Amino Acid derived enamides: synthesis and aminopeptidase activity |
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| Authors: | Cesati Richard R Dwyer Greg Jones Reinaldo C Hayes Megan P Yalamanchili Padmaja Casebier David S |
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| Institution: | Pharmaceutical Research and Development, Bristol-Myers Squibb Medical Imaging, North Billerica, Massachusetts 01862, USA. richard.cesati@bms.com |
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| Abstract: | Recently developed copper-catalyzed coupling methodology has been applied to the synthesis of amino acid derived enamides. Bond formation proved to be strongly influenced by protection strategy and vinyl iodide substitution while tolerant of limited side chain functionality. Assessment of aminopeptidase activity revealed a preference for (E)-1,2-disubstituted constructs. |
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