An improved method for the incorporation of fluoromethyl ketones into solid phase peptide synthesis techniques
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Dhira Joshi Jennifer Milligan Theresa Zeisner Nicola O'Reilly John Diffley George PapageorgiouAbstract
An improved and expedient technique for the synthesis of peptidyl-fluoromethyl ketones is described. The methodology is based on prior coupling of an aspartate fluoromethyl ketone to a linker and mounting it onto resin-bound methylbenzhydrylamine hydrochloride. Subsequently, by utilising standard Fmoc peptide procedures, a number of short Z-protected peptides were synthesised and assessed as possible inhibitors of the main protease from SARS-CoV-2 (3CLpro).
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Volume 11
Issue number 33
Pages 20457-20464
Available online
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Publisher website (DOI) 10.1039/d1ra03046a
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Europe PubMed Central 34178310
Pubmed 34178310
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