HEXAHYDROPYRAZINOQUINOLINE DERIVATIVE

PURPOSE: To obtain the subject derivative excellent in serotonin IA receptor agonistic action, sedative action on mental stress, hallucination inhibitory action, having only a slight side effect such as sleepiness, etc., useful for treating and preventing anxiety, depression, hypertension, etc. CONS...

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Hauptverfasser: HONMA HIROSHI, KOJIMA KOICHI, SUGIMOTO MASAHIKO, HISAMOTO MARIE, HARA TAKAO, SAKAI JUNICHI, AIZAWA YUICHI, SAFUKU NAOZUMI, TONOHIRO TOSHIYUKI, KOYAMA KAZUO
Format: Patent
Sprache:eng
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Zusammenfassung:PURPOSE: To obtain the subject derivative excellent in serotonin IA receptor agonistic action, sedative action on mental stress, hallucination inhibitory action, having only a slight side effect such as sleepiness, etc., useful for treating and preventing anxiety, depression, hypertension, etc. CONSTITUTION: This derivative (salt) is shown by formula I or formula II [R is CO-R (R is a 1-7C alkyl, a 3-6C cycloalkyl, etc.); R is H or forms a group of formula III, etc., with R and N; R is a (substituted) 6-14C aryl, etc.; X is methylene or O; (m) is 2-6] such as 3-(4-phthalimidobutyl)-2,3,4,4a,5,6- hexahydro-1H-pyrazino[1,2-a]quinoline-dihydrochloride. The derivative is obtained by reacting a compound of formula IV with a compound of formula V in an inert solvent in the presence or absence of a base (preferably in the presence of the base).