申请人:Sydnes Leiv K.
公开号:US20120149908A1
公开(公告)日:2012-06-14
In a first aspect, the present invention relates to a method for the preparation of alkynylpiperidine and alkynylpiperidine derivatives. In particular, a method is provided for preparing alkynylpiperidine derivatives starting from epoxide compounds. Further, the alkynylpiperidine derivatives according to the present inventions are substituted trans-3-4-alkynylpiperidine derivatives. In another aspect, triazolylpiperidine compounds and methods for said preparation are provided. In particular, the triazolylpiperidine compounds according to the present invention are obtained by reacting an alkynylpiperidine derivatives with an organic azid, preferably, in the presence of a Cu (I) or Ru catalyst. In a preferred embodiment, 1,4-disubstituted or 1,5-disubstituted 1,2,3-triazolylpiperidine compounds are provided.
在一个方面,本发明涉及一种制备炔基哌啶和炔基哌啶衍生物的方法。具体来说,提供了一种从环氧化合物起始制备炔基哌啶衍生物的方法。此外,根据本发明的炔基哌啶衍生物是取代的反式3-4-炔基哌啶衍生物。在另一个方面,提供了三唑基哌啶化合物及其制备方法。具体来说,根据本发明的三唑基哌啶化合物是通过将炔基哌啶衍生物与有机叠氮化合物反应而获得的,优选地,在Cu(I)或Ru催化剂存在的情况下。在一个首选实施方式中,提供了1,4-二取代或1,5-二取代1,2,3-三唑基哌啶化合物。