A practical synthesis of (1S,4S)-2,5-diazabicyclo[2.2.1]heptane |
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| Authors: | Corinne Beinat Samuel D. Banister Christopher S.P. McErlean Michael Kassiou |
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| Affiliation: | 1. School of Chemistry, The University of Sydney, Sydney, NSW 2006, Australia;2. Brain and Mind Research Institute, Sydney, NSW 2050, Australia;3. Discipline of Medical Radiation Sciences, The University of Sydney, Sydney, NSW 2006, Australia |
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| Abstract: | The rigid piperazine homologue 2,5-diazabicyclo[2.2.1]heptane (DBH) finds extensive application in medicinal chemistry and pharmaceutical research, but access to this scaffold is non-trivial. This letter details a concise synthetic sequence that gives ready access to DBH on gram scale. The route features a Staudinger reduction of an azide to facilitate a transannular cyclisation |
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| Keywords: | 2,5-Diazabicyclo[2.2.1]heptane Amines Transannular cyclisation Heterocycles Nicotinic acetylcholine receptors |
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