N-Methylsulfamoyl chloride → N-methyl-N'-{4-[3-(morpholin-4-yl)quinoxalin-6-yl]phenyl}sulfuric diamide

Participants

Reaction Steps

A mixture of 4-(3-morpholin-4-yl-quinoxalin-6-yl)-phenylamine [Intermediate Example 4.1] (100 mg) and pyridine (0.5 mL) was treated with a solution of methylsulfamyl chloride (75 mg, 0.65 mmol) in pyridine (0.6 mL) and stirred at room temperature overnight. The reaction was partitioned between dichloromethane and water, the phases separated and the organic layer concentrated in vacuo. The residue was purified by preparative reverse phase HPLC to give the title compound (30 mg), contaminated by ca. 20% formic acid.

Provenance & Evidence