| 主权项 |
1. A method for preparing a pentasaccharide having the sequence α-L-Rhap-(1→3)-β-D-Glcp-(1→4)-[α-L-Rhap-(1→3)]-α-D-Glcp-(1→2)-α-D-Glcp and represented by structure 1 or 1′ or a derivative thereof in which at least one hydroxyl group thereof is substituted by at least one other functional group or atom, said method comprising a) assembling a monosaccharide building block 2′, wherein the specific protected amino linker of building block 2 is replaced by a different protected or unprotected linker L, and building blocks 3 or 4 to yield the corresponding disaccharide 21′, reacting the disaccharide 21′ with building block 4 to form the trisaccharide 23′, subjecting the trisaccharide 23′ to a bis-glycosylation reaction with 2 molecules of building block 5 to yield the corresponding fully protected pentasaccharide 24′ and finally, after deprotection, to yield pentasaccharide 1′, wherein the specific amino linker of pentasaccharide 1 is replaced by a different linker L, or b) assembling a monosaccharide building block 2′, wherein the specific protected amino linker of building block 2 is replaced by a different protected or unprotected linker L, and building block 27 to yield the corresponding disaccharide 30′, reacting the disaccharide 30′ with building block 4 or 29 to form the corresponding protected trisaccharide 32′, deprotecting the trisaccharide 32′ to obtain trisaccharide 33′, subjecting the trisaccharide 33′ to a bis-glycosylation reaction with 2 molecules of building block 5 to yield the corresponding fully protected pentasaccharide 34′ and finally, after deprotection, to yield pentasaccharide 1′, wherein the specific amino linker of pentasaccharide 1 is replaced by a different linker L, wherein the different linker L is (CH2)nNH2, with n being an integer from 2 to 50, and where 2, 2′, 3, 4, 5, 21′, 23′, 24′, 27, 29, 30′, 32′, 33′, 34′ are defined as follows: |
