反应详情

To a solution of 25 mg (S)-2-Amino-N-(3,4-dimethyl-phenyl)-2-phenyl-N-[2-(6-trifluoromethyl-pyridin-3-yl)-ethyl]-acetamide (from example 1) in 1.5 ml dry CH2Cl2 under argon in a sealed tube was added 1.1 eq. oxetan-3-one. The reaction mixture was stirred at RT for 20 min, followed by the addition of 3.0 eq., Sodium triacetoxyborohydride and the reaction stirred for 16 h at RT. The reaction mixture diluted with 10 ml CH2Cl2 and washed with 2M aq. Na2CO3 2M, dried and concentrated then chromatographed on silica gel (EtOAc/Heptane, gradient elution) to give the desired compound. MS(m/e): 484.2 [M+H]+.

1. stirringthe reaction stirred for 16 h at RT
2. washwashed with 2M aq. Na2CO3 2M
3. customdried
4. concentrationconcentrated
5. customthen chromatographed on silica gel (EtOAc/Heptane, gradient elution)