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1,3-双(乙氧甲酰基)氮戊环-4-酮与羟胺作用,变为肟,后者经催化氢化,并再与酸作用,得到4-氨基-3-羧基氮戊环(Ⅰ)。1-乙氧甲酰基氮戊环-3-酮与氯化铵及氰化钾作用,继用氢溴酸水解,制成(±)-3-氨基-3-羧基氮戊环(Ⅱ)。动物试验中Ⅱ有抑制血吸虫童虫生长的作用,Ⅰ则无效,红外吸收光谱及纸上层析的R_f值观察中,Ⅱ均与天然南瓜子氨酸一致。于是,将Ⅱ制成(+)-樟脑酸盐,以水及丙酮混合剂纯化拆开,获得(一)-3-氨基-3-羧基氮戊环(+)-樟脑酸盐,并制成相应游离碱及高氯酸盐,又酰化成二苯甲酰及二对硝基苯甲酰衍生物。以上各化合物的比旋光度及熔点与天然南瓜子氨酸相应衍化物一致,证明天然南瓜子氨酸是(一)-3-氨基-3-羧基氮戊环。左旋体樟脑酸盐分去后,从母液中又得到右旋体。动物试验中左旋体对日本血吸虫童虫有明显抑制作用,右旋体则无效。
The 1,3-bis (ethoxycarbonyl) azulen-4-one is reacted with hydroxylamine to become an oxime which is catalytically hydrogenated and reacted with acid to give 4-amino-3-carboxynilolane Ⅰ). 1-Ethoxyformylazacyclo-cyclopentan-3-one is reacted with ammonium chloride and potassium cyanide to give (±) -3-amino-3-carboxynilolane (II) following hydrobromic acid hydrolysis. In animal experiments Ⅱ inhibited the growth of Schistosoma japonicum, while Ⅰ was ineffective. In the observation of infrared absorption spectrum and R_f value on paper chromatography, Ⅱ was consistent with that of natural pumpkin. Thus, the II is made into (+) - camphor acid salt, with water and acetone mixture was purified to obtain (a) -3-amino-3-carboxydiazepine (+) - camphorate and made The corresponding free base and perchlorate are acylated to dibenzoyl and di-p-nitrobenzoyl derivatives. The specific rotation and melting point of the above compounds are consistent with the corresponding derivative of the natural squash subunit, which proves that the natural squash subunit is (i) -3-amino-3-carboxynilolane. L-carnitine acid salt points, get from the mother liquor dextral body. Animal experiments leptospirosis schistosomula Schistosomiasis significantly inhibited, dextromere is invalid.