Pyridine → Water TFA acetonitrile

Participants

Reaction Steps

To 2-(4-fluorobenzyl)-9-hydroxy-7-(morpholin-3-ylmethyl)-3,4-dihydro-2H-pyrazino[1,2-c]pyrimidine-1,6,8(7H)-trione mono TFA salt (72 mg, 0.14 mmol, Example 17) dissolved in dry methylene chloride (1 mL) was added pyridine (13 μL, 0.17 mmol) and acetic anhydride (28 mg, 0.28 mmol). The reaction was stirred overnight at room temperature. The reaction was purified by prep HPLC using a C18 stationary phase and a water/acetonitrile/TFA gradient to obtain the title compound as a white powder after lyophilization from dioxane. High Resolution FT-ICR C21H23FN4O6+H=447.1677; calculated 447.1675.

Provenance & Evidence