1421780-61-1Relevant articles and documents
Chemoselective preparation of 1,2,3-triazole-isoxazole bisfunctional derivatives and their application in peptidomimetic synthesis
Niu, Teng-Fei,Lv, Mei-Fang,Wang, Liang,Yi, Wen-Bin,Cai, Chun
, p. 1040 - 1048 (2013/02/26)
A novel kind of bisfunctional nitrogen heterocycle containing both 1,2,3-triazole and isoxazole scaffolds has been prepared. The protocol utilized alkynyl substituted amines as the bifunctional linkers to combine a copper-free triazole synthesis with a hypervalent iodine-mediated isoxazole cycloaddition through a chemoselective process. This method has also been exemplified in the construction of bisfunctional-modified peptidomimetics by combining three reactions in a sequential procedure. This straightforward metal free process may find biological applications. In addition, all of the compounds were analysed by Lapinski's rule-of-five which is expected to help drug discovery.