Incorporation of carbohydrates and peptides into large triazine-based screening libraries using automated parallel synthesis

A procedure for the sequential, selective derivatization of cyanuric chloride that allows for the incorporation of carbohydrates and peptides has been elucidated. As a result, large combinatorial arrays of individual derivatives, over 40,000 in all, have been produced in 50μmole quantities using aut...

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Bibliographic Details
Published in:Tetrahedron 1998-04, Vol.54 (16), p.4051-4065
Main Authors: Gustafson, Gary R., Baldino, Carmen M., O'Donnell, Mary-Margaret E., Sheldon, Adrian, Tarsa, Robert J., Verni, Christopher J., Coffen, David L.
Format: Article
Language:English
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Summary:A procedure for the sequential, selective derivatization of cyanuric chloride that allows for the incorporation of carbohydrates and peptides has been elucidated. As a result, large combinatorial arrays of individual derivatives, over 40,000 in all, have been produced in 50μmole quantities using automated parallel solution phase synthesis. The use of this technology in a search for protease inhibitors, glycopeptide surrogates and other bioactive compound classes will also be discussed. A procedure for the sequential, selective derivatization of cyanuric chloride that allows for the incorporation of carbohydrates and peptides has yielded over 40,000 individual derivatives to date in 50 μmole quantities using automated parallel solution-phase synthesis.
ISSN:0040-4020
1464-5416
DOI:10.1016/S0040-4020(98)00134-3