申请人:Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt
公开号:US04940716A1
公开(公告)日:1990-07-10
Diuretic and saluretic tetrahydro-isoquinoline derivatives of the Formula (I) ##STR1## wherein R stands for hydrogen or chlorine, R.sup.1 and R.sup.2 are hydrogen, methoxy or ethoxy, and R.sup.3 and R.sup.4 are hydrogen or methyl, and a process for the preparation thereof as well as pharmaceutical compositions containing as active ingredients isoquinoline derivatives of the Formula (I). The compounds of Formula I are prepared by reacting a 2-amino-tetrahydro-isoquinoline derivative of the Formula (II) ##STR2## with a carboxylic acid derivative of the Formula (III) ##STR3## wherein x stands for chlorine, --OH, --OCH.sub.2 CN, --OCH.sub.3, --OC.sub.2 H.sub.5, --OCOOCH.sub.3 or --OCOOC.sub.2 H.sub.5 R.sup.5 and R.sup.6 stand for hydrogen or together from CHN(CH.sub.3).sub.2 and in case of the Formula (Ia) ##STR4## splitting off the protective group in alkaline medium.
Formula (I)的利尿和排钠四氢异喹啉衍生物的中文翻译如下:其中R代表氢或氯,R.sup.1和R.sup.2代表氢、甲氧基或乙氧基,R.sup.3和R.sup.4代表氢或甲基,以及一种制备这些化合物的方法,以及含有作为活性成分的Formula (I)的异喹啉衍生物的药物组合物。通过将Formula (II)的2-氨基四氢异喹啉衍生物与Formula (III)的羧酸衍生物反应制备Formula I的化合物。在这里,x代表氯、--OH、--OCH.sub.2 CN、--OCH.sub.3、--OC.sub.2 H.sub.5、--OCOOCH.sub.3或--OCOOC.sub.2 H.sub.5,R.sup.5和R.sup.6代表氢或共同形成CHN(CH.sub.3).sub.2,对于Formula (Ia),在碱性介质中裂解保护基。