发明公开
EP0496064A1 Process for the preparation of substituted benzofuran derivatives
失效
维尔法赫尔（Zur Herstellung）取代物Benzofuranderivate。
- 专利标题： Process for the preparation of substituted benzofuran derivatives
- 专利标题（中）： 维尔法赫尔（Zur Herstellung）取代物Benzofuranderivate。
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申请号： EP91121073.0申请日： 1991-12-09
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公开(公告)号： EP0496064A1公开(公告)日： 1992-07-29
- 发明人: Bedeschi, Angelo , Cabri, Walter , Candiani, Ilaria , de Bernardinis, Silvia , Marchi, Marcello
- 申请人： PHARMACIA S.p.A.
- 申请人地址： Via Robert Koch, 1.2 I-20152 Milano IT
- 专利权人： PHARMACIA S.p.A.
- 当前专利权人： PHARMACIA S.p.A.
- 当前专利权人地址： Via Robert Koch, 1.2 I-20152 Milano IT
- 代理机构： Giambrocono, Alfonso, Dr. Ing.
- 优先权： GB9028105 19901227
- 主分类号： C07D405/12
- IPC分类号： C07D405/12 ; C07D453/02 ; C07D451/04 ; C07D451/14 ; C07D455/02 ; C07D453/06 ; C07D471/08 ; C07D307/84
摘要：
The present invention relates to a process for the preparation of a compound of the following formula (I)
wherein
one of R₁ and R₂ is hydrogen or halogen and the other is independently, an amino group or a C₂-C₄ alkanoyl amino group;
R₃ is hydrogen; a linear or branched alkyl, C₁-C₄ alkoxy or C₂-C₄ alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C₁-C₄ alkyl group;
A is a group -(CH₂) n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms and n is zero or an integer of 1 to 3; and the symbol .... ¯ represents a single or double bond and the pharmaceutically acceptable salts thereof.
The compounds of the invention can be useful as 5HT3 receptor antagonists.
wherein
one of R₁ and R₂ is hydrogen or halogen and the other is independently, an amino group or a C₂-C₄ alkanoyl amino group;
R₃ is hydrogen; a linear or branched alkyl, C₁-C₄ alkoxy or C₂-C₄ alkoxycarbonyl group; halogen; or phenyl unsubstituted or substituted by a C₁-C₄ alkyl group;
A is a group -(CH₂) n -Het wherein Het is an optionally substituted heteromonocyclic or heterobicyclic ring containing one or two nitrogen atoms and n is zero or an integer of 1 to 3; and the symbol .... ¯ represents a single or double bond and the pharmaceutically acceptable salts thereof.
The compounds of the invention can be useful as 5HT3 receptor antagonists.
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