A facile method for preparing various functional cycloalkynes, including proteins installed with a cycloalkyne moiety, from corresponding azides is developed. Treatment of diynes bearing strained and terminal alkyne moieties with a copper salt enabled the terminal alkyne-selective click conjugation with azides, whereas a more azidophilic strained alkyne moiety was transiently protected from click reaction by complexation with copper.

JOURNAL:
Chemical Communications

TITLE:
A facile preparation of functional cycloalkynes via an azide-to-cycloalkyne switching approach

DOI:
https://pubs.rsc.org/en/Content/ArticleLanding/2019/CC/C9CC01113G#!divAbstract

Takamitsu HOSOYA, Ph.D.,Professor
Department of Chemical Bioscience
Institute of Biomaterials and Bioengineering,
Tokyo Medical and Dental University(TMDU)
E-mail:thosoya.cb(at)tmd.ac.jp

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