Triethylamine → HCID 9966285, compound

Participants

Reaction Conditions

Reaction Steps

Under Ar, the mixture of cyclopropanecarboxylic acid (500 mg, 5.81 mmol), diphenylphosphoryl azide (1.58 g, 5.81 mmol), and triethyl amine (0.81 mL, 5.8 mmol) in 3 mL of N,N-dimethyl-formamide was heated to 80° C. for 3 hours. The mixture was cooled to room temperature, 3-amino-6-chloro-2-hydroxybenzenesulfonamide (200 mg, 0.89 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 (74 mg, 27%). LC-MS (m/z) 306.2 (M+).

Provenance & Evidence