01537nas a2200157   4500008004100000022001400041245017800055210006900233260000800302300001400310490000700324520086900331100002501200700002801225856012601253       2025                        eng d  a1523-706000aTf2O-Induced C(sp2)-N(sp2) bond formation: one-pot synthesis of N-heteroarene quaternary salts in nonbenzenoid skeleton of tropolone alkaloids under mild reaction conditions0 aTf2OInduced Csp2Nsp2 bond formation onepot synthesis of Nheteroa  cMAR  a2592-25960 v273 a<p>
	Naturally occurring protoalkaloids, such as colchicine and colchicoside, have significant medical applications and are used globally to treat a variety of diseases. We report herein a C(sp2)-N(sp2) bond formation protocol via a Tf2O (triflic anhydride)-assisted one-pot aromatic nucleophilic substitution (SNAr) reaction on various naturally occurring biologically active compounds such as colchicine, 3-demethyl colchicine, and 2-methoxy tropone under mild reaction conditions. Synthesis of bench-stable heterotropone quaternary salts was achieved by the reaction of tropolone alkaloids with diverse non-nucleophilic N-heterocycles. The developed methodology demonstrates wide substrate scope with good to very good yield. Our devised approach paves the way for future drug design efforts involving bioactive natural products with tropolone skeletons.</p>
1 aLohote, Mahendra, V.1 aBhattacharya, Asish, K.  uhttps://library.ncl.res.in/content/tf2o-induced-csp2-nsp2-bond-formation-one-pot-synthesis-n-heteroarene-quaternary-salts