| 摘要 |
PURPOSE:To obtain a vasopressin antagonistic agent useful as a vasodilator, hypotensor, diuretic, antithrombotic agent, etc., by using a new benzoheterocyclic compound as an active component. CONSTITUTION:The compound of formula I [R<1> is H, alkyl, amino, etc.; R<2> is H, halogen, alkoxy, OH, alkyl, benzoyloxy, etc.; R<3> is NR<4>R<5> (R<4> is H, benzoyl, etc.; R<5> is phenylalkoxy, alkanoyl, naphthylcarbonyl, furoyl, thenoyl, etc.) or CONR<11>R<12> (R<11> is H or alkyl; R<12> is cycloalkyl or phenyl); W is (CH2)p (p is 3-5) or CH=CH-(CH2)q (q is 1-3)], e.g. 4-methylamino-1-[4-(3,5- dichlorobenzoylamino)benzoyl]-1,2,3,4-tetrahydroquinoline. The compound can be produced e.g. by reacting a benzoyl heterocyclic compound of formula II with a carboxylic acid of formula III under the condition of conventional amide- bond forming reaction. |
