Higher Yield Synthetic Route To Cyclic Enediynes Developed

Abstract

patent has been awarded for a cyclization reaction that makes it possible to synthesize cyclic enediyne compounds in yields as high as 92%—compared with about 2.5% for the reaction used most frequently until now. The new synthesis can be used to make combinatorial libraries of enediyne compounds as a source of potential anticancer drugs and other therapeutics. The cyclization is covered by U.S. Patent No. 5,436,361, issued on July 25. The inventors are chemistry professor Graham B. Jones and graduate student Robert S. Huber of Clemson University, Clemson, S.C. A lot of other people in the field have been working on this, says Jones. Waiting for the patent held us up for a year, but we can now begin to show the world what we've got. I really think there's something here because we can synthesize enediynes on such a large scale that it really is a possibility now to make libraries with these ...