摘要 |
<p>Benzo 6,7 cyclohepta 1,2,3-de pyrido 2,1-a isoquinoline derivs. of formula (I) and their acid-addn. salts are new. In the formula, R1-5 are each H or lower alkyl, pref. H; L is OH or lower alkanoyloxy; M is benzyl, phenyl substd. by a lower alkyl, lower alkoxy, halogen or trihalomethyl gp., furyl, thienyl or pyridyl. Cpds. (I) are CNS depressants (tranquilizers) with a high ratio of CNS depression to ataxic properties and effects on the autonomic nervous system. A typical cpd. (I) is (6a, 15b-trans)-(5-OH, 15b-H-trans)-5-p-anisyl-1,4,5,6,6a,10,11,15b-octahydro-3H-benzo 6- ,7 cyclohepta 1,2,3-de pyrido 2,1-a isoquinolin-5-ol. In an example, this was prepd. from the corresp. ketone and p-methoxyphenylmagnesium bromide.</p> |