Citric Acid → HCID 44544416, compound

Participants

Reaction Steps

To the solution of (6S,9S)—N-benzyl-6-(4-hydroxybenzyl)-2,9-dimethyl-4,7-dioxo-8-(quinolin-8-ylmethyl)octahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide (Compound 1-5) 325 mg (0.43 mmol) and TEA 179 μl (1.29 mmol) in tetrahydrofuran 6 ml, phosphoryl chloride 200 μl (2.15 mmol) was added at 0° C. and stirred at room temperature for 4 hours. Water was added to the reaction mixture and stirred additional overnight. The reaction mixture was acidified with 10%-citric acid 30 ml and extracted with chloroform 150 ml. The organic phase was dried with magnesium sulfate and filtered. The filtrate was concentrated in vacuo to obtain the title compound 179 mg (60%).

Provenance & Evidence