反应详情

(R)-Alaninol (107.3 g, 1.43M) was added dropwise with stirring to a solution of potassium tertiary butoxide (160 g, 1.43M) in tetrahydrofuran (1L). After the exothermic reaction had cooled to room temperature, 2-chloropyridine (162.4 g, 1.43M) was added dropwise. The reaction mixture was heated under reflux overnight, cooled, filtered and evaporated to an oil. The oil was dissolved in xylene (1,5L) and toluene-p-sulphonic acid (0.5 g) was added. The mixture was heated under reflux overnight. On cooling to room temperature the product crystallised to give (R)-N-(2-pyridyl)-2-aminopropanol (190 g), [α]D26 =30° (c=1 in CHCl3).

1. customAfter the exothermic reaction
2. temperatureThe reaction mixture was heated
3. temperatureunder reflux overnight
4. temperaturecooled
5. filtrationfiltered
6. customevaporated to an oil
7. dissolutionThe oil was dissolved in xylene (1,5L)
8. additiontoluene-p-sulphonic acid (0.5 g) was added
9. temperatureThe mixture was heated
10. temperatureunder reflux overnight
11. temperatureOn cooling to room temperature the product
12. customcrystallised