Process for the preparation of pyrimidine compounds
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United States of America Patent
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Sep 25, 2012
Grant Date -
Oct 22, 2009
app pub date -
Mar 16, 2009
filing date -
Dec 16, 2002
priority date (Note) -
Expired
status (Latency Note)
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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.
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