- The Reaction of 3,4-Dihydroisoquinolines With Malonic Acid and Its Derivatives
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The reaction of various 3,4-dihydroisoquinolines with malonic acid gives the corresponding 1,2,3,4-tetrahydro-1-isoquinolineacetic acids in good yield, while the reaction with cyanoacetic acid and malonic acid half ethyl ester affords 1,2,3,4-tetrahydro-1
- Pelletier, Jeffrey C.,Cava, Michael P.
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p. 474 - 477
(2007/10/02)
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- Ring Transformation of 1-isoquinolines into 2-Acylaminopyrazoloisoquinolines
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Selective reduction of 1--3,4-dihydroisoquinolines (8) gives the tetrahydro derivatives (12) which readily isomerize to 2-acylaminopyrazoloisoquinolines (13).Compounds (13) were also obtained by reaction of the isoquin
- Bata, Imre,Heja, Gergely,Kiss, Pal,Korbonits, Dezso
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- 1,2,4-Oxadiazolin-5-one derivatives, process for their preparation and pharmaceutical compositions containing them
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The invention concerns new compounds of the formula (I) STR1 wherein R1 is hydrogen, phenyl or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; R2 is alkyl having 1 to 4 carbon atoms, cycloalkyl having 5 to 7 carbon atoms, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro; R3 is alkoxy having 1 to 4 carbon atoms or hydrogen, R4 is hydrogen, alkyl having 1 to 4 carbon atoms unsubstituted or substituted with alkoxy having 1 to 4 carbon atoms, benzyloxy or cyano, phenyl, or phenyl substituted with at least one alkyl having 1 to 4 carbon atoms, halogen, alkoxy having 1 to 4 carbon atoms or nitro, or phenyl-(C1-4 alkyl)-alkyl, in which the phenyl moiety may bear an alkoxy substituent having 1 to 4 carbon atoms or a halogen; m and n are each 0, 1 or 2 or a pharmaceutically acceptable acid addition or quaternary salt thereof. The compounds are potent vasodilators and exert a favorable influence on the extremital blood flow. They also show a heart function influencing activity. Methods for the preparation of said compounds and pharmaceutical compositions containing them are also the subject of the invention.
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