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69050-79-9

2,6-di-tert-butylpyrimidin-4(3H)-one synthesis

1synthesis methods
-

Yield:-

Reaction Conditions:

Stage #1: pivalamidine hydrochloridewith sodium methylate in methanol;ethanol at 20; for 0.5 h;
Stage #2: Methyl 4,4-dimethyl-3-oxopentanoate in methanol;ethanol at 78; for 3 h;

Steps:

25.1

2,2-Dimethylpropanimidamide hydrochloride (1.0 g, 7.3 mmol) was dissolved in ethyl alcohol (18 mL), sodium methoxide (0.5 M in methanol, 29 mL) added and the solution stirred at RT for 30 minutes. Methyl 4,4-dimethyI-3-oxovalerate (1.2 g, 7.3 mmol) was added and the solution stirred at 78 0C for 3 hours. The mixture was cooled to RT, poured into water (500 mL), acidified with acetic acid, followed by aqueous/EtOAc work-up to afford the titled compound.

References:

WO2007/64553,2007,A2 Location in patent:Page/Page column 70