An improved synthesis of rupintrivir (AG7088) was accomplished using three amino acids (L-glutamic acid, D-4-fluorophenylalanine, and L-valine) as the building blocks. The key fragment ketomethylene dipeptide isostere was constructed with the valine derivative and phenylpropionic acid derivative, followed by coupling with a lactam derivative and an isoxazole acid chloride to provide AG7088 totally in eight steps.
LIN DaiZongQIAN WangKeHILGENFELD RolfJIANG HuaLiangCHEN KaiXianLIU Hong
Soft corals of the genus Sinularia are one of the most widespread soft corals.They are a rich source of bioactive su bstances with intriguing and unique structural features.The present paper reviews the latest progress in the chemistry and pharmacological activities of terpenoids from Sinularia soft corals and provides a perspective on future areas of research interest.
A series of A-B type sterically regular bicyclio[3.3.0] diene-based polymers were designed and synthesized as immobilized chiral diene ligands for asymmetric catalysis. With polymeric diene 6b, good to excellent enantiose- lectivities can be achieved in Rh-catalyzed asymmetric 1,4-addition of arylboronic acids to a,β-unsaturated ketones.