4-Toluenesulfonyl chloride → 3,5-Dichloro-N-(4-(4-fluorophenoxy)benzyl)-2-hydroxy-N-(3-((4-methylphenylsulfonamido)methyl)benzyl)benzenesulfonamide

Participants

Reaction Steps

To a suspension of 4-methylbenzene-1-sulfonyl chloride (25 mg, 0.13 mmol) in CH2Cl2 (3 mL) were added Et3N (0.10 ml, 075 mmol) and N-(3-(aminomethyl)benzyl)-3,5-dichloro-N-(4-(4-fluorophenoxy)benzyl)-2-hydroxybenzenesulfonamide (70 mg, 0.13 mmol). The reaction mixture was stirred at rt. under nitrogen for 2 h. The mixture was concentrated and dissolved in MeOH, purified by preparative HPLC. The fractions containing the desired product were combined, concentrated and lyophilized to give white solid (52 mg, 58%).

Provenance & Evidence