1,4-Diazepan-5-one → [2-(5-Oxo-1,4-diazepan-1-yl)pyrimidin-5-yl]boronic acid

Participants

Reaction Conditions

Reaction Steps

(2-Chloropyrimidin-5-yl)boronic acid (200 mg, 1.26 mmol) and 1,4-diazepan-5-one (288.34 mg, 2.53 mmol) were suspended in 1,4-dioxane (3 mL) and the mixture was heated at 100° C. under microwave irradiation for 45 minutes. The resulting slurry was concentrated under vacuum and triturated with MeOH to afford the title compound (145 mg, 30%) as a cream precipitate, which was used without further purification. Method C HPLC-MS: MH+ m/z 237, RT 0.40 minutes.

Provenance & Evidence