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Quantitative Determination of Click Reaction in the Presence of Glycine Derivatives and in Dilute Solution

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Author(s): Yui Ogasawara | Yuta Murai | Yasuko Sakihama | Yasuyuki Hashidoko | Makoto Hashimoto

Journal: International Journal of Organic Chemistry
ISSN 2161-4687

Volume: 02;
Issue: 03;
Start page: 302;
Date: 2012;
Original page

Keywords: Click Chemistry | Quantitative Determination | Propargylglycine | Cu(I) | Buffer

ABSTRACT
The click reaction is one of the latest techniques for the functional analysis of bioactive compounds and the analysis makes novel concepts and strategies for medicinal chemistry. N-methylated glycine derivatives have inhibitory activity for the click reaction in direct Cu(I) system because of decrease of Cu(I) concentration. The Cu(I) concentration recovered effectively by sodium ascorbate. Quantitative determination of click reaction at various ligand concentrations revealed that the decrease in reaction yields was observed in a substrate concentration-dependent manner.
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