Pitt and FTI Research Team Announces New Methods to Synthesize Drug Candidates

Pittsburgh, March 1 -- Researchers from the University of Pittsburgh and Fluorous Technologies, Inc. (FTI) report in the March 2 issue of Science that they have developed new "fluorous mixture" techniques for synthesizing small organic molecules, which hold promise as potential drug candidates, as catalysts, and in many other types of applications. The techniques enable chemists to discover and optimize new and interesting molecules more quickly.

"Organic chemists have traditionally synthesized molecules one-by-one in a slow, painstaking process," explains research team leader Dennis P. Curran, a Pitt chemistry professor and founder and chief scientific officer of FTI. "This slow, serial process is now being augmented by more rapid parallel synthesis methods. However, both traditional and modern methods are limited because only one new compound is synthesized in each individual reaction vessel.

"The fluorous mixture synthesis methods we are introducing will allow organic chemists to better use both methods by making more than one compound per vessel. We already make four, or even eight, compounds per reaction vessel with just a little more effort and expense than making one compound. However, unlike past mixture methods, our final products are not a mixture but individual pure compounds."

"Our scientists already are using fluorous mixture synthesis techniques here in our labs to make libraries," explains Philip E. Yeske, executive vice president and chief operating officer of FTI. "We initially will use the technology to create chemical libraries for contract partners, but we already are evaluating plans to commercialize both the tags and separation media so that others can use the techniques."

In fluorous mixture synthesis methods, members of a series of simple starting compounds are tagged with a corresponding series of fluorous tags and then mixed and converted over several reactions to new, more complex products. In the key step, the mixtures are then "de-mixed," or separated. The products emerge in order of increasing fluorine content of the tag, and then the tags are removed to yield the individual pure products.

"The fluorous tag is the key," comments Curran. "The inherent efficiency of making more compounds as mixtures has not been reaped in solution phase synthesis before now, because there has been no way to separate the mixtures or to identify the resulting products if the separation problem is solved. Fluorous tagging solves both of these problems. We know that the separation will be possible because it is controlled by the tag, and we know which final product is which simply because we know which starting material got each individual tag."

In addition to Curran, the Bayer Professor and Distinguished Service Professor of Chemistry at the University of Pittsburgh, the team includes Pitt graduate student Qisheng Zhang and postdoctoral fellow Yoji Oderaotoshi, and FTI Senior Scientist Zhiyong Luo. Before joining FTI, Luo did graduate and postdoctoral work in the chemistry department at Pitt. The University of Pittsburgh has filed for patent protection on the new invention and granted an exclusive license on the pending patents to Fluorous Technologies, Inc.

Fluorous Technologies is a new chemical company located in Pittsburgh and founded upon proprietary fluorous chemistry technologies for synthesis and separation of small organic molecules. For additional information, visit www.fluorous.com or contact info@fluorous.com.

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