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氮八环、氮七环、氮六环与甲醛及甲酰氨基丙二酸二乙酯缩合,生成相应的α-(N-氮杂环甲基)甲酰氨基丙二酸二乙酯(Ⅳ),再用盐酸水解后得α-氨基-β-(N-氮杂环基)丙酸(Ⅲ).氮八环、氮七环、氮六环与氯乙酸乙酯及α-氯丙酸乙酯缩合,生成相应的α-(N-氮杂环基)丙酸乙酯及乙酸乙酯(Ⅴ),然后用盐酸水解,制得α-(N-氮杂环基)取代的丙酸及乙酸(Ⅱ)的盐酸盐.V分别和水合肼、苯甲肼或苯乙肼在封管中加热缩合,制成相应的酰肼(Ⅵ).其中某些化合物具有降压及冠脉扩张作用.
Nitrogen octa-ring, nitrogen-hepta-ring, nitrogen-six ring and diethylformamide and formamidomalonate are condensed to form the corresponding diethyl α- (N-azacyclicmethyl) carboxamidomalonate ) And hydrolyzed with hydrochloric acid to give (III) a-amino-β- (N-azacyclopentano) propanoic acid. Nitrogen ring, nitrogen ring, nitrogen ring with ethyl chloroacetate and α-chloropropionic acid Ethyl ester to give the corresponding ethyl α- (N-azacyclyl) propionate and ethyl acetate (V) which is then hydrolyzed with hydrochloric acid to give α- (N-azacyclo) substituted propionic acid And acetic acid (II) hydrochloride.V and hydrazine hydrate respectively, hydrazine or phenelzide in the sealed tube heating condensation, the corresponding hydrazide (Ⅵ). Some of these compounds have antihypertensive and coronary Expansion effect.