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    • 8. 发明申请
    • PROCESS FOR THE PREPARATION OF 4-AMINO-3-QUINOLINECARBONITRILES
    • 制备4-氨基-3-喹啉酮的方法
    • WO2005019201A3
    • 2005-08-04
    • PCT/US2004026329
    • 2004-08-13
    • WYETH CORPWIGGINS SUTHERLAND KARENFEIGELSON GREGG BRIANBOSCHELLI DIANE HARRISBLUM DAVID MICHAELSTRONG HENRY LEE
    • WIGGINS SUTHERLAND KARENFEIGELSON GREGG BRIANBOSCHELLI DIANE HARRISBLUM DAVID MICHAELSTRONG HENRY LEE
    • C07D215/54C07D405/04C07D495/04
    • C07D405/04C07D215/54C07D495/04
    • This invention discloses a process for the preparation of a 4-amino-3quinolinecarbonitrile comprising combining an amine compound with a cyanoacetic acid and an acid catalyst to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up-to tetra-substituted aniline in an alcoholic solvent and a trialkylorthoformate to yield an 2-amino-2-cyanoacrylamide; combining the 3-amino2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine­6-carbonitrile comprising combining a 3-amino thiophene with a cyanoacetamide and trial kylorthoformate in an alcoholic solvent to obtain a 3-amino2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride and acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile and also discloses a process for the preparation of a 4 amino-3-quinolinecarbonitrile comprising: combining an amine compound with cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension; to yield cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline with an alcoholic solvent to yield a 4-amino-3-quinolinecarbonitrile, and the invention discloses a process for obtaining a cyanoacetamide.
    • 本发明公开了一种制备4-氨基-3-喹啉腈的方法,包括将胺化合物与氰基乙酸和酸催化剂混合以产生氰基乙酰胺; 将氰基乙酰胺与醇溶剂和原甲酸三烷基酯中的任选的上述四取代的苯胺缩合,得到2-氨基-2-氰基丙烯酰胺; 将3-氨基-2-氰基丙烯酰胺与磷酰氯在乙腈,丁腈,甲苯或二甲苯中,任选在催化剂存在下合并,得到4-氨基-3-喹啉腈,并公开了制备7-氨基 - 噻吩并[ 3,2-b]吡啶-6-甲腈,其包括将3-氨基噻吩与氰基乙酰胺组合并在醇溶剂中试验草酸甲酯,得到3-氨基-2-氰基丙烯酰胺; 并将3-氨基-2-氰基丙烯酰胺与磷酰氯和乙腈,丁腈,甲苯或二甲苯组合,任选在催化剂存在下,得到7-氨基 - 噻吩并[3,2-b]吡啶-6-甲腈和 还公开了一种制备4氨基-3-喹啉腈的方法,包括:将胺化合物与氰基乙酸和肽偶联剂混合以获得悬浮液; 过滤悬浮液; 得到氰基乙酰胺; 将氰基乙酰胺与任选至多四取代的苯胺与醇溶剂缩合,得到4-氨基-3-喹啉腈,本发明公开了一种获得氰基乙酰胺的方法。