反应详情

温度

180 °C

3-Amino-6-[3-(hydroxymethyl)phenyl]pyrazine-2-carbonitrile (514.0 mg, 2.27 mmol) and 1,1-dimethylethyl (3S)-3-(hydrazinocarbonyl)piperidine-1-carboxylate (1.66g, 6.83 mmol) were combined together and heated to 180° C. for 1-2 h. The reaction mixture was poured into water (100 mL), and extracted with ethyl acetate (2×35 mL) then dried over anhydrous sodium sulfate and filteration, concentration and purified by MPLC to give 1,1-dimethylethyl (3R)-3-(5-{3-amino-6-[3-(hydroxymethyl)phenyl]pyrazin-2-yl }-1H-1,2,4-triazol-3-yl)piperidine-1-carboxylate. (655.0 mg, 64.2% yield): MS (EI) for C23H29N7O3: 452.29 (MH+).

1. extractionextracted with ethyl acetate (2×35 mL)
2. dry with materialthen dried over anhydrous sodium sulfate and filteration, concentration
3. custompurified by MPLC