反应详情

2-Chloro-5-carboxy-6H-thieno[3,2-b]pyrrole (Method 4a, 5.0 g, 25.0 mmol), trans-2-amino-1-[(1,1-dimethylethoxy)carbonylamino]indan (Method 6, 6.25 g, 25.0 mmol), DIPEA (4.35 mL, 25.0 mmol) and HOBT (3.4 g, 25.0 mmol) were dissolved in DCM (200 mL) and stirred for 5 mins. EDCI (6.0 g, 31.0 mmol) was added, the reaction stirred for 24 hours and evaporated under reduced pressure. EtOAc (150 mL) was added and the mixture filtered, washed with water (2×200 mL), brine (200 mL), dried (MgSO4) and the volatiles removed by evaporation under reduced pressure to give the title compound (10.6 g, 98%) as a brown solid.

1. stirringthe reaction stirred for 24 hours
2. customevaporated under reduced pressure
3. additionEtOAc (150 mL) was added
4. filtrationthe mixture filtered
5. washwashed with water (2×200 mL), brine (200 mL)
6. dry with materialdried (MgSO4)
7. customthe volatiles removed by evaporation under reduced pressure