反应详情

3,4-Dichloro-5-methyl-N-piperidin-4-yl-1H-pyrrole-2-carboxamide hydrochloride (Intermediate 1; 1 g, 3.2 mmol) was dissolved in NMP (10 ml). Bromothiazole (2.65 g; 16 mmol) was added followed by the addition of N,N-diisopropylethylamine (2.75 ml, 16 mmol). Using a Smith Microwave Synthesizer, the mixture was subjected to single-mode microwave at 150° C. for a total of 3 h. The mixture was diluted with EtOAc and washed well with water, NaHCO3, brine. The organic phase was dried over Na2SO4 and concentrated in vacuo to give the title compound as a brown solid (692 mg).

1. customat 150° C.
2. customfor a total of 3 h
3. washwashed well with water, NaHCO3, brine
4. dry with materialThe organic phase was dried over Na2SO4
5. concentrationconcentrated in vacuo