A Versatile New Substituent for Optimizing the Structures of Drugs and Crop Protection Agents is Now AvailableThe New Substituent of the Future
Catylix, Inc. (Burbank, California) and Aspira Scientific (Milpitas, CA) announce today the launch of the “New Substituent of the Future” for the discovery and development of novel bioactive compounds. Supported by technology developed by Prof. John F. Hartwig at University of California Berkeley, Catylix and Aspira are commercializing new building blocks and chemistry for the broad introduction of the fluorine-containing functional group pentafluoroethyl (C2F5)—the New Substituent of the Future.
Developing improved biologically active molecules has benefited from the use of substituents that are chemically stable, resistant to metabolism, and combine lipophilicity with polarity to modulate receptor binding and bioavailability. Fluorinated functional groups, in particular, have been used to accomplish these objectives, and the benefits of fluorine are well-appreciated by medicinal chemists and crop protection scientists. It is estimated that more than 25% of small-molecule drugs currently under development contain fluorine.
In launching pentafluoroethyl as the New Substituent of the Future, Catylix and Aspira are making available the C2F5 substituent to provide benefits that improve the performance of prospective drugs and crop protection agents: 1) size intermediate between trifluoromethyl and t-butyl; 2) combination of lipophilicity and eletronegativity which can improve bioavailability; and 3) high metabolic and chemical stability.
Most importantly, pentafluoroethylbrings the additional important benefit of broad synthetic access, allowing incorporation into almost any position of an aryl or heteroaryl ring, or attached to almost any carbon-carbon double bond. “Incorporating the C2F5 substituent offers the potential for creating patentable new compounds with superior biological activity,” stated Dr. David Rozzell, CEO of Catylix. “Furthermore, the methods developed by Catylix for introducing the pentafluoroethyl group promise to be scalable, efficient, and cost-effective.”
To help chemists evaluate pentafluoroethyl as the New Substituent of the Future, Catylix and Aspira are launching a new product line focused on C2F5-containing compounds called Penta-F-Blocks. Dr. Rozzell explained, “All Penta-F-Blocks are pre-functionalized with the C2F5 group and contain an additional ‘chemical handle’ allowing the straightforward incorporation of the pentafluoroethyl fragment into the synthetic route of a more complex molecule.”
Sales will be handled through the recently-announced joint venture between Catylix and Aspira Scientific. Dr. John Chan of Aspira commented, “We are excited to work with Catylix to bring the New Substituent of the Future into the mainstream of modern synthetic chemistry. Our production and distribution will make pentafluoroethyl-substituted building blocks available to research and process chemists world-wide.”
In addition to offering novel Penta-F-Blocks, Catylix and Aspira also provide synthesis of compounds containing the C2F5 functional group on a custom basis.