反应详情

2-(3,3-Dicyclohexyl-ureido)-thiazole-5-carboxylic acid (53 mg, 0.15 mmol), piperazine sulfonic acid dimethylamide hydrochloride (44 mg, 0.19 mmol), and HBTU (74 mg, 0.19 mmol) were weighed out and added to a 10 mL reaction flask. DMF (1.5 mL) and DIEA (65 μL, 0.38 mmol) were added. The reaction was stirred under nitrogen at ambient temperature overnight. The reaction was diluted with EtOAc (5 mL) and quenched with saturated aqueous NH4Cl (5 mL). After separation and extraction with EtOAc (2×5 mL) the combined organic portions were dried over MgSO4. Purification with silica gel (10% EtOAc and 1% MeOH in CH2Cl2) afforded 53 mg (67%) of the desired compound.

1. additionadded to a 10 mL reaction flask
2. customquenched with saturated aqueous NH4Cl (5 mL)
3. customAfter separation and extraction with EtOAc (2×5 mL) the combined organic portions
4. dry with materialwere dried over MgSO4
5. customPurification with silica gel (10% EtOAc and 1% MeOH in CH2Cl2)