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)-1, and racemic (endo)-5-oxa-2-azabicyclo[ 2.2.1] heptane-3carboxylic 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.