发明申请
- 专利标题: Process for preparation of 4-amino-3-quinolinecarbonitriles
- 专利标题(中): 制备4-氨基-3-喹啉碳腈的方法
-
申请号: US10918947申请日: 2004-08-16
-
公开(公告)号: US20050043537A1公开(公告)日: 2005-02-24
- 发明人: Karen Sutherland , Gregg Feigelson , Diane Boschelli , David Blum , Henry Strong
- 申请人: Karen Sutherland , Gregg Feigelson , Diane Boschelli , David Blum , Henry Strong
- 申请人地址: US NJ Madison
- 专利权人: Wyeth Holdings Corporation
- 当前专利权人: Wyeth Holdings Corporation
- 当前专利权人地址: US NJ Madison
- 主分类号: C07D215/54
- IPC分类号: C07D215/54 ; C07D405/04 ; C07D495/04 ; C07D215/38
摘要:
This invention discloses a process for the preparation of a 4-amino-3-quinolinecarbonitrile 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 a 3-amino-2-cyanoacrylamide; combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride in acetonitrile, butyronitrile, toluene or xylene, optionally in the presence of a catalyst to yield a 4-amino-3-quinolinecarbonitrile and also discloses a process for the preparation of a 7-amino-thieno[3,2-b]pyridine-6-carbonitrile comprising combining a disubstituted 3-amino thiophene with a cyanoacetamide and trialkylorthoformate in an alcoholic solvent to obtain a 3-amino-2-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 by combining an amine compound with a cyanoacetic acid and a peptide coupling reagent to obtain a suspension; filtering the suspension to yield a cyanoacetamide; condensing the cyanoacetamide with an optionally up to tetra-substituted aniline, an alcoholic solvent, and triethylorthoformate to yield a 3-amino-2-cyanoacrylamide; and combining the 3-amino-2-cyanoacrylamide with phosphorus oxychloride to yield a 4-amino-3-quinolinecarbonitrile.
公开/授权文献
- US07297795B2 Process for preparation of 4-amino-3-quinolinecarbonitriles 公开/授权日:2007-11-20