发明授权
US5693800A N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide and a process for its
preparation
失效
N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺及其制备方法
- 专利标题: N-(2-amino-4,6-dichloropyrimidine-5-yl) formamide and a process for its preparation
- 专利标题(中): N-(2-氨基-4,6-二氯嘧啶-5-基)甲酰胺及其制备方法
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申请号: US693521申请日: 1996-08-08
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公开(公告)号: US5693800A公开(公告)日: 1997-12-02
- 发明人: Gerhard Stucky , Rene Imwinkelried
- 申请人: Gerhard Stucky , Rene Imwinkelried
- 申请人地址: CHX Basel
- 专利权人: Lonza AG
- 当前专利权人: Lonza AG
- 当前专利权人地址: CHX Basel
- 优先权: CHX01299/94 19940427
- 主分类号: A61K31/70
- IPC分类号: A61K31/70 ; A61P31/12 ; C07D239/48
摘要:
A novel pyrimidine derivative, N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide for use, e.g., in the production of antiviral nucleotide derivatives, can be made by a process involving cyclyzing an aminomalonic ester with guanidine or its salt in the presence of a base to produce 2,5-diamino-4,6-dihydroxypyrimidine or its salt, chlorinating this product with a chlorinating agent in the presence of an amide to produce 4,6-dichloropyrimidine, and reacting the 4,6-dichloropyrimidine with an aqueous solution of a carboxylic acid to produce the N-(2-amino-4,6-dichloropyrimidine-5-yl)formamide. Novel also are 4,6-dichloropyrimidine, 4,6-dichloro-N'-(dimethylaminomethylene)pyrimidine-2,5-diamine, 4,6-dichloro-N'-(piperidine-1-ylmethylene)pyrimidine-2,5-diamine, and a process for making 2,5-diamino-4,6-dichloropyrimidine of the formula ##STR1##
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