TFA For Pharmaceutical Applications

Peptide synthesis and solid-phase synthesis remain fundamental processes in the development of today’s most advanced pharmaceutical applications. For over 30 years, Halocarbon has been a leading supplier of BioGrade® Trifluoroacetic Acid (TFA). Halocarbon enables high-quality, GMP-grade, reliable peptide synthesis solutions at a commercially relevant scale. With innovative purification technologies, the fluorochemical experts at Halocarbon continue to support large-scale production of high-purity BioGrade® TFA for use in both laboratory-scale procedures and analysis to manufacturing-scale peptide synthesis and peptide purification. 

Peptides in Pharmaceuticals

Synthetic peptides are short amino acid chains used in several approved biotherapeutics over the last few decades chiefly for their high-specificity in binding proteins and enzymes.  These compounds are made up of multiple amino acids, linked together in a specific sequence, and have been used in pharmaceutical applications ranging from vaccines to treat a broad variety of conditions to therapeutics to alleviate seasonal allergies. As they offer lower toxicity and extremely high specificity, peptide-based drugs are gaining popularity across multiple disease domains within the pharmaceutical industry. 

Peptides are often synthesized through solid-phase synthesis, a process in which the carboxylic group of an incoming amino acid is chemically coupled to the N-terminus of a growing peptide chain.  Since most amino acids contain reactive side-chains that can interfere in this coupling process, the manufacture of a synthetic peptide relies upon the use of protecting groups to chemically block non-productive side reactions. Depending upon the step in the peptide synthesis sequence, these protecting groups are either removed via deprotection or cleavage. Halocarbon BioGrade® TFA was specifically designed for the high-purity and high-quality required in the deprotection of tert-butoxycarbonyl (Boc) and benzyl (Bzl) protecting groups, or the cleavage of 9-fluorenylmethoxycarbonyl (Fmoc) and tert-butyl (tBut) protecting groups in pharmaceutical-grade peptides. 

What is TFA?

TFA is an organofluorine compound with the chemical formula CF3CO2H. TFA is a stronger acid than acetic acid and is widely utilized in a variety of applications in organic chemistry. It is a precursor to many other fluorinated compounds, such as trifluoroacetic anhydride (TFAA), and its unique combination of properties makes it an ideal reagent in organic synthesis. TFA demonstrates excellent volatility, solubility in organic solvents, and overall strength as an acid. At a low concentration, TFA is frequently used as an ion-pairing agent in the high-performance liquid chromatography (HPLC) of organic and bioorganic compounds, such as peptides and small proteins. Halocarbon Biograde® TFA, is manufactured at very high quality and purity standards, making it well-suited for both the synthesis and purification of polypeptides, at both a laboratory and industrial scale.

TFA in Peptide Synthesis

TFA is often the choice additive for HPLC in instances where high-purity and reliability are integral. Because characterization can be challenging due to adsorption, varying hydrophobicities, and other issues, TFA’s unique characteristics of strength, volatility, and solubility are beneficial in the liquid chromatography processes and analyses. Additionally, TFA is useful in the purification stage of peptide synthesis, as well as in protection and deprotection chemistry. 

Halocarbon: Long-Standing Supplier of TFA for Pharmaceuticals

As a long-standing supplier of TFA, Halocarbon remains an industry leader in peptide synthesis solutions. Looking to learn more about TFA and peptide synthesis for pharmaceuticals? Contact a Halocarbon sales manager to learn more about our BioGrade® TFA solutions today.

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