Facile synthesis of an azido-labeled thalidomide analogue.

Org Lett

Department of Chemistry, University of Virginia, P.O. Box 400319, Charlottesville, Virginia 22904, USA.

Published: August 2003

[reaction: see text] A five-step synthesis of an azido-thalidomide analogue is presented. The sequence requires cheap and readily available starting materials and reagents, and only two steps require purification. Additionally, the azido-labeled analogue possesses activity comparable to that of thalidomide in inhibiting the proliferation of human microvascular endothelial cells, thus providing impetus for its use as a potential photoaffinity label of thalidomide.

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http://dx.doi.org/10.1021/ol034906wDOI Listing

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