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7-Methyl-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxylic acid ethyl ester synthesis

6synthesis methods
-

Yield:5435-82-5 58%

Reaction Conditions:

with 1,8-diazabicyclo[5.4.0]undec-7-ene in acetonitrile at 150; for 0.333333 h;Microwave (CEM);

Steps:

236.1

A mixture of diethyl 2-(ethoxymethylene)malonate (0.60 g, 3 mmol), 5-methylpyridin-2-amine (0.20 g, 2 mmol), DBU (0.1 ml, 0.9 mmol) in acetonitrile (2 g, 49 mmol) was heated under Microwave (CEM) at 1500C (150 W) for 20 min. The resultant was diluted with dichloromthane and water, and the organic layer was dried over sodium sulfate. The organic solution was concentrated, and the residue was crystallized in dichloromethane and diethyl ether to give the title compound as a pale yellow solid (0.25 g, 58 %): MS (ESI pos. ion) m/z: 233 (MH+). Calc'd exact mass for Ci2H12N2O3: 232.

References:

WO2006/116713,2006,A1 Location in patent:Page/Page column 208