申请人:Allergan, Inc.
公开号:US05171863A1
公开(公告)日:1992-12-15
Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons; X is H, OH, NH.sub.2, I or Br; R.sub.4 is H, alkyl of 1-20 carbons, phenyl[C.sub.1 -C.sub.20 alkyl], naphthyl[C.sub.1 -C.sub.20 alkyl], CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, CH.sub.2 --COOH or CH.sub.2 --COOR.sub.5, and R.sub.5 is alkyl of 1 to 6 carbons, with the proviso that when X is hydrogen then R.sub.4 is selected from the group consisting of CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, or CH.sub.2 --COOR.sub.5 ; ##STR2## in which R.sub.1, R.sub.2 R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.sub.5 is alkyl of 1 to 6 carbons; ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.sub.6 is phenyl, or alkyl of 1 to 6 carbons, and ##STR4## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons.
抗炎4-取代2-呋喃酮是由中间体制备而成,其化学式如下:##STR1## 其中,R.sub.1、R.sub.2和R.sub.3独立地是1到6个碳的n-烷基,或者是1到6个碳的支链烷基;X是H、OH、NH.sub.2、I或Br;R.sub.4是H、1-20个碳的烷基、苯基[C.sub.1-C.sub.20烷基]、萘基[C.sub.1-C.sub.20烷基]、CH.sub.2 OH、CH.sub.2 NH.sub.2、CH.sub.2 CH.sub.2 OH、CH.sub.2 --CHO、CH.sub.2 --COOH或CH.sub.2 --COOR.sub.5,其中R.sub.5是1到6个碳的烷基,但是当X是氢时,R.sub.4的选择范围包括CH.sub.2 OH、CH.sub.2 NH.sub.2、CH.sub.2 CH.sub.2 OH、CH.sub.2 --CHO或CH.sub.2 --COOR.sub.5;##STR2## 其中,R.sub.1、R.sub.2和R.sub.3独立地是1到6个碳的n-烷基,或者是1到6个碳的支链烷基,而R.sub.5是1到6个碳的烷基;##STR3## 其中,R.sub.1、R.sub.2和R.sub.3独立地是1到6个碳的n-烷基,或者是1到6个碳的支链烷基,而R.sub.6是苯基或1到6个碳的烷基;##STR4## 其中,R.sub.1、R.sub.2和R.sub.3独立地是1到6个碳的n-烷基,或者是1到6个碳的支链烷基。