127346-48-9Relevant academic research and scientific papers
Yohimbine derivatives and use thereof
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Page/Page column Sheet 1 of 9, (2009/01/24)
Yohimbine derivatives are disclosed having modification of the C-16 carboxyl group to include a sidechain and where the resulting derivative does not possess a second yohimbine pharmacophore (i.e., the compound is not a yohimbine dimer). The yohimbine derivatives of the present invention are preferably characterized by selective activity as α2c-AR antagonists. Use of the compounds, or pharmaceutical composition containing them, for treating or preventing an α2c adrenergic receptor mediated condition or disorder, and for antagonizing activity of an α2c adrenergic receptor are also disclosed.
Mono-Protected Diamines. Nα-tert-Butoxycarbonyl α,ω-Alkanediamine Hydrochlorides from Amino alcohols.
Mattingly, Phillip G.
, p. 366 - 368 (2007/10/02)
Nα-tert-Butoxycarbonyl α,ω-alkanediamine hydrochlorides 3a-e are prepared from the amino alcohols in yields of 66-87percent.Reaction of the free amine with di-tert-butyl dicarbonate gives the N-tert-Butoxycarbonylamino alcohol 1a-e.One-pot conversion to the azide 2a-e via the mesylate under phase-transfer conditions followed by hydrogenolysis in the presence of chloroform yields the title compounds.
