发明授权
- 专利标题: Process for the preparation of pyrimidine compounds
- 专利标题(中): 嘧啶化合物的制备方法
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申请号: US12404575申请日: 2009-03-16
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公开(公告)号: US08273878B2公开(公告)日: 2012-09-25
- 发明人: Lee Newton , Mark Bailey
- 申请人: Lee Newton , Mark Bailey
- 申请人地址: GB London
- 专利权人: AstraZeneca UK Limited
- 当前专利权人: AstraZeneca UK Limited
- 当前专利权人地址: GB London
- 代理机构: Morgan, Lewis & Bockius LLP
- 优先权: GB0229243.1 20021216; GB0303589.6 20030217; GB0318515.4 20030807
- 主分类号: C07D239/02
- IPC分类号: C07D239/02
摘要:
A process for the preparation of a compound of Formula (1) and intermediates useful therein are provided. The process comprises reacting a compound of formula R1—CO—CH2-E with a compound of formula R2—CHX1X2 in the presence of a compound of formula R3R4N—C(═NH)NH2 and a catalyst, thereby to form a dihydropyrimidine; and oxidizing the dihydropyrimidine to form the compound of Formula (I). R1 is H or an alkyl group; R2 is H, an alkyl or aryl group; R3 and R4 are each independently H, alkyl or aryl, or R3 and R4 are linked to form, together with the nitrogen to which they are attached to form a 5 to 7 membered heterocyclic ring; E is H, an unsubstituted alkyl group, an aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ═O.
公开/授权文献
- US20090264654A1 PROCESS FOR THE PREPARATION OF PYRIMIDINE COMPOUNDS 公开/授权日:2009-10-22
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