Since the first fluorine-containing drug was developed in 1957, the number of fluorinated drugs on the market has risen steadily. For instance, the fluorine-containing new drug of Larotrectinib (LOXO-101, ARRY-470) is an oral selective tropomyosin receptor kinase (TRK) inhibitor in clinical development for the treatment solid tumors harboring NTRK-fusion proteins. Its wide range of applications is due to the drastic influence on metabolic stability, lipophilicity, bioavailability, binding affinity and selectivity conferred by fluorinated substituents.
The fluorinating reagents are roughly divided into two groups: electrophilic and nucleophilic fluorinating reagents.
1. Electrophilic fluorinating reagents are those where the electron-deficient fluorine atom serves as reaction active species.The most electrophilic fluorinating reagents are ultimately derived from fluorine gas,which is not suitable for partial fluorination due to its high toxicity and strong oxidization.
2. Nucleophilic fluorinating reagents are those where the fluoride anion serves as reaction active species. The most basic nucleophilic fluorinating reagent is hydrogen fluoride,which is precluded to its use or generation highly valuable to fluorination chemistry due to its toxicity,corrosivity and its low reactivity resulting from high H-F bond energy.
Fluorine gas and hydrogen fluoride are classically used as fluorine sources, but they are highly toxic and corrosive and of requirements for special equipments and techniques. Therefore, alternate fluorinating reagents have been developped and will be explored accordingly with new fluorination methods. For example, 3,3-difluoro-1,2-diarylcyclopropenes (CpFluors) are a class of novel fluorination reagents with all-carbon scaffold(CCF reagents). They are crystalline, thermally stable, readily available, operationally simple and reactivity-tunable deoxyfluorinating reagents for the preparation of alkyl fluorides. In the selective and direct deoxyfluorination of multiple alcohos via nucleophilic fluorination, CpFluors (kumi2F35, kumi2F36 and kumi2F37) are important complementary toolbox to other representative SF reagents( such as DAST, Deoxo-Fluor, DAST Difluoro-sulfinium Salt, Morpho-DAST Difluorosulfinium Salt, Fluolead and PyFluor) and representative NCF reagents( such as Ishikawa reagent, DFMBA,TFFH and PhenoFluor).
With this in mind, we are devoted to identify and provide a growing product catalogue of new and novel alternative reagents for both nucleophilic and electrophilic fluorination. Along with these well-selected fluorinating reagents, we also provide a broad range of fluorinated building blocks for different applications. For instance, Sulfonyl fluoride electrophiles not only can be important sulfonyl halide precursors(e.g. perfluorooctanesulfonyl derivatives), but also they are new-recognized SuFEx clickable building blocks with significant utility as reactive probes in chemical biology, molecular pharmacology and drug development. With the right balance of biocompatibility(including aqueous stability) and protein reactivity, Sulfonyl Fluorides can specifically react with residues based on serine,threonine,tyrosine,lysine,cysteine and histidine.Sulfonyl fluoride probes will find greater utility in areas such as covalent protein modifier, covalent enzyme inhibition, target identification and validation and the mapping of enzyme binding sites, substrates and protein-protein interactions and post-polymerization modification(PPM) in material science.
Fluorinating Reagents Overview
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You can either buy our fluorinating reagents and then introduce fluorine atom into your own desired compounds, or you can simply order the building blocks pre-loaded with the fluorinated subsitituent.
For more information about additional fluorinated building blocks, please contact us by sending email to firstname.lastname@example.org.
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