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Functionalised polymer supports for solid-phase synthesis

机译:用于固相合成的功能化聚合物载体

摘要

Polymer supports are claimed which have a methacryloyl group of formula P-Z-CO-C(=CR1R2)-CR3R4-X (I). P = a natural, semisynthetic or synthetic polymer support; R1, R2 = H, alkyl, aryl or halogen; R3, R4 = H, alkyl or aryl; X = group suitable for coupling chosen from OH, halo, sulphonate, phosphonate, azido, amino, alkoxy, thioether, amido or acyloxy (derived from carboxylic acid); Z = alkylene, NH, NR or O; R is not defined. Also claimed is a process for synthesising optionally protected peptides, oligosaccharides, glycopeptides, nucleotides or proteins, by cleaving a compound (I; X = alkoxy or COR) by reaction with a nucleophile, or by cleaving a compound (I; X = acyloxy) with a catalytic amount of Pd. R = organic residue, and COR = is especially the optionally protected residue of an aminoacid, peptide or glycopeptide; alkoxy = residue of an alcohol, especially the optionally protected residue of a saccharide or nucleotide.
机译:要求保护的聚合物载体具有式P-Z-CO-C(= CR 1 R 2)-CR 3 R 4 -X(I)的甲基丙烯酰基。 P =天然,半合成或合成聚合物载体; R1,R2 = H,烷基,芳基或卤素; R3,R4 = H,烷基或芳基; X =适于偶合的基团,选自OH,卤素,磺酸盐,膦酸酯,叠氮基,氨基,烷氧基,硫醚,酰胺基或酰氧基(衍生自羧酸); Z =亚烷基,NH,NR或O; R未定义。还要求保护的是通过与亲核试剂反应裂解化合物(I; X =烷氧基或COR)或裂解化合物(I; X =酰氧基)来合成任选保护的肽,寡糖,糖肽,核苷酸或蛋白质的方法。催化量的钯R =有机残基,并且COR =尤其是氨基酸,肽或糖肽的任选保护的残基;烷氧基=醇的残基,特别是糖或核苷酸的任选被保护的残基。

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