A variation of the Fischer indolization involving condensation of quinone monoketals and aliphatic hydrazines
A new twist: A one-pot nitrous acid free, diazonium-free, and transition-metal-free variation of the Fischer indole synthesis has been developed. Condensation of quinone monoketals and aliphatic hydrazine hydrochlorides afforded indoles via intermediate alkylaryldiazenes. This method will complement the classical Fischer indole synthesis by providing indoles in two steps from widely available phenols under mild conditions. Copyright
Synthesis, biological evaluation, and structural studies on N1 and C5 substituted cycloalkyl analogues of the pyrazole class of CB1 and CB2 ligands
A series of N1 and C5 substituted cycloalkyl and C5 4-methylphenyl analogues of the N-(piperidin-1-yl)-4-methyl-1H-pyrazole-3-carboxamide class of cannabinoid ligands were synthesized. The analogues were evaluated for CB1 and CB2 receptor binding affinities and receptor subtype selectivity. The effects of pyrazole substitution on ligand conformation and as such receptor affinities was not readily apparent; therefore, the geometries of the N1 and C5 substituents relative to the pyrazole ring were studied using high field NMR spectroscopy and systematic molecular mechanics geometry searches. An analysis of the relative ring geometries and functional group orientations provides new insight into the structural requirements of the CB1 and CB2 ligand binding pocket.
Krishnamurthy, Mathangi,Li, Wei,Moore II, Bob M.
p. 393 - 404
(2007/10/03)
A High-Yielding Synthesis of Monoalkylhydrazines
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Ghali, N. I.,Venton, D. L.,Hung, S. C.,Le Breton, G. C.
p. 5413 - 5414
(2007/10/02)
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