p-Toluenesulfonic acid → 9-Methyl-2-propyl-4H-pyrido[1,2-a]pyrimidin-4-one

反応式

[NH2:1][C:2]1[C:7]([CH3:8])=[CH:6][CH:5]=[CH:4][N:3]=1.[C:9]([CH2:14][C:15](OC)=[O:16])(=O)[CH2:10][CH2:11][CH3:12].C1(C)C=CC(S(O)(=O)=O)=CC=1>COCCO>[CH3:8][C:7]1[C:2]2=[N:1][C:9]([CH2:10][CH2:11][CH3:12])=[CH:14][C:15](=[O:16])[N:3]2[CH:4]=[CH:5][CH:6]=1

参加物

反応条件

温度: -30 °C

実験手順

A solution of 54.0g of 2-amino-3-methylpyridine, 144.0g of methyl butyrylacetate, 5.0g of p-toluenesulfonic acid, and 750ml of ethylene glycol monomethyl ether is heated in a nitrogen atmosphere, under reflux, for 60 hours. The solution is concentrated to dryness in vacuo, and the residual oil extracted with two 250ml portions of pentane. The pentane solution is concentrated to a volume of 250ml and cooled at -30°C to yield the title compound, melting point 59°-60°C.