吡嗪酰胺置于三氯氧磷体系中,化学反应 1.5H,以85%的收率获得2-氰基吡嗪 参考文献:5-Alkyl-2-Pyrazinecarboxamides,5-Alkyl-2-Pyrazinecarbonitriles And 5-Alkyl-2-Acetylpyrazines As Synthetic Intermediates For Antiinflammatory Agents 标题:5-Alkyl-2-Pyrazinecarboxamides,5-Alkyl-2-Pyrazinecarbonitriles And 5-Alkyl-2-Acetylpyrazines As Synthetic Intermediates For Antiinflammatory Agents 摘要:2-吡啶基腈,2-乙酰吡嗪,5-烷基-2-吡嗪羧酰胺,5-烷基-2-吡嗪腈和5-烷基-2-乙酰吡嗪被制备为合成潜在抗炎药物的中间体.将吡啶羧酰胺的自由基烷基化结果与已发表的数据进行了比较.2-乙酰吡嗪及其5-(1,1-二甲基乙基)衍生物被筛选用于生物活性,但未发现有趣的效果. Doi:10.1135/cccc19961093
专利号:US-6566292-B2 优先权日:2001-03-27 标 题 :Process for the enhancement of the cycle life of a zinc-chromium based catalyst in the synthesis of 2-methylpyrazine 发明人:POTHARAJU SEETHARAMANJANEYA SA; RAGHAVAN KONDAPURAM VIJAYA; RAO PANJA KANTA; KULKARNI SHIVANAND JANARDAN; RAO KATABATHINI NARASIMHA; GOPINATH RAJESH; FARSINAVIS SURESH; MESHRAM HARSHADAS MITARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to enhancement of the cycle life of a zinc chromium based catalyst used in the synthesis of 2-methylpyrazine by increasing the reaction temperature step-wise, starting from a low temperature, while monitoring the levels of total conversion and selectivity towards pyrazine. The catalyst can be regenerated after each cycle of use without substantial loss of activity.
专利号:EP-1373226-B1 优先权日:2001-03-30 标题 :Process for the enhancement of cycle life of a zinc-chromium based catalyst in the synthesis of 2-methylpyrazine 发明人:POTHARAJU SEETHARAMANJANEYA SA; RAGHAVAN KONDAPURAM VIJAYA; RAO PANJA KANTA; KULKARNI SHIVANAND JANARDAN; RAO KATABATHINI NARASIMHA; GAPINATH RAJESH; FARSINAVIS SURESH; MESHRAM HARSHADAS MITARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to enhancement of the cycle life of a zinc chromium based catalyst used in the synthesis of 2-methylpyrazine by increasing the reaction temperature step-wise, starting from a low temperature, while monitoring the levels of total conversion and selectivity towards pyrazine. The catalyst can be regenrated after each cycle of use without substantial loss of activity.
专利号:US-12428656-B2 优先权日:2020-02-28 标题 :Nitrilase mutant and application thereof in the synthesis of 1-cyanocyclohexyl acetic acid 发明人:XUE YAPING; XIONG NENG; LI QIAN; ZHENG YUGUO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:The present invention provides a nitrilase mutant and application thereof in the synthesis of 1-cyanocyclohexyl acetic acid, the nitrilase mutant is obtained by mutating one or two of the amino acids at position 180 and 205 of the amino acid sequence shown in SEQ ID No. 2. In the present invention, by semi-rational design and protein molecular modification, the specific enzyme activity of the nitrilase double mutant AcN-G180D/A205C was increased by up to 1.6 folds, and the conversion rate>99%. And the reaction time was shortened to a quarter of the original using the recombinant Escherichia coli containing the nitrilase mutant to hydrolyze 1-cyanocyclohexylacetonitrile at high temperature (50° C.). Therefore, the mutants obtained by the present invention have a good application prospect in efficiently catalyzing 1-cyanocyclohexylacetonitrile to synthesize gabapentin intermediate, 1-cyanocyclohexyl acetic acid.
专利号:US-2010278715-A1 优先权日:2009-04-29 标 题:Systems, Devices, and/or Methods Regarding Specific Precursors or Tube Control Agent for the Synthesis of Carbon Nanofiber and Nanotube 发明人:KHE NGUYEN 权利人:TH LLC 摘要:Certain exemplary embodiments can comprise, via a tube control agent (TCA) and a metallic catalyst, producing a carbon nanotube. At least some carbon used to form the carbon nanotube can be obtained from a plant, a cellulose product, and/or a cellulosic product. At least some of the carbon can be converted into powder.
专利号:US-5698556-A 优先权日:1995-06-07 标题 :Methotrexate analogs and methods of using same 发明人:CHAN CARCY L 摘要:The present invention provides methotrexate analogs having the formula: +TR wherein R is methyl or hydro, X is halo or hydro, and D1 is -NR1R2 wherein either both R1 and R2 are hydrogen, or one is hydrogen and the other is C1-C5 alkyl, C1-C5 haloalkyl, cyano C1-C5 alkyl, C1-C5 hydroxyalkyl, alkoxyalkyl wherein the alkoxy and the alkyl have 1-5 carbon atoms, carboxy C1-C5 alkyl, phenyl, C1-C5 alkyl phenyl, C(=O)R' wherein R' is hydrogen, C1-C5 alkyl, phenyl, or C1-C5 alkyl phenyl, C(=O)OR'' wherein R'' is hydrogen, C1-C5 alkyl, phenyl, or C1-C5 alkyl phenyl, amino, C(=NH)NH2, C(=O)NH2, or C(=S)NH2, and structurally related derivatives, as well as pharmaceutical compositions comprising such MTX analogs, methods of synthesis of the MTX analogs, and use of the MTX analogs in modulating cellular functions, or in treating cancer and other diseases or disorders capable of being treated using MTX.
专利号:US-9181203-B2 优先权日:2010-11-12 标题:Substituted pyrazino[2,3-d]isooxazoles as intermediates for the synthesis of substituted pyrazinecarbonitriles and substituted pyrazinecarboxamides 发明人:NAKAMURA KOUKI; MURAKAMI TAKESHI; NAITOU HIROYUKI; HANAKI NAOYUKI; WATANABE KATSUYUKI 权利人:FUJIFILM CORP; TOYAMA CHEMICAL CO LTD 摘要:The object of the present invention is to provide a compound which is useful as a production intermediate of pyrazine carboxamide derivative such as 6-fluoro-3-hydroxy-2-pyrazine carboxamide. The present invention provides a pyrazino[2,3-d]isoxazole derivative represented by the formula (I): n nwherein X represents a halogen atom, a hydroxyl group or a sulfamoyloxy group, and Y represents —C(â•?O)R or —CN; wherein R represents a hydrogen atom, an alkoxy group an aryloxy group, an alkyl group, an aryl group or an amino group.