A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thio...A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thioureas) 4 by treatment with isocyanates (isothiocyanates). Preparation of the hydro-uracils and thiouracils 5 is achieved by acidic cyclization-cleavage from the resin. The synthesis is designed to be amenable for structure based library approach to photosystem II D1 protein inhibitors.展开更多
文摘A general method for the solid phase synthesis of hydro-uracils and thiouracils is described. Resino ester 2 reacts with various primary amines to give secondary amines 3, which are converted to the resino ureas (thioureas) 4 by treatment with isocyanates (isothiocyanates). Preparation of the hydro-uracils and thiouracils 5 is achieved by acidic cyclization-cleavage from the resin. The synthesis is designed to be amenable for structure based library approach to photosystem II D1 protein inhibitors.
