Preparation of Apoptotic Inducers, 2,2-Diphenyl-1,3,2-oxazaborolidin-5-ones, Under Alkaline Conditions

An efficient and high-yielding procedure has been developed for the synthesis of a set of fifteen 2,2-diphenyl-1,3,2-oxazaborolidin-5-ones, through the reaction of the corresponding α-amino acid with diphenyl borinic acid under alkaline conditions (pH 7.5-8). It is of note that these compounds showed potent cytotoxic activity on K-562 and HCT-15 cell lines.