反应详情

(R)-(−)-Spiro[1-azabicyclo[2.2.2]octane-3,2′ (3′H)-furo[2,3-b]pyridine] (3.03 g, 14 mmol) was dissolved in concentrated sulfuric acid (7 ml) at 0–5° C., fuming nitric acid (3.3 ml, 70.2 mmol) was added over 10 minutes, the mixture was stirred for 1 hour, and heated at 65–70° C. for 24 hours, cooled, poured onto ice (200 g), added 300 ml of water, basified to pH 10 with solid potassium carbonate, stirred for 1 hour, filtered off and dried, provided the solid title compound (3.6 g, 13.8 mmol, 98%): electrospray MS 262 ([MH]+, 100).

1. temperatureheated at 65–70° C. for 24 hours
2. temperaturecooled
3. additionpoured onto ice (200 g)
4. stirringstirred for 1 hour
5. filtrationfiltered off
6. customdried