1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → Tert-butyl((1r,2r)-2-{[(2,3-dichloro-4h-thieno[3,2-b]pyrrol-5-yl)carbonyl]amino}-2,3-dihydro-1h-inden-1-yl)methylcarbamate

Participants

Reaction Steps

5-Carboxy-2,3-dichloro-4H-thieno[3,2-b]pyrrole (Method 4, 472 mg, 2.0 mmol), tert-butyl[(1R,2R)-2-amino-2,3-dihydro-1H-inden-1-yl]methylcarbamate (Method 13; 524 mg, 2.0 mmol), DIPEA (348 μL, 2.0 mmol), HOBT (270 mg, 2.0 mmol) and EDCI (480 mg, 2.5 mmol) were dissolved in DCM (10 mL) and stirred at ambient temperature for 20 hours. The volatiles were removed by evaporation under reduced pressure, the residue dissolved in EtOAc (50 mL), washed with water (3×25 mL), brine (25 mL) and dried (MgSO4). The volatiles were removed by evaporation under reduced pressure to give the title compound (900 mg, 93%) as a pale brown foam.

Provenance & Evidence