发明授权
- 专利标题： Process for the preparation of 9-deazaguanine derivatives
- 专利标题（中）： 9-脱氮鸟嘌呤衍生物的制备方法
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申请号： US10878035申请日： 2004-06-29
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公开(公告)号： US06946554B2公开(公告)日： 2005-09-20
- 发明人: Arthur J. Elliott , David A. Walsh , Philip E. Morris
- 申请人： Arthur J. Elliott , David A. Walsh , Philip E. Morris
- 申请人地址： US AL Birmingham
- 专利权人： BioCryst Pharmaceuticals, Inc.
- 当前专利权人： BioCryst Pharmaceuticals, Inc.
- 当前专利权人地址： US AL Birmingham
- 代理机构： Connolly, Bove, Lodge & Hutz, LLP
- 主分类号： A61K31/519
- IPC分类号： A61K31/519 ; A61K31/5377 ; A61K31/541 ; C07D487/04 ; C07D207/34
摘要：
Derivatives of 9-deazaguanine of the formula I: are prepared by reacting an aldehyde or ketone of the formula II: with a dialkylaminomalonate to produce an enamine. The enamine is then reacted with a base to produce a pyrrole represented by the formula: The pyrrole is reacted with a compound represented by the formula R3OC(O)N═C(Z)NHC(O)OR3 or a derivative of carbamimidoic acid to provide a protected guanidine compound. The guanidine compound is converted to the desired deazaguanine by reaction with 1) trifluoracetic acid or 2) C1-C4 alkoxide or alkali metal or alkaline earth metal hydroxide followed by neutralization with an acid.
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