Abstract: Norepinephrine, the chemical mediator for the transmission at peripheral adrenergic junctions, is formed by the decarboxylation of dihydroxyphenylalanine (DOPA). It has been reported that amino acids structurally related to DOPA have specific pharmacological properties. In view of the fact that guanethidine (I), a clinically useful hypotensive agent, is an azacyclo compound, it would be interesting to prepare some amino acids carrying cyclic amino substituents. Heptamethyleneimine, hexamethyleneimine, and piperidine were reacted respectively with formaldehyde and diethyl formamido-malonate, giving the corresponding α-(Nazacycloalkyl)-formamidomalonic esters (Ⅳ). The latter afforded α-amino-β-(N-azacydoalkyl)-propionic acids (Ⅲ) on acid hydrolysis. Ethyl α-(N-azarycyloalkyl)-propionates and acetates (Ⅴ) were formed on condensation of heptamethyleneimine, hexamethyleneimine, or piperidine with ethyl chloroacetate or ethyl α-chloropropionate. Hydrolysis of these esters with hydrochloric acid gave the corresponding hydrochlorides of α-(N-azarycyloalkyl)-propionic acids or acetic acids (Ⅱ). In view of the high biological activities of hydrazides, the esters (Ⅴ) were subjected to hydrazinolysis with phenylethyl hydrazine, benzyl hydrazine, or hydrazine hydrate, forming numerous hydrazides (Ⅵ). Pharmacological tests revealed that compounds Ⅵ_k and VIn had hypotensive activity, and compound Ⅵm dilated coronary vessels without exerting marked influence on heart rate and contractile force of the heart.