Over the recent years there has been a noticeable upsurge of interest in aza‐analogs of tryptophan which are isosteric to the latter and found numerous applications in medicinal, bioorganic chemistry, and peptide research. In the present review article, five aza‐tryptophan derivatives are profiled, including aza‐substitution in the positions 2, on the five‐membered ring, as well as in positions 4, 5, 6, and 7 on the six‐membered ring. A detailed and comprehensive literature overview of the synthetic methods for the preparation of these aza‐tryptophans is presented and general facets of the biological properties and most promising applications are discussed.

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