A Versatile New Substituent for Optimizing the Structures of Drugs and Crop Protection Agents is Now Available

New substituent of the future The 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.

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TrifluoromethylatorCatylix, Inc. and Aspira Scientific announced today a cooperation to produce and distribute Catylix’s breakthrough reagent for trifluoromethylation. The reagent will be produced and distributed by Aspira under sublicense from Catylix. Trifluoromethylator® reagent is available now in sizes ranging from 1 gram to multi-kilograms. Through their recently announced joint venture the companies are planning for future production of Trifluoromethylator® to meet demand in multi-ton quantities.

Based on the discoveries of Professor John Hartwig, now at the University of California Berkeley, Trifluoromethylator® offers a number of advantages for adding trifluoromethyl groups to aryl, heteroaryl, and vinyl compounds. The reagent is shelf stable, functions at or near ambient temperature, and has unprecedented functional group compatibility. “Trifluoromethylator® is the fastest, easiest way to add a trifluoromethyl group to almost any aryl iodide or bromide. Through this new cooperation with Aspira, the availability of Trifluoromethylator® will be expanded, and we will be working to bring down the cost for large scale applications so that chemists will enjoy the benefits of this reagent from lab scale to commercial scale.”

Trifluoromethylation is a frequently used chemical reaction, particularly in the pharmaceutical and crop protection industries. Dr. John Chan, CEO of Aspira commented, “We are delighted to bring Aspira’s expertise in distribution and production to make this breakthrough trifluoromethylation reagent more widely available to both researchers and process chemists. As we bring down the cost, we anticipate wider application and significantly increased demand.” More information is available on the Aspira web site: http://aspirasci.com/trifluoromethylator.

Dr. David Rozzell, CEO of Catylix, and Dr. John Chan, CEO of Aspira Scientific, will be available for consultations and meetings during the 2014 ACS Meeting and Exhibition in San Francisco on August 11 and 12 at Booth 1136.

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Catylix and Aspira Scientific Create Joint Venture for Novel Fluorinated Compounds

July 31, 2014

Catylix, Inc. (Burbank, California) and Aspira Scientific (Milpitas, California) announced today the formation of a joint venture to develop and commercialize new fluorination products and related chemistry. 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 improve binding and […]

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What is the New Substituent of the Future?

May 16, 2014

Much has been written in recent years about SF5 as the “substituent of the future.” By bringing the troika of enhanced lipophilicity, electronegativity, and metabolic stability into medicinal chemistry, the SF5 functional group has been widely considered to offer a path to the discovery of new chemical entities with features that are desirable in drug […]

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Catylix and SpiroChem Announce Cooperation in Fluoroalkylation

May 6, 2013

Catylix and SpiroChem are pleased to announce a cooperation for the development and sale of novel fluoroalkylated building blocks and custom synthesis services.   Novel fluorine-containing building blocks and custom synthesis services for fluoroalky-substituted compounds are available from SpiroChem and Catylix through a new cooperation between the companies. This strategic cooperation will offer both products […]

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Trifluoromethylator Scaled-Up Enabling Larger-Scale Trifluoromethylation

January 10, 2013

Catylix has  successfully scaled-up the synthesis of its trifluoromethylation reagent, (1,10-phenanthroline trifluoromethylcopper). Trademarked as  Trifluoromethylator®, Catylix’s shelf-stable reagent for trifluoromethylation has unprecedented functional-group compatibility, allowing the derivatization of a broad range of aryl and vinyl iodides and bromides with a CF3 group under mild, near-ambient conditions.  The Trifluoromethylator® reagent is currently distributed for Catylix through […]

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Trifluoromethylation Reagent Featured in Technology Spotlight

August 18, 2011

Trifluoromethylator (TM), the trifluoromethylation reagent developed by John Hartwig and co-workers, is now featured in a Technology Spotlight by Sigma-Aldrich. See examples of trifluoromethylation reactions with Catylix’s new Trifluoromethylation Reagent

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Hartwig Trifluoromethylation: A New Broadly Useful Trifluoromethylation Reagent

July 11, 2011

Catylix, Inc. has launched its first product: a new reagent for trifluoromethylation with broad applications for chemists in the life sciences. Sold under the trade name Trifluoromethylator (TM), Catylix’s product is the first trifluoromethylation reagent that is Stable Tolerant of a wide range of other chemical functionality Usable at or near room temperature without a […]

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Catylix Licenses Hartwig Trifluoromethylation Technology

July 7, 2011

Trifluoromethylation has been a long-standing challenge for chemists, particularly for compounds containing additional functionality. Most trifluoromethylation methods require harsh conditions, and the reaction scope is limited. A new broadly-useful method for trifluoromethylation of aryl and vinyl iodides was recently developed by Professor John Hartwig and co-workers at the University of Illinois. Using a copper phenanthroline […]

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Catylix, Inc. Launches

February 3, 2011

Catylix, Inc. was created to exploit the importance of fluorine-containing functionality for improving the pharmacokinetic properties of bio-active compounds. Technology developed by Professor john Hartwig at the University of Illinois for the introduction of fluorine-containing substituents into molecules.

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