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4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yloxy)quinazoline (0)tetrakis(triphenylphosphine) palladium(0) pyrimidine 5-boronic acid 4-(pyrimidin-5-yloxy)benzaldehyde 3-fluoro-5-(pyrimidin-5-yloxy)benzonitrile 合成工艺路线路线简述
- 合成目标产物 5-Hydroxypyrimidine 主要起始原料 Pyrimidine, 5-(Phenylmethoxy)-
- (文献来源)合成步骤主要原料 Pyrimidine, 5-(Phenylmethoxy)-
📜5-甲氧基嘧啶置于sodium Hydride,乙硫醇体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 4.0H,以50%的收率获得5-羟基嘧啶
参考文献:环氮原子对酚类化合物的均相反应性的影响:了解5-嘧啶的清除自由基的能力.
标题:环氮原子对酚类化合物的均相反应性的影响:了解5-嘧啶的清除自由基的能力.
摘要:合成了六个取代的5-嘧啶醇,研究了它们与自由基反应的热化学和动力学,并将其与同等取代的酚进行了比较.为了评估其作为自由基的氢原子供体的潜力,我们使用自由基平衡电子顺磁共振技术测量了其oh键离解焓(bde).这表明,5-嘧啶醇中的oh Bde平均比同等取代的酚类中的高约2.5 Kcal Mol(-1).结果与理论预测吻合非常好,证实了取代基对5-嘧啶醇的oh Bde的影响与对苯酚中obond; H Bde的影响基本相同.通过抑制aibn引发的苯乙烯的自氧化,以及通过竞争动力学与烷基和烷氧基的反应,研究了这些化合物与过氧自由基的反应动力学.尽管它们的oh Bde较大,但5-嘧啶醇似乎将其酚氢原子转移到过氧自由基上的速度与同等取代的酚一样快,而它们对烷基自由基的反应性却远远超过了相应的酚.我们建议,这种速率的提高是由于这些原子的过渡态中的极性效应引起的,该速率的提高在烷基自由基反应的情况下较大,在
Doi:10.1002/chem.200304960
专利信息
专利号:US-5350851-A
优先权日:1992-03-16
标题 :Intermediates and a process for synthesis of tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolate and N5-formyl-(6S)-tetrahydrofolate
发明人:BAILEY STEVEN W; AYLING JUNE E
权利人:UNIV SOUTH ALABAMA
摘要:Intermediates and a process for the synthesis of 6-monosubstituted tetrahydropteridine C6-stereoisomers, including (6S)-tetrahydrofolic acid. The intermediates are shown in their two enantiomeric forms as follows: ##STR1## wherein R 1 and R 2 are the same or different and represent hydrogen, methyl, hydroxy, amino, alkyl or dialkylamino, alkoxy, benzyloxy, or benzylthio; R 3 represents an alkene, alkyne, cycloalkyl, benzyl, alkyl (substituted with hydroxy, acetoxy, benzyloxy, alkoxy, alkylthio, amino, carboxy, oxo, or phosphate), a protected aldehyde, or ##STR2## wherein n=1 or 2, R 4 is hydrogen, formyl, methyl, or propargyl, and ZZ represents an amino acid or amino acid polymer.
专利号:US-4940712-A
优先权日:1989-05-26
标 题 :Derivatives of hydroxyprimidines as leukotriene synthesis inhibitors
发明人:WALKER FREDERICK J; MELVIN LAWRENCE S
权利人:PFIZER
摘要:2-Amino and 2-thio-4-substituted-5-(hydroxy or alkoxy)-pyrimidines, which may be 6-substituted, and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are, therefore, useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases. The compounds are also cytoprotective and therefore, useful in the treatment of peptic ulcers.
专利号:US-4847258-A
优先权日:1986-08-26
标 题:Substituted benzoylphenylureas compounds useful as pesticides
发明人:STURM ELMAR; LANG ROBERT W; KRISTIANSEN ODD
权利人:CIBA GEIGY CORP
摘要:The invention relates to novel N-benzoyl-N,-4-(5-phenylpyrimid-2-yloxy)phenylureas of formula +TR wherein X1 is hydrogen, halogen, C1-C3alkoxy or C1-C3alkylthio, X2 is halogen, methyl, C1-C3alkoxy or C1-C3alkylthio, Y1, Y2, Y3 and Y4 are each independently hydrogen, halogen, methyl, trifluoromethyl or methoxy, Z is methyl, halomethyl containing 1 to 3 halogen atoms or pentafluoroethyl; and R1, R2 and R3 are each independently hydrogen, halogen, C1-C3alkyl, trifluoromethyl or C1-C3alkoxy, to the preparation thereof and to intermediates for the synthesis of these compounds, as well as to compositions containing them for use in pest control, especially for controlling representatives of the order Acarina that attack plants and animals and for controlling insects. The novel compounds exhibit especially pronounced activity against plant-destructive mites.
专利号:WO-9319069-A1
优先权日:1992-03-16
标题:Intermediates and a process for synthesis of tetrahydropteridine c6-stereoisomers, including (6s)-tetrahydrofolate and n5-formyl-(6s)-tetrhydrofolate
专利号:CN-105457680-B
优先权日:2015-11-18
标题 :A Cu Composite Catalyst for Oxidative Carbonylation Synthesis of Alkyl Carbonates
专利号:CN-105457680-A
优先权日:2015-11-18
标题 :A Cu Composite Catalyst for Oxidative Carbonylation Synthesis of Alkyl Carbonates