Orthogonally Protected Thiazole and Isoxazole Diamino Acids: An Efficient Synthetic Route

An efficient strategy has been developed for the synthesis of heteroaromatic amino acids (HAAs). These methods generate mono- or orthogonally protected diamino acids from β-amino acids (see scheme). Their synthetic reliability and biological potential was demonstrated through the synthesis of an anthranilate synthase (AS) and isochorismate synthase (IS) inhibitor with improved potency.