Sodium hydride → 5-Cyclopropyl-4-((R)-2,2,2-trifluoro-1-methyl-ethoxy)-pyridine-2-carboxylic acid (3-carbamoylmethyl-oxetan-3-yl)-amide

関与物質

反応手順

To a solution of 4-Chloro-5-cyclopropyl-pyridine-2-carboxylic acid (3-carbamoylmethyl-oxetan-3-yl)-amide (Example 63b, 40 mg, 129 μmol) in dry DMF (1.5 mL) in a microwave-vial were added (R)-1,1,1-trifluoropropan-2-ol (CAN 17628-73-8, 42.1 mg, 258 μmol) and sodium hydride 60% (15.5 mg, 387 μmol) and the reaction mixture was stirred at room temperature for 10 minutes. The reaction mixture was heated to 100° C. for 30 minutes under microwave radiation. The reaction was directly purified by preparative HPLC without any work-up to yield the title compound (3.5 mg, 7.0%) as a grey solid. MS (ESI, m/z): 388.0 (M+H+).

情報源と証拠