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Synthetic Studies on Sialoglycoconjugates 66: First Total Synthesis of a Cholinergic Neuron-Specific Ganglioside GQ1bα1

 

作者: Kenji Hotta,   Hideharu Ishida,   Makoto Kiso,   Akira Hasegawa,  

 

期刊: Journal of Carbohydrate Chemistry  (Taylor Available online 1995)
卷期: Volume 14, issue 4-5  

页码: 491-506

 

ISSN:0732-8303

 

年代: 1995

 

DOI:10.1080/07328309508005353

 

出版商: Taylor & Francis Group

 

数据来源: Taylor

 

摘要:

A first total synthesis of a cholinergic neuron-specific ganglioside, GQ1bα (IV3Neu5Acα, III6Neu5Acα, II3Neu5Acα2-Gg4Cer) is described. Regio- and stereo-selective monosialylation of the hydroxyl group at C-6 of the GalNAc residue in 2-(trimethylsilyl)ethylO-(2-acetamido-2-deoxy-3,4-O-isopropylidene-β-d-galactopyranosyl)-(1→4)-O-(2,6-di-O-benzyl-β-dgalactopyranosyl)-(1→4)-O-2,3,6-tri-O-benzyl-β-dglucopyranoside (4) with methyl (phenyl 5-acetamido-4,7,8,9-tetra-O-acetyl-3,5-dideoxy-2-thio-dglycero-dgalacto-2-nonulopyranosid) onate (5), and subsequent dimericsialylation of the hydroxyl group at C-3 of the Gal residue with methyl [phenyl 5-acetamido-8-O-(5-acetamido-4,7,8,9-tetra-O-acetyl-3,5-dideoxy-dglycero-α-dgalacto-2-nonulopyranosylono-1′,9-lactone)-4, 7-di-O-acetyl-3,5-dideoxy-2-thio-dglycero-dgalacto-2-nonulopyranosid]onate (7), usingN-iodosuccinimide (NIS)-trifluoromethanesulfonic acid (TfOH) as a promoter, gave the desired hexasaccharide8containing α-glycosidically-linked mono- and dimeric sialic acids. This was transformed into the acceptor9by removal of the isopropylidene group. Condensation of methylO-(methyl 5-acetamido-4,7,8,9-tetra-O-acetyl-3,5-dideoxy-dglycero-α-dgalacto-2-nonulopyranosylonate)-(2→3)-2,4,6-tri-O-benzoyl-1-thio-β-dgalactopyranoside (10) with9, using dimethyl(methylthio)sulfonium triflate (DMTST) as a promoter, gave the desired octasaccharide derivative11in high yield. Compound11was converted into α-trichloroacetimidate14,viareductive removal of the benzyl groups,O-acetylation, removal of the 2-(trimethylsilyl)ethyl group, and treatment with trichloroacetonitrile, which, on coupling with (2S,3R,4E)-2-azido-3-O-benzoyl-4-octadecene-1,3-diol (15), gave the β-glycoside16. Finally,16was transformed,viaselective reduction of the azido group, coupling with octadecanoic acid,O-deacylation, and hydrolysis of the methyl ester group, into the title ganglioside18in good yield.

 

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