Trifluoroacetic acid → Trifluoroacetic acid

Participants

Reaction Steps

5-(benzyloxy)-2-[4-(methylsulfonyl)piperazin-1-yl]pyrimidine (57.9 g, 0.17 mol) was dissolved in TFA (600 mL) and the reaction heated to reflux, with stirring, for 7 hours then cooled to room temperature. The TFA was then in vacuo and the residue azeotroped with toluene (2×300 mL). The resulting solid was triturated with DCM, filtered off, washed with ether and dried to give 2-[4-(methylsulfonyl)piperazin-1-yl]pyrimidin-5-ol as a pale yellow solid (54.4 g, 0.15 mol, 88%, TFA salt).

Provenance & Evidence