Synthesis of Full Agonists of the Rev-Erb Receptor
Start Date
April 2026
Location
2nd floor - Library
Abstract
Nuclear Receptor Subfamily 1, Group D, Member 1 and 2 (Rev-Erb) is a nuclear receptor involved in circadian rhythm and metabolic regulation, making it an attractive target for therapeutic development. Consistent with the Mullins Lab's mission to synthesize medicinally relevant molecules, we are using a convergent approach for the construction of Rev-Erb agonists from the public domain to use for benchmarking purposes. Our approach begins with the preparation of a common headpiece featuring a triazolopyridazine for coupling with three distinct phenolic biaryl compounds. The phenolic biaryls are prepared via bromination of trifluoromethyl-substituted phenols followed by palladium-catalyzed cross-coupling reactions of each. Once synthesized, the triazolopyridazine will be coupled with the phenolic biaryls to produce the potential Rev-Erb agonists. This presentation will focus on the synthesis and biological evaluation of the derivatives thus obtained.
Synthesis of Full Agonists of the Rev-Erb Receptor
2nd floor - Library
Nuclear Receptor Subfamily 1, Group D, Member 1 and 2 (Rev-Erb) is a nuclear receptor involved in circadian rhythm and metabolic regulation, making it an attractive target for therapeutic development. Consistent with the Mullins Lab's mission to synthesize medicinally relevant molecules, we are using a convergent approach for the construction of Rev-Erb agonists from the public domain to use for benchmarking purposes. Our approach begins with the preparation of a common headpiece featuring a triazolopyridazine for coupling with three distinct phenolic biaryl compounds. The phenolic biaryls are prepared via bromination of trifluoromethyl-substituted phenols followed by palladium-catalyzed cross-coupling reactions of each. Once synthesized, the triazolopyridazine will be coupled with the phenolic biaryls to produce the potential Rev-Erb agonists. This presentation will focus on the synthesis and biological evaluation of the derivatives thus obtained.
