Pharmacologically active piperazino derivatives and the process for their preparation
申请人:RAVIZZA S.p.A.
公开号:EP0171636A1
公开(公告)日:1986-02-19
New piperazino derivatives of formula
in which R is a phenyl radical substituted with at least one sulphonamido group or a substituted nitrogenated heterocyclit ring, and A is C0, CH2' SO2' possessing inhibiting activity towards carbonic anhydrase.
The new products are prepared from compounds of formula R-A-X in which X is OH, SH, halogen, OR"" or SR"" in which R'''' is methyl, ethyl, phenyl, carbomethoxy, carboethoxy, and from a piperazino derivative of formula
The R' group can also be introduced on termination of the reaction, by removing and substituting a protective group present at the nitrogen.
式中的新哌嗪衍生物
其中 R 是被至少一个磺酰胺基团或取代的氮杂环取代的苯基,A 是 C0、CH2' SO2',具有抑制碳酸酐酶的活性。
新产品由式 R-A-X 的化合物制备,其中 X 是 OH、SH、卤素、OR""或 SR"",其中 R'''' 是甲基、乙基、苯基、羰基甲氧基、羧基甲氧基,以及由式 R-A-X 的哌嗪衍生物制备。
R'基团也可以在反应终止时通过移除和取代存在于氮上的保护基团而引入。