Invention Grant
- Patent Title: Process for the preparation of pyrimidine compounds
- Patent Title (中): 嘧啶化合物的制备方法
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Application No.: US12404575Application Date: 2009-03-16
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Publication No.: US08273878B2Publication Date: 2012-09-25
- Inventor: Lee Newton , Mark Bailey
- Applicant: Lee Newton , Mark Bailey
- Applicant Address: GB London
- Assignee: AstraZeneca UK Limited
- Current Assignee: AstraZeneca UK Limited
- Current Assignee Address: GB London
- Agency: Morgan, Lewis & Bockius LLP
- Priority: GB0229243.1 20021216; GB0303589.6 20030217; GB0318515.4 20030807
- Main IPC: C07D239/02
- IPC: C07D239/02

Abstract:
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.
Public/Granted literature
- US20090264654A1 PROCESS FOR THE PREPARATION OF PYRIMIDINE COMPOUNDS Public/Granted day:2009-10-22
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