Cyclopentylamine → 3-(1-{[3-(cyclopentylamino)propyl]sulfonyl}-4-piperidinyl)-5-(2-thienyl)-1H-indole-7-carboxamide

Participants

Reaction Steps

Following the general procedure for aminosulfonamide formation outlined in example 2, 3-{1-[(3-chloropropyl)sulfonyl]-4-piperidinyl}-5-(2-thienyl)-1H-indole-7-carboxamide (50 mg, 0.12 mmol) and cyclopentyl amine (54 uL, 0.60 mmol) were allowed to react in the presence of K2CO3 (74 mg, 0.55 mmol) and NaI (Cat. 5 mg) in DMF at 120° C. The resulting residue was purified by reverse phase HPLC eluting with 10% B to 80% B, where A=H2O (0.1% trifluoroacetic acid) and B=CH3CN (0.1% trifluoroacetic acid) to give the title compound (27.2 mg, 44%).

Provenance & Evidence