Abstract

New derivatives of the diterpene alkaloid lappaconitine containing a 1H-substituted 1,2,3-triazol-4-yl substituent in the anthranilate C-5 ′ -position were synthesized via the reaction of 5 ′ -ethynyllappaconitine with aromatic or aliphatic azides in the presence of aqueous CuSO4 and sodium ascorbate in DMF. The yields of the 1,4-disubstituted 1,2,3-triazoles were 40–73% and depended on the nature of the azide.

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