Ceftaroline fosamil and ceftobiprole medocaril are recently approved fifth-generation cephalosporins that are active against serious Gram-negative and Gram-positive bacterial infections, including methicillin-resistant Staphylococcus aureus (MRSA). This article provides a brief background on the mechanisms of β-lactam antibacterial resistance and reviews the patent literature on synthetic routes and final forms of ceftaroline fosamil and ceftobiprole medocaril.