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.
专利号:US-7060818-B2 优先权日:2003-02-21 标题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process 发明人:HORWITZ COLIN P; GHOSH ANINDYA 权利人:UNIV CARNEGIE MELLON 摘要:An improved method of synthesizing a macrocyclic tetraamido compound includes protecting the amino portion of an amino carboxylic acid to form a protected amino carboxylic acid; exposing the protected amino carboxylic acid to a first solvent, preferably a hydrocarbon solvent, such as toluene or 1,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane. The carboxylic acid portion of the protected amino carboxylic acid is then converted to an activated carboxylic acid by one of esterification or acid halide formation, to form a protected amino activated carboxylic acid derivative. The protected amino activated carboxylic acid derivative is reacted with a diamine in the presence of a second solvent, such as THF or ,2-dichloroethane, dichloromethane, dibromomethane and 1,2-dibromoethane, to form a protected diamide diamine intermediate. Following deprotection, the diamide diamine intermediate is reacted with an activated diacid, such as an activated malonate, oxalate or succinate derivative to form the macrocyclic tetraamido compound. The macrocyclic tetraamido compound may further be complexed with a transition metal.
专利号:US-6011152-A 优先权日:1996-07-22 标 题 :Synthesis of macrocyclic tetraamido-N ligands
专利号:US-2004167329-A1 优先权日:2003-02-21 标 题:Synthesis of macrocyclic tetraamido compounds and new metal insertion process
专利号:WO-2004076425-A1 优先权日:2003-02-21 标题:Improved synthesis of macrocyclic tetraamido compounds and new metal insertion process
专利号:US-2005113397-A1 优先权日:2002-01-31 标题:Imidazo[1,2-a]pyridine derivative 发明人:TAKEMURA MAKOTO; TAKAHASHI HISASHI; KAWAKAMI KATSUHIRO; TAKESHITA HIROSHI; KIMURA YOUICHI; WATANABE JUN; SUGIMOTO YUICHI; KITAMURA AKIHIRO; NAKAJIMA RYOHEI; KANAI KAZUO; FUJISAWA TETSUNORI 摘要:A compound reprsented by the following formula (I), its salts or nsolvates thereof capable of specifically or selectively expressig an antifungal activity in a broad spectrum based on the novel mechanism thereof of 1,6-β-glucan synthesis inhibition, and an antifungal agent containing any of them.
[参考文献]: I Bryndal, Et Al. Molecular And Crystal Structures, Vibrational Studies And Quantum Chemical Calculations Of 3 And 5-Nitroderivatives Of 2-Amino-4-Methylpyridine. Spectrochim Acta A Mol Biomol Spectrosc. 2012 Oct:96:952-62.
合成参考文献
参考文献:10.1055/s-2004-834926 摘要:Yang D, Fokas D, Li J, Yu L, Baldino C. A Versatile Method for the Synthesis of Benzimidazoles from o-Nitroanilines and Aldehydes in One Step via a Reductive Cyclization. Synthesis. 2004 Nov 24;2005(01):47–56. doi: 10.1055/s-2004-834926.