Publications by authors named "Rebekah J Carson"
Article Synopsis
- Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) has led to new molecules that can effectively inhibit HIV integrase variants while reducing enterohepatic recirculation in rats.
- Structure-activity relationships identified modifications at the C6 position that minimized enterohepatic recirculation and allowed for better potency against HIV variants.
- The final result is compound 20, which shows promising antiviral efficacy and reduced biliary excretion, making it a potential candidate for clinical HIV treatment.
A one-pot, two-step process that transforms terminal alkynes into ethyl methyl-substituted benzylic quaternary carbon centers is described. (E)-2,2-Disubstituted-1-alkenyldimethylalanes have been shown to participate in 1,2-alkyl migration from aluminum to carbon with concomitant arylation at the 2-position to furnish ethyl methyl-substituted benzylic quaternary carbon centers, when reacted intramolecularly with aryl halides and triflates in the presence of a Pd(0) catalyst. The protocol is initiated with Cp2ZrCl2-catalyzed methylalumination of terminal alkynes followed by palladium-catalyzed intramolecular arylation of the resulting (E)-2,2-disubstituted-1-alkenyldimethylalanes, leading to 1,2-methyl shift from aluminum to carbon.
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