反应详情

275 mg 8-tert-Butyl-3,4-dihydro-benzo[e][1,4]diazepin-5-one was dissolved in 5 mL methanol. Sodium cyanoborohydride (139 mg, 2 mmol, 2 eq) was added and the reaction was stirred for 16 hours. The reaction was quenched with water, extracted ethyl acetate 3×, washed saturated sodium bicarbonate, brine, and dried over MgSO4. Solvent was removed under vacuum and the residue chromatographed over silica gel eluting with 80% to 100% ethyl acetate in hexanes to give the title compound, 98 mg, (M+H)+=219.

1. customThe reaction was quenched with water
2. extractionextracted ethyl acetate 3×
3. washwashed saturated sodium bicarbonate, brine
4. dry with materialdried over MgSO4
5. customSolvent was removed under vacuum
6. customthe residue chromatographed over silica gel eluting with 80% to 100% ethyl acetate in hexanes