1-Hydroxybenzotriazole → HCID 86603103, compound

Participants

Reaction Steps

To a solution of 64 mg (0.33 mmol) of 4-chloro-1H-indole-7-carboxylic acid in 2 ml DCM 50 mg of HOBT (0.33 mmol) were added and the reaction mixture was stirred for 15 min at rt under nitrogen. 85 mg (0.3 mmol) of (4-tert-butyl-benzyl)-[2-(4-fluoro-phenyl)-ethyl]-amine in 1 ml DCM were added and then 63 mg (0.33 mmol) of EDC.HCl. The reaction mixture was stirred over night at rt to yield a slight turbid yellow solution. The solvent was evaporated and the residue was dissolved in 1,2-dichloro ethane. The reaction mixture was stirred at reflux for 3 h. The solvent was evaporated and the residue was purified by column chromatography (25 g silica gel, heptane/EtOAc 7:3) to yield 90 mg (65%) product as a light yellow viscous oil. MS (ISP) 463.4 (M+H)+.

Provenance & Evidence