3-Amino-5-chlorothiophene-2-sulfonamide → 5-Hydroxy-2-(3-methyl-butyl)-3-oxo-6-thiophen-2-yl-2,3-dihydro-pyridazine-4-carboxylic acid (5-chloro-2-sulfamoyl-thiophen-3-yl)-amide

Participants

Reaction Conditions

Reaction Steps

The ester (13a) made by Method 4 (86 mg, 0.26 mmol) and 3-Amino-5-chloro-thiophene-2-sulfonic acid amide (14b) (54 mg, 0.26 mmol) were mixed in a reaction vial and stirred in a preheated oil-bath at 160° C. for 10 mins to give the corresponding 5-hydroxy-2-(3-methyl-butyl)-3-oxo-6-thiophen-2-yl-2,3-dihydro-pyridazine-4-carboxylic acid (5-chloro-2-sulfamoyl-thiophen-3-yl)-amide (15a) as a dark yellow solid which was used directly in next step without further purification. LC-MS (ESI+): m/e=503.09 [M+1]+(exact ms: 502.02).

Provenance & Evidence