(2,4-Dichlorophenyl)boronic acid → HCID 9956495, compound

Participants

Reaction Steps

A solution of 5-bromo-2-(1-(4-cyanobenzyl)-5-imidazolylmethyl)-1,2,3,4-tetrahydroisoquinoline (Example 10; 100 mg, 250 0.25 mmol), 2,4-dichlorophenyl boronic acid (53 mg, 0.275 mmol) and tetrakis(triphenylphosphine)palladium(0) in DME (2 mL) and water (0.5 mL) was heated to 80° C. for 20 h. The mixture was partitioned between water and EtOAc, washed with aqueous NaHCO3, water (2×), dried and evaporated. Column chromatography of the residue (silica gel; CHCl3 /MeOH 80:1) afforded the title compound as a white solid. FAB ms (m+1) 473.2

Provenance & Evidence