Highly selective sialylation and total syntheses of tumor-related antigens N3 by the iterative one-pot synthesis strategy

ORGN 411

Bin Sun, bin.sun@utoledo.edu, Youling Zeng, youlinzengcn@gmail.com, and Xuefei Huang, xuefei.huang@utoledo.edu. Department of Chemistry, The University of Toledo, 2801 W. Bancroft Street, MS 602, Toledo, OH 43606
There are two parts of this poster. One is the synthesis of an N-trichloroacetyl derivative of neuraminic acid with phenyltrifluoroacetimidate as the anomeric leaving group. This new glycosyl donor reacted with p-tolyl-1-thio-4,6-O-benzylidene-β-D-galactopyranoside, and exhibited exclusive α selectivity in 60% yield. The influences of solvent, additives and concentration of promoter (TMSOTf) on sialyation were investigated. The other part is the total syntheses of two octasaccharides tumor associated antigens N3 major and N3 minor by using the iterative one-pot strategy. The building blocks triaccharide Lea and trisaccharide Lex were constructed using p-tolyl-1-thio-galactoside as the donor and partially protected p-tolyl-1-thio-glucoside as the acceptors via stereoselective condensation reactions. The strategy proved that complex molecules can be rapidly assembled using near stoichiometric amount of building blocks.