The primary amino group has been seldom utilized as a transformable functionality in organic synthesis. Reported herein is a deaminative halogenation of primary amines using -anomeric amide as the nitrogen-deletion reagent. Both aliphatic and aromatic amines are competent substrates for direct halogenations. The mildness and robustness of the protocol are evidenced by the successful reactions of several complex- and functional group-enriched bioactive compounds or drugs. Elaboration of the resulting products provides interesting analogues of drug molecules.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9993034 | PMC |
| http://dx.doi.org/10.1016/j.isci.2023.106255 | DOI Listing |
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