Abstract

Substituted tryptamines, an important class of heterocycle in both natural products and medicinal chemistry, are readily accessible through a Larock indolization approach. The acetylene precursors are in turn routinely accessed as single enantiomers from ring opening of chiral cyclic sulfamidate precursors. Using this two-step protocol, a range of unnatural substituted tryptamines have been synthesised in good yields.

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