反应详情

To a stirring solution of N-benzyloxycarbonyl-L-leucine (4.6 g, 17.3 mmol) in THF, cooled to -40° C., was added N-methylmorpholine (3.68 g, 36.4 mmol; 4.0 mL) and isobutyl chloroformate (2.37 g, 17.3 mmol; 2.25 mL). After stirring for 15 min, ammonia was bubbled through the solution for 5 min. The solution was warmed to room temperature, evaporated, and the residue was dissolved in ethyl acetate, washed with 0.1 N Hcl, and saturated brine, then dried (MgSO4), filtered and evaporated to dryness to give the title compound as a white solid (4.58 g, 100%).

1. customammonia was bubbled through the solution for 5 min
2. customevaporated
3. dissolutionthe residue was dissolved in ethyl acetate
4. washwashed with 0.1 N Hcl, and saturated brine
5. dry with materialdried (MgSO4)
6. filtrationfiltered
7. customevaporated to dryness