Abstract
Introduction of the Ns (o-nitrobenzenesulfonyl) group into 2-F3C-aziridine enhanced the useful electrophilic character of the ring, which in turn enabled a base-free ring-opening reaction with indoles under thermal conditions. This method constitutes a practical synthetic route to a variety of CF3-containing β-tryptamine derivatives, one of which could be transformed to the CF3-containing melatonin analogue in high overall yields.
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