Process for the production of quinoline containing heterocycles, intermediates, and process for the production of the intermediates
申请人:FISONS plc
公开号:EP0077090A1
公开(公告)日:1983-04-20
There is described a process for the production of a compound of formula 1,
in which R is hydrogen or alkyl CI to 6, and R5 and R10, which may be the same or different, are each hydrogen or alkyl CI to 6, or a pharmaceutically acceptable derivative thereof, which comprises removal of an activating group from a compound of formula II,
or a suitable derivative thereof, in which R, R5 and R,o are as defined above, and X represents an activating group, and if desired or necessary converting the resulting compound of formula I to a pharmaceutically acceptable derivative thereof, or vice versa.
There is also described a process for the production of a compound of formula II in which R is hydrogen, or a suitable derivative thereof, which comprises reaction of a compound of formula III,
or a suitable derivative thereof, in which R5 and R10 are as defined above, with a compound of formula IV,
in which X is as defined above.
这里介绍一种生产式 1 化合物的工艺、
其中 R 是氢或 CI-6 烷基,R5 和 R10(可以相同或不同)各自是氢或 CI-6 烷基,或其药学上可接受的衍生物,该工艺包括从式 II.或其适当衍生物中去除活化基团,其中 R、R5 和 R,o 如上文所定义,X 代表活化基团、
或其适当的衍生物,其中 R、R5 和 R,o 如上文所定义,X 代表活化基团,如果需要或必要,将得到的式 I 化合物转化为其药学上可接受的衍生物,反之亦然。
还描述了一种生产式 II 化合物(其中 R 为氢)或其适当衍生物的工艺,该工艺包括式 III、
或其适当衍生物(其中 R5 和 R10 如上文所定义)与式 IV 的化合物反应、
其中 X 如上所定义。