Beaucage reagent

Beaucage reagent is found to be potent in causing DNA cleavage^[1][2][3]. In Vitro:The synthesis of Beaucage reagent:^[1]
Under the condition of 5℃, 2-amino-3-methyl benzoic acid is subjected to diazonium reaction following the procedure described by Allen andcoworkers[2]. Upon the diazonium salt formation, it was treated immediately with sulfide to generate disulfide under strongly alkaline conditions.Using activated zinc in refluxing glacial acetic acid, the disulfide bond was cleaved off to yield thiol 2-mercapto group-3-carboxyl benzoic acid. The reaction of thioacetic acid with 2-mercapto group-3-carboxyl benzoic acid in concentrated sulfuric acid gave rise to the cyclic compound. Employ dimethyldioxirane as potential oxidizing agent. A one-pot procedure in which Oxone^TM was added to a solution of the cyclic compound in acetone led to the successful preparation of Beaucage reagent.
Beaucage reagent causes DNA cleavage:^[1]
Assays were performed in 50 mM sodium phosphate buffer (pH 7.0) containing 0.5 mg of supercoiled pBR322 DNA in the presence of Beaucage reagent at different concentrations (total volume 20 mL) for 12 h. Beaucage reagent can effectively cause DNA-cleaving activities.