申请人:Cedona Pharmaceuticals B.V.
公开号:US05190589A1
公开(公告)日:1993-03-02
A process is provided for preparing novel substituted or unsubstituted 4(5)-.omega.-aminoalkyl)imidazoles of the formula ##STR1## wherein n is 1 to 6, R.sub.1 is hydrogen or a linear, branched or cyclic, saturated or unsaturated alkyl group having 1-6 C-atoms or a phenyl ring being unsubstituted, or mono- or di-substituted with groups such as lower alkyl, halogen, alkoxy, methylenedioxy or a combination thereof, and R.sub.2 is hydrogen or methyl. The process comprises brominating an .omega.-phthalimidoalkan-2-one with bromine in anhydrous methanol to a 1- or 3-bromo-.omega.-phthalimido-alkan-2-one, subjecting said derivative to ring closure with an amidine in N.N-dimethylformamide with potassium carbonate under mild conditions followed by hydrolytic separation of the phthalic residue. Pharmaceutical compounds, compositions and a method of treatment are also provided.
提供了一种用于制备新型取代或未取代的4(5)-.omega.-氨基烷基)咪唑的过程,其化学式如下:其中n为1至6,R.sub.1为氢或具有1-6个碳原子的线性、支链或环状、饱和或不饱和烷基基团,或者为未取代的苯环,或者为单取代或双取代的基团,例如较低的烷基、卤素、烷氧基、亚甲二氧基或其组合,R.sub.2为氢或甲基。该过程包括使用溴在无水甲醇中对.omega.-邻苯二甲酰胺烷基-2-酮进行溴化,得到1-或3-溴-.omega.-邻苯二甲酰胺基-烷基-2-酮,将该衍生物在N.N-二甲基甲酰胺中与碳酸钾在温和条件下进行环闭合,随后水解分离邻苯二甲酰残基。还提供了药用化合物、组合物和治疗方法。