Copper-Catalyzed Asymmetric Radical Oxysulfonylation of 2-Vinylbenzoic Acids to Access Chiral Sulfonyl Phthalides.

This study presents the development of a radical enantioselective alkene oxysulfonylation approach for the synthesis of enantioenriched sulfonyl phthalides via a catalyst system consisting of a copper salt and an OPPA ligand. The reaction proceeded under mild conditions with a wide range of substrates, good yields, and excellent enantioselectivities. Mechanistic studies suggested that the reaction proceeded through a radical-mediated process.

Design, synthesis and evaluation of a series of potential prodrugs of a Bruton's tyrosine kinase (BTK) inhibitor.

BTK has become a particularly attractive therapeutic target in autoimmune diseases and B-cell malignancies, making BTK inhibitors a valuable and important therapeutic option. We present the design, synthesis, and evaluation of a series of prodrugs of a BTK inhibitor with an insoluble 2,5-diaminopyrimidine structure. Tails containing different solubilizing groups were added to the parent molecule an ester linkage.

Wedelolactone metabolism in rats through regioselective glucuronidation catalyzed by uridine diphosphate-glucuronosyltransferases 1As (UGT1As).

Background: Wedelolactone (WEL), a medicinal plant-derived coumestan, has been reported to exhibit a diverse range of pharmacological activities. However, the metabolism and disposition of WEL remain unexplored.

Purpose: The present study aims to investigate the metabolism of WEL in rats and identify the enzymes responsible for forming major WEL metabolites.