Piperidine derivative and pharmaceutical composition containing it
Piperidine derivatives of formula (I) and their pharmaceutically acceptable salts have antihypertensive action. The compounds may be included in pharmaceutical compositions for oral or parenteral administration.
-
(2008/06/13)
SOME FURTHER 2-(4-SUBSTITUTED 1-PIPERAZINYL)ACETAMIDES DERIVED FROM 6,11-DIHYDRODIBENZOTHIEPIN. TRANSFORMATIONS OF 6,11-DIHYDRODIBENZOTHIEPIN DERIVATIVES INTO ANTHRAQUINONES,ANTHRONES AND ANTHRACENES
Reactions of the secondary amines I and VIII with chloroacetyl chloride gave the 2-chloroacetamides II and IX affording by substitution reactions with 1-methylpiperazine, 2-(1-piperazinyl)ethanol and 3-(1-piperazinyl)propanol the title compounds III-V and
POTENTIAL ANTIDEPRESSANTS: SATURATED SIDE CHAIN AMINES DERIVED FROM 6,11-DIHYDRODIBENZOTHIEPIN AND 4,9-DIHYDROTHIENO-2-BENZORHIEPIN
Reduction of IV with hydroiodic acid afforded almost quantitatively the spirocyclic amino sulfide VII, evidently via V and VI.The carbamate II was chlorinated with N-chlorosuccinimide, the product (XII) was reacted with phenylmagnesium bromide and the reduced with LiAlH4 to give the 6-phenyl derivative X of the antidepressant agent hydrothiadene (I).Treatment of 11-methyl-6,11-dihydrodibenzothiepin (XIII) with butyllithium followed by alkylation with 3-dimethylaminopropyl chloride resulted in 6-(3-dimethylaminopropyl) derivative XIV.Reaction of XIV with ethyl chloroformate and the following alkaline hydrolysis gave the 6-(3-methylaminopropyl) derivative XV (mixture of stereoisomers).Reduction of the corresponding olefinic amine and the tertiary alcohol with hydroiodic acid gave the saturated side chain amines derived from 4,9-dihydrothieno-2-benzothiepin XVIII and XIX.The dihydroderivative of dithiadene XVIII (VUFB-17031) proved very effective in a series of tests predictive of antidepressant activity.
Treatment of xanthene carbinol 1a or xanthenylidene derivative 2a with refluxing formic acid unexpectedly gave dihydro compound 3a.Thioxanthene and acridine carbinols 1b and 1c and acridinylidene derivative 2c were also partially reduced when treated with formic acid.
Loughhead, David G.
p. 5701 - 5702
(2007/10/02)
More Articles about upstream products of 1447-70-7