反应详情

To a solution of 132.8 g (0.65 moles) 1-(+)-(S)-(2-pyridyl)-2-cyclohexylethylamine in 550 mL methylene chloride was added 109 g (0.65 moles) 2-chloro-5-methylbenzoxazole followed by 168 g (1.3 moles) diisopropylethylamine. The reaction mixture was heated to reflux for 5-40 hours, cooled and concentrated under reduced pressure. The mixture was dissolved in 2 L of ethanol. Addition of 2-3 L of water gave crude [(2-cyclohexyl-1-(2-pyridyl)ethylamino]-5-methylbenzoxazole. Recrystallization from ethanol/water gave 190 g (83%) as a hydrate; mp 80°-86° C.

1. temperatureThe reaction mixture was heated
2. temperatureto reflux for 5-40 hours
3. temperaturecooled
4. concentrationconcentrated under reduced pressure
5. dissolutionThe mixture was dissolved in 2 L of ethanol
6. additionAddition of 2-3 L of water