Synthesis of Chiral δ‐Aminoboronic Esters by Enantioselective Hydrogenation of 1,2‐Azaborines

Abstract We describe herein an iridium‐catalyzed highly diastereo‐ and enantioselective hydrogenation of 1,2‐azaborines to access δ‐aminoboronic esters of potential biological importance. This method represents the first enantioselective hydrogenation of a boron‐containing heteroarene and features diverse substitution patterns and wide scope. The synthetic utility of our method was demonstrated by the synthesis of (−)‐phenibut and the formal synthesis of (+)‐3‐PPP and fluvirucinine A 1 .