The sulfinate alkylation reaction described by Prof. Baran is a powerful late stage functionalization tool. Our kit allows to conveniently produce analogues of the lead compound using 6 different sulfinate alkylation reagents. Each vial contains 100 μmol of sulfinate alkylation reagent and a stirring bar to react with 50 μmol of substrate. C-H functionalization will primarily occur on electron-deficient heteroarenes at one or several positions.
Standard Protocol: Several solvents or solvent mixtures can be used to perform the reaction (DMSO, DMSO/H2O/TFA, CHCl3/ H2O/TFA… ). A solution of substrate is made with 300 μmol of substrate in 2.1 ml selected solvent. 350 μl is added in each vial followed by 20.8 μl of TBuOOH (70% in water). The reactions are allowed to stir at 50°C for 12-24 hours.
Kit contents: 2 reaction vials of each reagents (100 μmol), 12 reaction vials total.