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Solid supports for the synthesis of compounds having an alpha-oxo-aldehyde group and peptides, made by solid phase synthesis using such supports
Solid supports for the synthesis of compounds having an alpha-oxo-aldehyde group and peptides, made by solid phase synthesis using such supports
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机译：用于合成具有α-氧-醛基的化合物和肽的固体载体，通过使用这种载体进行固相合成制得
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摘要
Solid supports, functionalized for the synthesis of compounds having an alpha -oxo-aldehyde group, a process for the synthesis of such compounds, and peptides made by the process. The solid supports are of formula (I): S = a solid support capable of being solvated on the surface by an aqueous or partially aqueous solvent; n and m = 0 or 1; Z when n is 1 = ether, thioether, ester, amine, amide, sulfonamide, hydroxylamine, hydrazine, hydrazone, thiazolidine, oxime, carbonate, carbamate, thiocarbamate, urea, or thiourea group, or their derivatives, or, when n is 0, it is ester, amide, N-acylhydroxylamine, hydrazide, hydrazone, oxime, or thiazolidine group, or their derivatives; P1 and P2 are the same or different or form a ring with the O atoms to which they are attached, and = H or protecting groups selected from R1, -COR1, -COOR1, -SO2OR1, -SiR'RR'', acetals, ketals; A and B = a chain that may be cyclic and may be unsaturated of 1-18C atoms and optionally 1 - 7 substituents from carbonyl, carbocyclic, heterocyclic, aryl, or heteroaryl, with A and/or B optionally containing 1 - 16 heteroatoms and optionally substituted by 1-16 OH or amino groups, that may be protected, at least one of A and B being optionally substituted by a group of formula II); R1, R', R, and R'' = 1-18C alkyl, that may be cyclic and may be unsaturated, aryl, or heteroaryl, (optionally substituted by one or more halogens, amino, OH, alkoxy, aryloxy, alkylthio or arylthio); A' = a group as defined for A; and X' = -OR1, or -NR'R where, in formula (II) R1, R' and R may also be H. Independent claims cover peptides having an alpha -oxoaldehyde group situated in a position other than a N-terminal extremity and not being linked through amide to an amine on a side chain of lysine or ornithine, prepared using a support as described.
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