申请人:N.V. Koninklijke Pharmaceutische Fabrieken v/h Brocades-Stheeman en
公开号:US03980650A1
公开(公告)日:1976-09-14
A process is described for the preparation of pyrimidine derivatives having therapeutic properties. They have the general formula: ##SPC1## Wherein A represents an alkylene or alkenylene grouping which together with the carbon atoms of the pyrimidine nucleus to which it is attached forms a homocyclic ring containing five to seven carbon atoms, which homocyclic ring may carry one or more halogen, lower alkyl and/or lower alkoxy substituents and R represents an amino, lower alkylamino or di(lower)alkylamino group, or a nitrogen-, oxygen- or sulphur-containing saturated or unsaturated mononuclear heterocyclic group linked to the pyrimidine ring either through a carbon atom or, when the group contains a nitrogen atom, either through the nitrogen atom or a carbon atom and are prepared by reacting a cycloaliphatic(A)oaminonitrile with a nitrile of the formula R-CN where A and R have the above meanings in the presence of a basic alkali metal-containing compound and then reacting the resultant intermediate with water. The compounds have heretofore undiscovered antimicrobial and antihypertensive properties.
描述了一种制备具有治疗特性的嘧啶衍生物的过程。它们具有以下通用公式: ##SPC1## 其中A代表与连接到嘧啶核的碳原子一起形成含有五至七个碳原子的同环环的烷基或烯基基团,该同环环可能携带一个或多个卤素、较低的烷基和/或较低的烷氧基取代基,R代表氨基、较低的烷基氨基或二(较低)烷基氨基团,或者是氮、氧或硫含有饱和或不饱和的单核杂环基团,通过碳原子或者当基团含有氮原子时,通过氮原子或碳原子连接到嘧啶环上,并通过将环状脂肪族(A)氨基腈与上述含有意义的R-CN公式的腈在碱性含碱金属化合物存在下反应,然后将所得的中间体与水反应制备而成。这些化合物具有迄今尚未发现的抗菌和降压特性。