反应详情

A mixture of 6-phenethyl-7-(trifluoromethyl)-1,2,3,4-tetrahydro-[1,4]diazepino[6,7,1-hi]indole (prepared as described in Example 2 above, 64 mg, 0.17 mmol), 3-(trifluoromethyl)butanoic acid (27 mg, 0.18 mmol), HATU (73 mg, 0.2 mmol) and triethylamine (85 mg, 0.84 mmol) in THF (7 mL) was stirred overnight. The resulting mixture was partitioned between ethyl acetate and water, and the organic layer was washed sequentially with NaHCO3 (sat'd) and brine, then dried and concentrated. The residue was purified by reverse-phase chromatography (CH3CN-water/TFA) to yield 4,4,4-trifluoro-3-methyl-1-(6-phenethyl-7-(trifluoromethyl)-3,4-dihydro-[1,4]diazepino[6,7,1-hi]indol-2(1H)-yl)butan-1-one (78 mg).

1. customThe resulting mixture was partitioned between ethyl acetate and water
2. washthe organic layer was washed sequentially with NaHCO3 (sat'd) and brine
3. customdried
4. concentrationconcentrated
5. customThe residue was purified by reverse-phase chromatography (CH3CN-water/TFA)