SciFluor Life Sciences' Founders Author Review Article in Nature on Advances to Overcome Challenges Associated with Fluorination
--Fluorination holds significant promise to improve biopharmaceutical drug properties--
BOSTON--(BUSINESS WIRE)--May 27, 2011 - SciFluor Life Sciences, LLC today announced the publication of a review paper detailing the intricate challenges associated with fluorination and recent advancements in the field to help overcome these challenges. Adding fluorine to organic molecules, such as pharmaceuticals, can significantly improve drug properties. Fluorination also plays an integral role in the development and production of agrochemicals, advanced materials, and as tracers for positron emission tomography. Fluorinated organic molecules, while often valuable, have been generally challenging to synthesize efficiently. Advancements made in fluorination reactions over the last five years, including SciFluor's late-stage fluorination technology, are now enabling complex fluorinated molecules that previously were not readily available.
The paper, “Catalysis for fluorination and trifluoromethylation,” was published in the May 26, 2011 issue of the journal Nature and includes a discussion of the fundamental challenges of organofluorine chemistry and new bond-forming reactions designed to incorporate fluorine into organic molecules that are not readily synthesized using traditional fluorination chemistry. In particular, the review discusses novel transition-metal-catalysed and organocatalysed C-F and C-F3 bond forming reactions. Recent successes in fluorine incorporation can be attributed to the design of these previously unavailable transition metal complexes, and the merger of modern synthesis techniques, such as organocatalysis, with fluorination chemistry. As a result of these advances, particularly in medicinal chemistry, functionalized fluorinated molecules are more readily accessible now than ever.
Dr. Tobias Ritter, scientific founder and Chief Technical Officer of SciFluor and an author of the paper, commented, “Fluorination of molecules can be beneficial across multiple applications and, in particular, for the development of pharmaceuticals. Despite fluorine's utility, the fluorination process – particularly late-stage fluorination – is often challenging and expensive in complex molecules. Recent advances in the field have begun to address some of the challenges in fluorine chemistry and may inform the evolving landscape of fluorination going forward.” Dr. Ritter is an Associate Professor of Chemistry and Chemical Biology at Harvard, and is a recognized expert in organo-metallic chemistry and fluorine chemistry.
SciFluor is playing a role in addressing challenges specifically related to late-stage fluorination. The Company's proprietary fluorine substitution technology, which enables late- or any-stage fluorination of a wide variety of organic compounds, has demonstrated its ability to overcome barriers in fluorination and has been used to make fluorinated analogs of multiple pharmaceuticals. Adding fluorine can improve drug properties, including metabolic stability, potency, binding affinity, bioavailability, and blood-brain-barrier penetration. The Company's technology is exclusively licensed from Harvard University.
SciFluor's late-stage fluorination technology has been validated across multiple therapeutic areas, including CNS, Infectious disease, Cardiovascular disease and Oncology, with proof-of-concept achieved via fluorinating dozens of marketed compounds. This technology has the potential to add value across the entire drug development process, including: lead optimization, preclinical and clinical development of novel new chemical entities, accessing inaccessible or unexplored therapeutics and lifecycle management of drugs with soon-to-expire patents.
SciFluor Life Sciences is an Allied Minds-funded company with a late-stage fluorination technology that improves drug properties such as metabolic stability, potency, bioavailability, and blood-brain barrier penetration. The company's late-stage fluorination technology, and its companion portfolio of fluorinated pharmaceuticals, are licensed exclusively from Harvard University. SciFluor's technology enables end-stage or any-stage fluorination of a wide variety of organic compounds. www.scifluor.com
Contact: for SciFluor Life Sciences, LLC
Jennifer Conrad, 781-235-3060
Posted: May 2011