反应详情

To a well stirred solution of tert-butyl 4-(3-chloropyrazin-2-yl)piperidine-1-carboxylate (92 g, 0.309 mol, 1 eq.) in dichloromethane (1 L) was added trifluoroacetic acid (119 mL, 1.545 mol, 5 eq.). The resulting mixture was heated to reflux overnight (16 h). The mixture was concentrated and the resulting TFA salt was dried with toluene (500 mL) azetropically to give 150 g 2-chloro-3-(piperidin-4-yl)pyrazine. This was used in the next step without further purification.

1. temperatureThe resulting mixture was heated
2. temperatureto reflux overnight (16 h)
3. concentrationThe mixture was concentrated
4. dry with materialthe resulting TFA salt was dried with toluene (500 mL) azetropically