发明授权
US5066803A 2- and
3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin
es
失效
2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪
- 专利标题: 2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin es
- 专利标题(中): 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪
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申请号: US509441申请日: 1990-04-16
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公开(公告)号: US5066803A公开(公告)日: 1991-11-19
- 发明人: Thomas E. D'Ambra , Malcolm R. Bell
- 申请人: Thomas E. D'Ambra , Malcolm R. Bell
- 申请人地址: NY New York
- 专利权人: Sterling Drug Inc.
- 当前专利权人: Sterling Drug Inc.
- 当前专利权人地址: NY New York
- 主分类号: C07D265/36
- IPC分类号: C07D265/36 ; C07D498/06 ; C07D505/00
摘要:
2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.