公开(公告)号：US4113731A

公开(公告)日：1978-09-12

申请号：US713011

申请日：1976-08-09

申请人： Giorgio Winters ,  Nunzio DiMola

发明人： Giorgio Winters ,  Nunzio DiMola

IPC分类号： C07D209/40 ,  C07D231/38 ,  C07D277/48 ,  C07D471/04 ,  C07D491/048 ,  C07D513/04 ,  C07D471/14 ,  C07D495/14 ,  C07D513/14

CPC分类号： C07D231/38 ,  C07D209/40 ,  C07D277/48 ,  C07D471/04 ,  C07D513/04

摘要： Fused isoquinoline derivatives of the general formula ##STR1## wherein: A is a divalent radical selected from the groups ##STR2## wherein R.sub.3 and R.sub.4 each independently represents hydrogen, alkyl,, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl, cycloalkyl-alkyl or, taken together with the adjacent double bond, represent a cycloalkene containing from 5 to 8 carbon atoms or an aromatic nucleus;R.sub.5 represents hydrogen, hydroxyl, alkyl, alkenyl, cycloalkyl, aryl, aralkyl, aralkenyl or cycloalkyl-alkyl;Y is .dbd.O, .dbd.S or .dbd.NH;X is --O--, --S-- or --NR.sub.6 -- wherein R.sub.6 represents hydrogen, alkyl, cycloalkyl, aryl, aralkyl or cycloalkyl-alkyl;R.sub.1 and R.sub.2 each independently represents hydrogen, alkyl, phenyl, cycloalkyl, alkoxy, alkenyloxy, methylenedioxy, cycloalkoxy, halo or di-alkylamino or, taken together with the adjacent carbon atoms of the benzene ring, form a cycloalkenyl group containing 5 or 6 carbon atoms or an aromatic nucleus fused on the benzene ring. The compounds are essentially prepared through thermal cyclization of a compound of the formula ##STR3## wherein A, X, Y, R.sub.1 and R.sub.2 have the same meanings given before, with the proviso that R.sub.1 and R.sub.2 cannot simultaneously occupy both the ortho positions, B represents hydrogen, R represents an --OR.sub.7 or --NR.sub.8 R.sub.9 radical wherein R.sub.7 is alkyl, aryl or aralkyl and R.sub.8 and R.sub.9 each independently represents hydrogen, alkyl, aryl, aralkyl, or taken together with the adjacent nitrogen atom represent a heterocyclic saturated radical of 5 or 6 atoms which may contain a further hetero-atom selected from oxygen and nitrogen, or the symbols B and R taken together represent a further bond between the adjacent carbon and nitrogen atoms.

摘要翻译： 通式（I）的稠合异喹啉衍生物其中：A是选自下组的二价基团，其中R 3和R 4各自独立地表示氢，烷基，烯基，环烷基，芳基，芳烷基，芳烯基，环烷基 或与相邻双键一起代表含有5-8个碳原子的环烯烃或芳族核; R5表示氢，羟基，烷基，烯基，环烷基，芳基，芳烷基，芳烯基或环烷基 - 烷基; Y = O，= S或= NH; X是-O - ， - S-或-NR 6 - ，其中R 6表示氢，烷基，环烷基，芳基，芳烷基或环烷基 - 烷基; R 1和R 2各自独立地表示氢，烷基，苯基，环烷基，烷氧基，烯氧基，亚甲二氧基，环烷氧基，卤代或二烷基氨基，或与苯环的相邻碳原子一起形成含有5或6个碳的环烯基 原子或稠合在苯环上的芳香核。 这些化合物基本上通过式（VI）化合物的热环化制备，其中A，X，Y，R 1和R 2具有以下相同的含义，条件是R 1和R 2不能同时占据邻位 位置，B表示氢，R表示-OR7或-NR8R9基，其中R7为烷基，芳基或芳烷基，R8和R9各自独立地表示氢，烷基，芳基，芳烷基或与相邻氮原子一起表示杂环饱和 可以含有另一个选自氧和氮的杂原子的5或6个原子的基团，或符号B和R一起代表相邻的碳原子和氮原子之间的另外的键。