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Structure Based Library Approach to Photosynthesis Inhibitors:The Solid Phase Synthesis of Hydro-Uracils and Thiouracils
作者姓名:Ai  Ming  Yu  and  Hua  Zheng  YANG
作者单位:Ai Ming Yu and Hua Zheng YANG(State Key Laboratory of Elemento-Organic Chemistry,Nankai University,Tianjin 300071
摘    要:Combinatorialchemistryhasemergedasanefficienttoolforchedriststosynthesize"comPoundslibraries"fortheraPididentificationandoPtforizationofnewleads-lSolidphaseorganicsynthesisprovidesaraPidmeansforpreparationofcomPoundslibraries,andhasbeenusedfortheconstrUctionofoligomericcomPounds,'andsmallorganicmoleculessuchasbenzodiazepine,'9-lactams,'andquinolones.'ThemajortargetfortheinhibitionofphotosystemII(PSII)istheDlprotein,apolyPePtidewithamolecularweightof32kDa.'Wehavedevelopedmodelsoftheher-b…


Structure Based Library Approach to Photosynthesis Inhibitors:The Solid Phase Synthesis of Hydro-Uracils and Thiouracils
Ai Ming Yu and Hua Zheng YANG.Structure Based Library Approach to Photosynthesis Inhibitors:The Solid Phase Synthesis of Hydro-Uracils and Thiouracils[J].Chinese Chemical Letters,1998(2).
Authors:Ai Ming Yu and Hua Zheng YANG
Abstract:A general method for the solid phase synthesis of hydro-uracils and thiouracils is de-scribed. 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 photosys-tem II D1 protein inhibitors.
Keywords:Solid Phase Synthesis  Hydro-Uracils and Thiouracils  Photosynthesis Inhibitors
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