申请人:Byk Gulden Lomberg Chemische Fabrik GmbH
公开号:US04016280A1
公开(公告)日:1977-04-05
4,4-Diarylpiperidine compounds, preferably 4,4-diphenylpiperidine which are substituted or unsubstituted in the 1-position of the piperidine nucleus, such as 1-(lower alkyl)-4,4-diphenylpiperidines, 1-(lower alkyl)-4-phenyl-4-tolylpiperidines, and their substantially non-toxic, pharmaceutically-acceptable acid addition salts, are highly effective central nervous system (CNS) stimulants which are superior to known amphetamine-type stimulants. A novel and highly advantageous process of making such 4,4-diarylpiperidine compounds comprises reacting a 4-aryl-4-hydroxypiperidine compound which may be substituted in its 3-position by an aroyl group, with an aromatic hydrocarbon, in particular with benzene, in the presence of a Friedel-Crafts-type catalyst.
4,4-二芳基哌啶化合物,最好是在哌啶核的1-位置被取代或未取代的4,4-二苯基哌啶,例如1-(较低烷基)-4,4-二苯基哌啶,1-(较低烷基)-4-苯基-4-甲苯基哌啶,以及它们的基本无毒、药用可接受的酸盐,是高效的中枢神经系统(CNS)兴奋剂,优于已知的苯丙胺类兴奋剂。制备这种4,4-二芳基哌啶化合物的一种新颖且非常有利的方法包括将一个4-芳基-4-羟基哌啶化合物(其3-位置可能被芳酰基取代)与芳香烃反应,特别是与苯反应,在Friedel-Crafts型催化剂的存在下。