Efficient asymmetric synthesis of beta-amino acid BAY 10-8888/PLD-118, a novel antifungal for the treatment of yeast infections

The beta-amino acid BAY 10-8888/PLD-118 is currently being investigated in phase II clinical studies as a novel antifungal for the treatment of yeast infections. An efficient asymmetric synthesis of this compound is described. The key step employed a highly enantioselective, quinine-mediated alcoholysis of a meso-anhydride intermediate.