反应详情

To a solution of 1-(1-benzyl-2-isopropyl-5-(methoxymethoxy)-1H-indol-3-yl)-N-(3,5-difluorobenzyl)methanamine (Compound 5, 117 mg, 0.25 mmol) in isopropanol (2.0 ml) and THF (2.0 ml) was added 6 M HCl (0.4 ml). The mixture was stirred at room temperature for 16 h, and concentrated under vacuum. The mixture was diluted with EtOAc, and washed with phosphate buffer (pH=7.2), and brine, and dried over Na2SO4, and concentrated under vacuum. The residue was purified by flash chromatography on silica gel eluting with 20-60% EtOAc-hexanes to yield 1-benzyl-3-((3,5-difluorobenzylamino)methyl)-2-isopropyl-1H-indol-5-ol (Compound 6) as a yellow solid.

1. concentrationconcentrated under vacuum
2. additionThe mixture was diluted with EtOAc
3. washwashed with phosphate buffer (pH=7.2), and brine
4. dry with materialdried over Na2SO4
5. concentrationconcentrated under vacuum
6. customThe residue was purified by flash chromatography on silica gel eluting with 20-60% EtOAc-hexanes