Synthesis of Bridged Bicyclic Morpholine Amino Acids as Compact Modules for Medicinal Chemistry

This manuscript depicts efficient synthesis of structurally novel morpholine amino acids, (1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptane-4-carboxylic acid (+)-1, its enantiomer (−)-1, and racemic (endo)-5-oxa-2-azabicyclo[2.2.1]heptane-3-carboxylic acid (±)-2, which could serve as compact modules in medicinal chemistry to potentially modulate physicochemical and pharmacokinetic properties of drug candidates, and to introduce intellectual properties.