Triethylamine → HCID 9836721, compound

Participants

Reaction Conditions

Reaction Steps

Under Ar, the mixture of cyclobutanecarboxylic acid (250 mg, 2.50 mmol), diphenylphosphoryl azide (756 mg, 2.74 mmol), and triethyl amine (0.38 mL, 2.74 mmol) in 3 mL of N,N-dimethyl-formamide was heated to 80° C. for 2 hours. The mixture was cooled to room temperature, 3-amino-6-chloro-2hydroxybenzenesulfonamide (556 mg, 2.50 mmol) was added. The resulting mixture was stirred at room temperature for 20 hours. Purification upon Gilson HPLC, eluting with acetonitrile/water (10/90, v/v to 90/10, v/v, over 10 min), gave the desired product (137 mg, 17%). LC-MS (m/z) 320.0 (M+).

Provenance & Evidence