发明授权
US07479558B2 Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives
失效
制备吡啶并[2,3-d]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-d]嘧啶-2(1H) - 酮衍生物的方法
- 专利标题: Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives
- 专利标题(中): 制备吡啶并[2,3-d]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-d]嘧啶-2(1H) - 酮衍生物的方法
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申请号: US11388375申请日: 2006-03-24
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公开(公告)号: US07479558B2公开(公告)日: 2009-01-20
- 发明人: James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
- 申请人: James F. Callahan , Jeffrey C. Boehm , Zehong Wan , Hongxing Yan , Xichen Lin
- 申请人地址: GB Greenford, Middlesex
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB Greenford, Middlesex
- 代理商 Dara L. Dinner; Stephen Venetiner; Charles M. Kinzig
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; C07D239/30 ; C07D413/04 ; C07D471/04
摘要:
The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.
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