Process for the preparation of pyrimidine compounds
US7524955B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Dec 9, 2003 |
| Grant date | Apr 28, 2009 |
| Priority date | — |
| Expiry date | Dec 3, 2025 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D403/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
A process for the preparation of a compound of Formula (I) 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 oxidising the dihydropyrimidine to form the compound of Formula (1). 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, and aryl group or an electron withdrawing group; and X1 and X2 are each independently leaving groups, or X1 and X2 together represent ═O.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.