Tag-and-Release Synthesis

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Science  20 Oct 2000:
Vol. 290, Issue 5491, pp. 409
DOI: 10.1126/science.290.5491.409a

The solid-phase supports used in combinatorial chemistry help to keep track of different compounds that have been synthesized or separated. However, the final cleavage step from the resin or bead has rarely been used to introduce chemical diversity.

Nicolaou et al. report that olefin compounds can be derivatized and attached to solid supports through an α-sulfonated ketone “tag,” and then released using numerous different chemical reactions to create libraries of new compounds. Several of these reactions yielded heterocyclic compounds, such as those containing diamines and dithiols. — PDS

J. Am. Chem. Soc., in press.

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