Sodium Carbonate → 2-{[(4-Fluorophenyl)methyl]oxy}-5-(1-methyl-1H-pyrazol-4-yl)-4-(4-morpholinylmethyl)-N-3-pyridinylbenzamide

Participants

Reaction Conditions

Reaction Steps

To a solution of 5-bromo-2-{[(4-fluorophenyl)methyl]oxy}-4-(4-morpholinylmethyl)-N-3-pyridinylbenzamide (may be prepared as described in Example 15; 95 mg, 0.19 mmol) in 1,2-dimethoxyethane (5 ml) was added 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (47.4 mg, 0.23 mmol), Pd(Ph3P)4 (13.16 mg, 0.01 mmol) and sodium carbonate (0.38 ml, 0.38 mmol). The mixture was heated at 120° C. in the microwave for 35 minutes, cooled and the solvent removed in vacuo to give a solid. Purification by MDAP yielded the title compound as a colourless gum. 36 mg.

Provenance & Evidence