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Synthetic Studies on Sialoglycoconjugates 82: First Total Synthesis of Sialyl Globopentaosyl Ceramide (V3Neu5AcGb5Cer) and its Positional Isomer (V6Neu5AcGb5Cer)1,2

 

作者: Hideharu Ishida,   Ryuichi Miyawaki,   Makoto Kiso,   Akira Hasegawa,  

 

期刊: Journal of Carbohydrate Chemistry  (Taylor Available online 1996)
卷期: Volume 15, issue 2  

页码: 163-182

 

ISSN:0732-8303

 

年代: 1996

 

DOI:10.1080/07328309608005436

 

出版商: Taylor & Francis Group

 

数据来源: Taylor

 

摘要:

The first, total synthesis of sialyl globopentaosyl ceramide (V3Neu5AcGb5Cer) and its positional isomer (V6Neu5AcGb5Cer) are described. α-Selective glycosylation of 2-(trimethylsilyl)ethylO-(2,3,6-tri-O-benzyl-β-D-galactopyranosyl)-(1→4)-2,3,6-tri-O-benzyl-β-D-glucopyranoside (7) with the suitably protected galactose donor, methyl 3-O-acetyl-2-O-benzyl-4,6-O-benzylidene-l-thio-β-D-galactopyranoside gave the desired trisaccharide, which was transformed into the trisaccharide acceptor, by removal of theO-acetyl group. Glycosylation of this acceptor with methyl 3-O-acetyl-4,6-O-benzylidene-2-deoxy-2-phthalimido-l-thio-β-D-galactopyranoside gave the globotetraose derivative, which was transformed into the acceptor12by removal of the phthaloyl andO-acetyl groups followed byN-acetylation. DMTST promoted coupling of this acceptor with methylO-(methyl 5-acetamido-4,7,8,9-tetra-O-acetyl-3,5-dideoxy-D-glycero-α-D-galacto-2-nonulopyranosylonate)-(2→3)-2,4,6-tri-O-benzoyl-l-thio-β-D-galactopyranoside afforded the desired sialyl globopentaoside derivative in good yield, which was transformed, by removal of the benzyl and benzylidene groups followed byO-acetylation, selective removal of the 2-(trimethylsilyl)ethyl group and subsequent imidate formation, into the final glycosyl donor17. Condensation of this imidate derivative with (2S,3R,4E)-2-azido-3-O-benzoyl-4-octadecene-1,3-diol (18) gave the β-glycoside, which on channeling through selective reduction of the azido group, coupling of the amino group with octadecanoic acid,O-deacylation and saponification of the methyl ester group, gave the title compound, sialyl globopentaosyl ceramide. The positional isomer was also obtained by coupling of the globotetraose acceptor with methylO-(methyl 5-acetamido-4,7,8,9-tetra-O-acetyl-3,5-dideoxy-D-glycero-α-D-galacto-2-nonulopyranosylonate)-(2→6)-2,4-di-O-benzoyl-3-O-benzyl-1-thio-β-D-galactopyranoside, followed by essentially the same procedure employed for the synthesis of sialyl globopentaosyl ceramide.

 

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