反应详情

To a solution of 5-chloro-1-ethylindole (6.17 g) and methyl (2R,3R)-N-benzyloxycarbonyl-3-methyl-2-aziridinecarboxylate (9.87 g) in dry methylene chloride (100 ml) which was cooled on an ice bath, was added boron trifluoride etherate (4 ml). The mixture was stirred for five minutes and washed with saturated sodium bicarbonate solution, treated with active charcoal, and dried over magnesium sulfate. After removal of the solvent, the crude residue was chromatographed on silica gel (100 g) (toluene as eluent) to give (αR,βR)-N-benzyloxycarbonyl-5-chloro-1-ethyl-β-methyltryptophan methyl ester (4.17 g) as an oil.

1. washwashed with saturated sodium bicarbonate solution
2. additiontreated with active charcoal
3. dry with materialdried over magnesium sulfate
4. customAfter removal of the solvent
5. customthe crude residue was chromatographed on silica gel (100 g) (toluene as eluent)