Balsells Jaume, Dimichele Lisa, Liu Jinchu, Kubryk Michele, Hansen Karl, Armstrong Joseph D
Department of Process Research, Merck Research Laboratories, P.O. Box 2000, Rahway, New Jersey 07065, USA.
Org Lett. 2005 Mar 17;7(6):1039-42. doi: 10.1021/ol0474406.
[reaction: see text] A concise, modular approach for the synthesis of [1,2,4]triazolo[4,3-alpha]piperazines via condensation of highly reactive chloromethyloxadiazoles with ethylenediamines is described. NMR studies of this reaction provide evidence that suggests a novel activation mechanism for electron-deficient chloromethyloxadiazoles.
