| 摘要 |
<p>NEW MATERIAL:The titled compound of formulaI(R is lower alkanoyl, lower alkoxycarbonyl, furoyl, lower alkanesulfonyl, etc.; A is lower alkylene; the C- bond between the 3- and 4-positions of the carbostyril skeleton is single or double) and its salt. EXAMPLE:6-[4-(3,4,5-Trimethoxybenzoyl)-1-piperazinylacetyl]-3,4-dihydr ocarbostyril.monohydrochloride.3/2-hydrate. USE:A cardiotonic drug useful for the remedy of cardiac diseases such as congestive heart failure, etc. It has high positive inotropic activity and coronary vessel flow increasing activity, and nevertheless has weak activity to increase the heart rate. PROCESS:The compound of formulaIcan be prepared e.g. by reacting 3,4-dihydrocarbostyril with the compound of formula III (X and X' are halogen) in a solvent in the presence of a Lewis acid, and reacting the resultant compound of formula IV with the piperazine derivative of formula V in the absence of a solvent or in an inert solvent.</p> |
