Sulfamide → 1-(4-Fluoro-phenyl)-1,4-dihydro-2H-3-thia-2,4,5-triaza-phenanthrene 3,3-dioxide

Participants

Reaction Steps

(8-Amino-quinolin-7-yl)-(4-fluoro-phenyl)-methanone 367 (100 mg, 0.38 mmol) and sulfamide (361 mg, 3.76 mmol) in pyridine (3 ml) and were heated in a microwave at 140° C. for 2 h. After cooling, the mixture was concentrated in vacuo. The residue was dissolved in anhydrous THF (5 ml). LiAlH4 (26 mg, 0.75 mmol) was added and the mixture was stirred at room temperature for 18 h. The reaction was quenched with water (5 ml) and the resulting precipitate was collected by filtration and dried. The crude solid was purified by preparative HPLC (acidic conditions 1) to give the title compound (27 mg, 22%).

Provenance & Evidence