A variety of esters of methyldopa was synthesized to obtain derivatives that would be more efficiently absorbed from the gastrointestinal tract than the free amino acid and would undergo conversion to methyldopa readily in the blood or target tissues. The esters, .alpha.-pivaloyloxyethyl and .alpha.-succinimidoethyl were more potent antihypertensive agents than methylodopa in animal [rat] models and were selected for further study in man. The amino esters were prepared by 3 different methods, including direct esterification of methyldopa without the use of N- or O-protecting groups.