Sodium Carbonate → (1S,2R)-3-Fluoro-4'-(2-hydroxy-1-methyl-4-pyridin-3-yl-butoxy)biphenyl-4-sulfonic acid amide

Participants

Reaction Conditions

Reaction Steps

Prepared according to the method described in Example 12b) from 4-[(2S,3R)-5-(pyridin-3-yl)-3-hydroxypent-2-yloxy]benzeneboronic acid (0.20 g, Example 33), 4-bromo-2-fluorophenylsulfonic acid amide (0.20 g), ethanol (3 ml), 2M aqueous sodium carbonate (1.0 ml) and tetrakis(triphenylphosphine)palladium (0) (0.03 g) with heating at 90° C. for 3 hours. After work-up, the residue was purified by normal-phase HPLC eluting with a gradient of 0-25% ethanol in dichloromethane, followed by recrystalisation from aqueous ethanol, to give the title compound as a solid (0.11 g).

Provenance & Evidence