4-(苯并三唑-1-基甲基-氨基)-苯甲酸置于sodium Tetrahydroborate体系中,用 四氢呋喃 用作溶剂,化学反应 0.33H,以91%的收率获得4-甲氨基苯甲酸 参考文献:Katritzky,Alan R.; Rachwal,Stanislaw; Rachwal,Bogumila,Journal Of The Chemical Society. Perkin Transactions I,1987,P. 805-810 标题:Katritzky,Alan R.; Rachwal,Stanislaw; Rachwal,Bogumila,Journal Of The Chemical Society. Perkin Transactions I,1987,P. 805-810
专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:EP-1431274-B1 优先权日:2002-12-18 标题 :Synthesis of mono-N-substituted functionalized anilines 发明人:SELVA MAURIZIO; TUNDO PIETRO 权利人:CONSORZIO INTERUNIVERSITARIO N 摘要:The present invention relates to a process for direct and selective synthesis of mono-N-substituted functionalized anilines by using alkylating agents selected from the class of organic carbonates, preferably of the dialkyl, dibenzyl and diallyl types, in the presence of suitable catalysts that are chemically related to the class of aluminosilicates.
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-5382582-A 优先权日:1993-03-26 标题:Methotrexate analogs and methods of using same 发明人:CHAN CARCY L 摘要:The methotrexate analogs 7-d-MTX, 7,9,9-d3-MTX, MTX halogenated or possessing some other such group at the 7-position capable of reducing oxidation to 7-OH-MTX, and structurally related analogs, as well as pharmaceutical compositions containing the analogs, the synthesis of the MTX analogs, and use of the analogs in modulating cellular function.
专利号:US-5446062-A 优先权日:1993-11-12 标 题:((4-alkoxypyran-4-yl) substituted) ether, arylalkyl-, arylalkenyl-, and arylalkynyl)urea inhibitors of 5-lipoxygenase 发明人:DELLARIA JOSEPH F; BASHA ANWER; BLACK LAWRENCE A; CHERNESKY LINDA J; LEE WENDY 权利人:ABBOTT LAB 摘要:Compounds of the structure where W is selected from where Q is oxygen or sulfur, R6 and R7 are hydrogen or alkyl, or R6 and R7, together with the nitrogen atoms to which they are attached, define a radical of formula Z is -CH2-, oxygen, sulfur, or -NR9, L1 and L2 are selected from a valence bond, alkylene, propenylene, and propynylene; R1 and R2 are independently selected from alkyl, alkoxy, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl; Y is selected from oxygen, >NR10, and L3 is selected from alkylene of one to three carbon atoms, propenylene, propynylene, and R3, R4, and R5 are hydrogen or alkyl of one to four carbon atoms inhibit the synthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
专利号:US-2011263540-A1 优先权日:2008-07-25 标题 :Small-molecule inhibitors of protein synthesis inactivating toxins 发明人:PANG YUAN-PING; TUMER NILGUN EREKEN; MILLARD CHARLES B 权利人:PANG YUAN-PING; TUMER NILGUN EREKEN; MILLARD CHARLES B 摘要:Small-molecule inhibitors of a protein synthesis inhibiting toxin, e.g., ricin, abrin, Shiga, and Shiga-like toxins, as well as methods of using the inhibitors are provided. Further provided are methods of identifying small-molecule inhibitors of a protein synthesis inhibiting toxin.
[参考文献]: Farook Adam, Et Al. Amino Benzoic Acid Modified Silica--An Improved Catalyst For The Mono-Substituted Product In The Benzylation Of Toluene With Benzyl Chloride. J Colloid Interface Sci. 2007 Jul 1;311(1):135-43. [参考文献]: Mitchell P Thayer, Et Al. Ph-Dependent Spectral Properties Of Para-Aminobenzoic Acid And Its Derivatives. Spectrochim Acta A Mol Biomol Spectrosc. 2011 Dec 15;84(1):227-32.
合成参考文献
摘要:Lai, J.; Thomson, B. J.; Sammis, G. M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 34. 参考文献:10.1107/s1600536810046258 摘要:Hökelek T, Sağlam EG, Tercan B, Aybirdi Ö, Necefoğlu H. Bis[μ-4-(methylamino)benzoato]-κ3O,O′:O;κ3O:O,O′-bis{aqua[4-(methylamino)benzoato-κ2O,O′](nicotinamide-κN)cadmium(II)}. Acta Crystallogr E Struct Rep Online. 2010 Nov 13;66(12):m1559–60. doi: 10.1107/s1600536810046258. 参考文献:10.1107/s1600536810046854 摘要:Hökelek T, Sağlam EG, Tercan B, Aybirdi Ö, Necefoğlu H. Diaquabis[4-(dimethylamino)benzoato-κO]bis(nicotinamide-κN1)zinc(II) dihydrate. Acta Crystallogr E Struct Rep Online. 2010 Nov 24;66(12):m1636–7. doi: 10.1107/s1600536810046854. 参考文献:10.1385/jmn:24:1:055 摘要:Wang Y, Klunk WE, Debnath ML, Huang G, Holt DP, Shao L, Mathis CA. Development of a PET/SPECT agent for amyloid imaging in Alzheimer’s disease. Journal of Molecular Neuroscience. 2004 Aug;24(1):55–62. doi: 10.1385/jmn:24:1:055.