Synthesis of Functionalized Proline‐Derived Azabicycloalkane Amino Acids and Their Applications in Drug Discovery: Recent Advances

After the first synthesis reported in 1994, azabicycloalkane amino acids have raised increasing interest, becoming one of most important classes constrained dipeptide mimics. Their incorporation into peptidomimetic structures allowed obtainment a wide range biologically active compounds. Over years, different research groups worked at development synthetic strategies to gain these rigid surrogates, nevertheless, methods affording functionalized and “easy-to-functionalize” derivatives are quite less described. The presence derivatizable azabicycloalkanone core could allow introduction chemical modifications aimed improve pharmaceutical properties compound without need for redesigning its synthesis. This account has collected critically surveyed relevant approaches acids, focusing attention on period 2010 present. Moreover, recent applications compounds drug discovery will be discussed.