反应详情

5-Carboxy-2,3-dichloro-4H-thieno[3,2-b]pyrrole (Method 4, 236 mg, 1.0 mmol), N-[(1S,2S)-2-amino-2,3-dihydro-1H-inden-1-yl]methanesulfonamide (226 mg, 1.0 mmol), DIPEA (174 μL, 1.0 mmol) and HOBT (135 mg, 1.0 mmol) were dissolved in DCM (10 mL) and stirred for approximately 5 mins. EDCI (240 mg, 1.25 mmol) was added and the reaction stirred for 20 hours. The volatiles were removed by evaporation, EtOAc (25 mL) added, the mixture washed with water (2×10 mL) and brine (10 mL) and dried (MgSO4). The volatiles were removed by evaporation under reduced pressure to give the title compound (430 mg, 97%) as a foam.

1. stirringthe reaction stirred for 20 hours
2. customThe volatiles were removed by evaporation, EtOAc (25 mL)
3. additionadded
4. washthe mixture washed with water (2×10 mL) and brine (10 mL)
5. dry with materialdried (MgSO4)
6. customThe volatiles were removed by evaporation under reduced pressure