专利号:WO-2009018504-A1 优先权日:2007-08-01 标题 :Process for the synthesis of diaminopyridine and related compounds 发明人:RITTER JOACHIM C 权利人:DU PONT; RITTER JOACHIM C 摘要:A process is provided for the synthesis of a diaminopyridine, such as 2,6-diaminopyridine and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a chlorine-ammonia displacement in the presence of a copper source.
专利号:US-8084569-B2 优先权日:2006-12-21 标 题 :Process for the synthesis of diaminopyridines from glutarimidines 发明人:MINTER AARON; STOKES BERLIN 权利人:MINTER AARON; STOKES BERLIN; DU PONT 摘要:A liquid-phase process is provided for the synthesis from glutarimidines of diaminopyridines and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a dehydrogenative aromatization process.
专利号:WO-2009018502-A3 优先权日:2007-08-01 标 题:Process for the synthesis of diaminopyridine and related compounds 发明人:RITTER JOACHIM C 权利人:DU PONT; RITTER JOACHIM C 摘要:A process is provided for the synthesis of a diaminopyridine, such as 2, 6-diaminopyridine and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a chlorine-ammonia displacement in the presence of a copper source.
专利号:US-8022167-B2 优先权日:2006-12-21 标 题 :Process for the synthesis of diaminopyridines from glutaronitriles 发明人:MINTER AARON; STOKES BERLIN 权利人:MINTER AARON; STOKES BERLIN 摘要:A liquid-phase process is provided for the manufacture from glutaronitriles and related compounds of 2,6-diaminopyridine and related compounds, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a dehydrogenative aromatization process.
专利号:US-7999057-B2 优先权日:2008-07-08 标 题:Gas-phase process for the synthesis of diaminopyridines from glutaronitriles 发明人:HUTCHENSON KEITH W; MINTER AARON; SUNSHINE GREGG 权利人:DU PONT 摘要:A gas-phase, continuous process is provided for the manufacture of 2,6-diaminopyridine and related compounds from glutaronitriles, which are used industrially as compounds and as components in the synthesis of a variety of useful materials. The synthesis proceeds by means of a dehydrogenative aromatization process.
专利号:US-9708317-B2 优先权日:2013-11-25 标 题 :Process for the preparation of 8-(4-aminophenoxy)-4H-pyrido[2,3-B]pyrazin-3-one derivatives 发明人:ZAMBON ALFONSO; NICULESCU-DUVAZ DAN; CHUBB RICHARD; SPRINGER CAROLINE JOY 权利人:CANCER RES TECH LTD; INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE); OXY SCIENT LTD; THE INST OF CANCER RESEARCH: ROYAL CANCER HOSPITAL 摘要:The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)-4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl-phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
[参考文献]: Dong-Mei Feng, Et Al. 2,3-Diaminopyridine As A Platform For Designing Structurally Unique Nonpeptide Bradykinin B1 Receptor Antagonists. Bioorg Med Chem Lett. 2005 May 2;15(9):2385-8. [参考文献]: G David, Et Al. Suppression By Phenytoin Of Convulsant-Induced Afterdischarges At Presynaptic Nerve Terminals. Brain Res. 1985 Jul 22;339(1):57-65. [参考文献]: H Y Huang, Et Al. Omega-Conotoxin Gvia Inhibits Release Of Noradrenaline From Rat Hippocampal Slices In The Absence Of Extracellular Calcium. Neuropharmacology. 1993 Feb;32(2):133-7. [参考文献]: Madhukar Hemamalini, Et Al. 2,3-Diamino-Pyridinium 3-Carb-Oxy-4-Hy-Droxy-Benzene-Sulfonate Monohydrate. Acta Crystallogr Sect E Struct Rep Online. 2011 Nov;67(Pt 11):O3122. [参考文献]: Maria Isabel Rodríguez-Cáceres, Et Al. Novel Hplc--Fluorescence Methodology For The Determination Of Methylglyoxal And Glyoxal. Application To The Analysis Of Monovarietal Wines "Ribera Del Guadiana". Food Chem. 2015 Nov 15:187:159-65.
合成参考文献
参考文献:10.1007/s00415-010-5472-0 摘要:Brugnoni R, Maggi L, Canioni E, Moroni I, Pantaleoni C, D'Arrigo S, Riva D, Cornelio F, Bernasconi P, Mantegazza R. Identification of previously unreported mutations in CHRNA1, CHRNE and RAPSN genes in three unrelated Italian patients with congenital myasthenic syndromes. J Neurol. 2010 Jul;257(7):1119–23. doi: 10.1007/s00415-010-5472-0. 参考文献:10.1039/c1pp05165b 摘要:Brenlla A, Veiga M, Ríos Rodríguez MC, Mosquera M, Rodríguez-Prieto F. Fluorescence of methylated derivatives of hydroxyphenylimidazopyridine. Resolution of strongly overlapping spectra and a new ESIPT dye showing very efficient radiationless deactivation. Photochemical & Photobiological Sciences. 2011 Oct;10(10):1622–36. doi: 10.1039/c1pp05165b.