Tetrahydrofuran → 3-Benzyloxy-7-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylic acid (2-oxo-2-phenyl-ethyl)-amide

Participants

Reaction Steps

To a stirred solution of the product from Example 8.2 (324 mg, 1 mmol) in tetrahydrofuran (15 mL) at room temperature, was added the product from Example 12.1 (162 mg, 1.2 mmol), 1-hydroxybenzotriazole (162 mg, 1.2 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (191 mg, 1 mmol) and triethylamine (112 mg, 1.1 mmol) successively. After 3 h the reaction solution was quenched with of saturated aqueous sodium bicarbonate solution (5 mL). The mixture was extracted with ethyl acetate and the organic phase washed with water, brine then dried over (Na2SO4) and concentrated in vacuo. Flash chromatography of the residue afforded the desired product (215 mg, 45%).

Provenance & Evidence