反应详情

A mixture of (6-amino-indol-1-yl)-acetic acid ethyl ester (100 mg, 0.46 mmol; WO 2003041714 A1), 5-(3-trifluoromethoxy-phenyl)-pent-4-ynoic acid (115 mg, 0.44 mmol), 1-[3-(dimethylamino)-propyl]-3-ethylcarbodiimide hydrochloride (90 mg, 0.46 mmol) and 4-(dimethylamino)pyridine (57 mg, 0.46 mmol) in dichloromethane (1.5 ml) was stirred for 14 h at ambient temperature. The reaction mixture was diluted with dichloromethane, successively washed with 1 N HCl, brine, 1 N NaOH and brine, and dried over sodium sulfate. The solvent was removed under reduced pressure and the residue purified by flash chromatography (silica gel, heptane/AcOEt) to give 152 mg (0.33 mmol, 72%) of the title compound as off-white crystals.

1. washsuccessively washed with 1 N HCl, brine, 1 N NaOH and brine
2. dry with materialdried over sodium sulfate
3. customThe solvent was removed under reduced pressure
4. customthe residue purified by flash chromatography (silica gel, heptane/AcOEt)