Bisubstrate Ketone Analogues as Serotonin <i>N</i>-Acetyltransferase Inhibitors
作者:Cheol Min Kim、Philip A. Cole
DOI:10.1021/jm010049v
日期:2001.7.1
called the melatoninrhythmenzyme, is thought to play an important regulatory role in circadian rhythm in animals and people. A series of analogues were synthesized in which indole and coenzyme A were linked via ketone tethers as designed inhibitors of this enzyme. These compounds were tested against purified serotonin N-acetyltransferase. The parent ketone compound was found to be as potent as an amide
The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
In the presence of gold(I)–phosphine catalysts, alkenyl- and arylsilanes undergo intramolecular cyclisation reactions onto appendant alkyne moieties to afford 1-silaindene derivatives. The reaction pathways vary depending on the substituent on silicon.
Synthesis of Cyclopropanes via Organoiron Methodology: Preparation and Rearrangement of Divinylcyclopropanes
作者:Nathaniel J. Wallock、William A. Donaldson
DOI:10.1021/ol050637t
日期:2005.5.1
ntadienyl)iron(1+) cation generates the corresponding (2-alkenylpent-3-en-1,5-diyl)iron complexes. Oxidatively induced-reductive elimination of these complexes gives divinylcyclopropanes which can undergo subsequent Cope rearrangement to give 1,4-cycloheptadienes.