A process for the preparation of nitrogen bridgehead condensed pyrimidine compounds of the general formula IMAGE I [wherein R represents hydrogen or lower alkyl; R1 represents hydrogen, lower alkyl, carboxy or a derivative thereof or styryl; R2 represents hydrogen or optionally substituted lower alkyl; R3 represents hydrogen, optionally substituted lower alkyl, aryl, aralkyl, halogen, carboxy or a derivative thereof, the group -(CH2)m-COOH (in which m is the integer 1, 2 or 3) or a carboxy derivative thereof, formyl, lower alkanoyl or a condensed thereof; R4 represents hydrogen, optionally substituted alkyl, aryl optionally substituted by one or more substituents, optionally substituted aralkyl, a heterocyclic group optionally substituted by one or more substituents, the group (CH2)m-Het (in which m is the integer 1, 2 or 3; Het is an optionally substituted heterocyclic group); R5 represents hydrogen, C1-6alkyl, aryl optionally substituted by one or more substituents, formyl, lower alkanoyl, optionally substituted aroyl or heteroaryl; or R4 and R5 together with the nitrogen therebetween represent an optionally substituted mono- or bicyclic heterocyclic ring optionally containing further heteroatom] and pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers and tautomers thereof.
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机译:通式为 I的氮桥头稠合嘧啶化合物的制备方法,其中R代表氢或低级烷基; R1代表氢,低级烷基,羧基或其衍生物或苯乙烯基; R 2代表氢或任选取代的低级烷基; R 3代表氢,任选取代的低级烷基,芳基,芳烷基,卤素,羧基或其衍生物,基团-(CH 2)m -COOH(其中m为整数1、2或3)或其羧基衍生物,甲酰基,低级烷酰基或其缩合物; R 4代表氢,任选取代的烷基,任选被一个或多个取代基取代的芳基,任选取代的芳烷基,任选被一个或多个取代基取代的杂环基,(CH 2)m -Het基团(其中m是整数1、2或3; Het是可取代的杂环基); R5代表氢,C1-6烷基,任选被一个或多个取代基取代的芳基,甲酰基,低级烷酰基,任选取代的芳酰基或杂芳基; R 4和R 5以及它们之间的氮一起表示任选取代的单环或双环杂环,其任选地包含另外的杂原子和其药学上可接受的盐,水合物,立体异构体,旋光异构体,几何异构体和互变异构体。
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