反应详情

温度

100 °C

In a 250 mL round-bottomed flask was placed 4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-6-(isopropylamino)pyrimidin-2-ol (29, 124 mg, 0.469 mmol) in POCl3 (20 ml) to give a yellow solution. The mixture was stirred at 100° C. for 16 h. The mixture was cooled to room temperature, concentrated, diluted with dichloromethane and washed with saturated NaHCO3 followed by 0.2 N NaOH. The organic phase was dried over MgSO4, filtered and concentrated to give the title compound (91 mg, 69%). Aryl chloride 30 could be transformed into aniline 18 as described in scheme 2 for the conversion of 5 into 6. Aniline 18 could be transformed into urea or carbamate compounds as described in scheme 2 (and illustrated in the experimental section for scheme 7).

1. customIn a 250 mL round-bottomed flask was placed
2. temperatureThe mixture was cooled to room temperature
3. concentrationconcentrated
4. additiondiluted with dichloromethane
5. washwashed with saturated NaHCO3
6. dry with materialThe organic phase was dried over MgSO4
7. filtrationfiltered
8. concentrationconcentrated