摘要
Based on the binding mode for hydrouracil in photosystem II (PS II) Dl protein, a general method for the solid phase combinatorial synthesis of hydrouracil library was developed. The acryloyl chloride or acid were coupled to Wang resin1 to afford the acryloyl ester2. Resin bound ester2 reacted with various primary amines to give secondary amines3, which were converted to the resin bound ureas4 by treatment with isocyanates. Preparation of the hydrouracils5 was achieved by the acidic cyclization-cleavage from the resin. For characterization purposes,8 hydrouracil analogues were synthesized in parallel, following which a small library of9 hydrouracil derivatives was prepared after cleavage from Wang resin. All the9 bydrouracil derivatives desired were identified by GCMS.
Based on the binding mode for hydrouracil in photosystem II (PS II) D1 protein, a general method for the solid phase combinatorial synthesis of hydrouracil library was developed. The acryloyl chloride or acid were coupled to Wang resin 1 to afford the acryloyl ester 2. Resin bound ester 2 reacted with various primary amines to give secondary amines 3, which were converted to the resin bound ureas 4 by treatment with isocyanates. Preparation of the hydrouracils 5 was achieved by the acidic cyclization_cleavage from the resin. For characterization purposes, 8 hydrouracil analogues were synthesized in parallel, following which a small library of 9 hydrouracil derivatives was prepared after cleavage from Wang resin. All the 9 bydrouracil derivatives desired were identified by GC_MS.
基金
ProjectsupportedbytheNationalNaturalScienceFoundationofChina (GrantNo .2 970 2 0 0 6)andtheNaturalScienceFoundationofTianjinMunicipality
