反应详情

Ethyl 3-[(4-fluorobenzoyl)amino]-6,6-dimethyl-5,6-dihydropyrrolo[3,4-c]pyrazole-1(4H)-carboxylate hydrochloride (2.0 g, 5.77 mmol) in dichloromethane (70 ml) was treated, at 0° C., with N,N-diisopropylethylamine (1.6 ml, 9.2 mmol, 1.6 eq) and with pivaloyl chloride (780 μL, 6.3 mmol, 1.1 eq). Gradually, the reaction was brought to room temperature and stirred overnight (TLC: CH2Cl2/EtOAc 90/10). The solution was washed with saturated sodium hydrogencarbonate aqueous solution and brine. The organic phase was dried over sodium sulfate, evaporated and purified by flash chromatography (eluent: CH2Cl2/EtOAc 90/10) to afford 2.03 g of the title compound in 82% yield.

1. customwas brought to room temperature
2. washThe solution was washed with saturated sodium hydrogencarbonate aqueous solution and brine
3. dry with materialThe organic phase was dried over sodium sulfate
4. customevaporated
5. custompurified by flash chromatography (eluent: CH2Cl2/EtOAc 90/10)