Piperazin-2-one → [2-(3-Oxopiperazin-1-yl)pyrimidin-5-yl]boronic acid

Participants

Reaction Conditions

Reaction Steps

(2-Chloropyrimidin-5-yl)boronic acid (1.0 g, 6.32 mmol) and piperazin-2-one (1.6 g, 16.0 mmol) were suspended in 1,4-dioxane (10 mL) and the mixture was heated at 100° C. under microwave irradiation for 45 minutes. The supernatant liquid was decanted from the suspension and the residue was triturated with methanol and diethyl ether. The resultant solids were filtered off and dried under vacuum to afford the title compound (706 mg, 30%) as a pale pink solid. Method B HPLC-MS: MH+ m/z 223, RT 0.25 minutes.

Provenance & Evidence