTD 摘要:Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R 1 and R 2 represent a hydrogen atom, a lower alkyl group or the like; R 3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, —OCONR a R b , —NR c R d or the like; R 4 and R 5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; R a and R b represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; R c and R d represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W 1 -W 2 represents N—C or C—N; and l and m represent 0, 1, 2 or 3.
专利号:US-8841457-B2 优先权日:2010-11-15 标题:Process for cyclooxygenase-2 selective inhibitor 发明人:SHAH DHARMESH MAHENDRA; SOLANKI SANJAY AMRATLAL; JARIWALA VIRAL NARENDRA; VYAS ASHOK VASANTRAY; MISTRY ASHOKKUMAR BHIKHUBHAI 权利人:SHAH DHARMESH MAHENDRA; SOLANKI SANJAY AMRATLAL; JARIWALA VIRAL NARENDRA; VYAS ASHOK VASANTRAY; MISTRY ASHOKKUMAR BHIKHUBHAI; VIRDEV INTERMEDIATES PVT LTD 摘要:The present invention describes a process for preparing a cyclooxygenase-2 selective inhibitor. It provides a synthetic procedure for the said substance namely 5-chloro-3-(4-methylsulphonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine of formula (I). The invention also relates to preparation of a new intermediate of formula (IV) and a process to prepare it. Furthermore, the invention describes a process for preparing another key intermediate of formula (II). Compounds of formula (IV) and formula (II) are useful intermediates in synthesis of the said cyclooxygenase-2 inhibitor.
专利号:WO-0129003-A1 优先权日:1999-10-15 标 题 :Process for the preparation of 1-(6-methylpyridin-3-yl)-2-(4-methylthiophenyl)-ethanone and its use in the synthesis of diarylpyridines
专利号:EP-1071745-A4 优先权日:1998-04-24 标题 :PROCESS FOR THE SYNTHESIS OF COX-2 INHIBITORS