Tetrahydrofuran → HCID 178426951, compound

Participants

Reaction Conditions

Reaction Steps

A small screw cap test tube was charged with 2,5-Dimethyl-2H-pyrazole-3-carboxylic acid [3-(3-hydroxymethylene-2-oxo-2,3-dihydro-1H-indole-6-carbonyl)-phenyl]-amide (as prepared in Example 60, 100 mg, 0.249 mmol) and THF (2.5 mL). To the resulting solution was 1-(4-amino-phenyl)-piperidin-4-ol (prepared below, 48.3 mg, 0.251 mmol), and the mixture was stirred for 24 h at 65° C. Subsequently, the reaction mixture was cooled to room temperature and diluted with EtOAc (5 mL) and Hexanes (40 mL). The precipitate that formed was then filtered and washed with 0° C. iPrOH (5 mL) to afford the title compound in 24% yield (0.034 g, 0.06 mmol).

Provenance & Evidence