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6-hydroxy-5-methyl-2-(pyridin-2-yl)-3,4-dihydropyrimidin-4-one synthesis

1synthesis methods
-

Yield:10198-75-1 69%

Reaction Conditions:

with sodium methylate in methanol; for 0.666667 h;Reflux;

Steps:

A Step A

NaOMe (4.46 g, 82.64 mmol) was added to a solution of diethyl 2- methylmalonate 26 (14.34 g, 82.64 mmol) and pyridine-2-carboxamidine 23 (10 g, 82.64 mmol) in MeOH (200 ml). The reaction mixture was heated under reflux for 40 mm resulting in the formation of a precipitate. The reaction mixture was diluted with MeOH (100 ml) and EtOAc (200 ml) and the precipitate was triturated and collected by filtration to give 27 (11.57 g, 57 mmol, 69 % yield).

References:

WO2018/237084,2018,A1 Location in patent:Paragraph 002091