400715-75-5Relevant academic research and scientific papers
HETEROAROMATIC MACROCYCLIC ETHER CHEMOTHERAPEUTIC AGENTS
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Page/Page column 114, (2021/11/23)
Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.
Novel reversible monoamine oxidase A inhibitors: Highly potent and selective 3-(1 H-pyrrol-3-yl)-2-oxazolidinones
Valente, Sergio,Tomassi, Stefano,Tempera, Giampiero,Saccoccio, Stefania,Agostinelli, Enzo,Mai, Antonello
supporting information; experimental part, p. 8228 - 8232 (2012/01/06)
Monoamine oxidases (MAOs) are involved in various psychiatric and neurodegenerative disorders; hence, MAO inhibitors are useful agents in the therapy of Parkinson's disease, Alzheimer's dementia, and depression syndrome. Herein we report a novel series of 3-(1H-pyrrol-3-yl)-2-oxazolidinones 3-7 as reversible, highly potent and selective anti-MAO-A agents. In particular, 4b, 5b, and 4c showed a Ki-MAO-A of 0.6, 0.8, and 1 nM, respectively, 4c being 200000-fold selective for MAO-A with respect to MAO-B.
Bu3SnH-mediated radical cyclisation onto azoles
Allin, Steven M.,Barton, William R.S.,Russell Bowman,Bridge (née Mann), Emma,Elsegood, Mark R.J.,McInally, Tom,McKee, Vickie
, p. 7745 - 7758 (2008/12/21)
Alkyl radicals have been cyclised onto pyrroles, imidazoles and pyrazoles, and acyl radicals cyclised onto pyrroles, using Bu3SnH-, (TMS)3SiH- and Bu3GeH-mediated aromatic homolytic substitution for the synthesis of bicyclic N-heterocycles. The reactions yield intermediate π-radicals that lose hydrogen in the?rearomatisation step of the aromatic homolytic substitution. Mechanistic studies of these rearomatisation steps indicate aromatic homolytic substitution in which the initiator or breakdown products from the inhibitor are responsible for the H-abstraction step.
Acyl radical cyclisation onto pyrroles
Allin, Steven M.,Barton, William R.S.,Bowman,McInally, Tom
, p. 7887 - 7890 (2007/10/03)
Synthetically useful [1,2-a]-fused pyrroles, e.g. 2,3-dihydro-1H-pyrrolizidines substituted in the 1- and 7-positions, have been generated by acyl radical cyclisation onto pyrroles using N-(ω-acyl)-radicals generated from acyl-selenide precursors. The protocol does not require high pressures of CO. Mechanistic studies indicate the key role of azo radical initiators as oxidants of the intermediate π-radicals.
