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Condensation of Carboxylic Acids with Non-Nucleophilic N-Heterocycles and Anilides Using Boc2O
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    Condensation of Carboxylic Acids with Non-Nucleophilic N-Heterocycles and Anilides Using Boc2O
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    Graduate School of Pharmaceutical Sciences, Tohoku University, Aoba 6-3, Aramaki, Aoba-ku, Sendai 980-8578, Japan
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    The Journal of Organic Chemistry

    Cite this: J. Org. Chem. 2016, 81, 22, 11444–11453
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    https://doi.org/10.1021/acs.joc.6b02097
    Published October 21, 2016
    Copyright © 2016 American Chemical Society

    Abstract

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    A novel condensation reaction of carboxylic acids with various non-nucleophilic N-heterocycles and anilides was developed. The reaction proceeds in the presence of di-tert-butyl dicarbonate (Boc2O), catalytic 4-(dimethylamino)pyridine (DMAP), and 2,6-lutidine and is applicable to the acylation of a wide range of non-nucleophilic nitrogen compounds, including indoles, pyrroles, pyrazole, carbazole, lactams, oxazolidinones, and anilides with high functional group compatibility. The scope of indoles, carboxylic acids, and anilides was also studied.

    Copyright © 2016 American Chemical Society

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    Supporting Information

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    The Supporting Information is available free of charge on the ACS Publications website at DOI: 10.1021/acs.joc.6b02097.

    • Copies of 1H and 13C NMR spectra of compounds 10a10w, 12a12n, and 14a14p; Copy of HPLC chromatogram of 10t (PDF)

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    Cited By

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    This article is cited by 16 publications.

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    The Journal of Organic Chemistry

    Cite this: J. Org. Chem. 2016, 81, 22, 11444–11453
    Click to copy citationCitation copied!
    https://doi.org/10.1021/acs.joc.6b02097
    Published October 21, 2016
    Copyright © 2016 American Chemical Society

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