The simple and straightforward method for the preparation of symmetrical bis(heteroaryl)methane (BHM)‐containing amino acids by the reaction of cyclic enecarbamate with heteroaromatics has been developed. The reaction goes in regioselective manner and we get only 3, 3′‐bis(heteroaryl)methane (BHM)‐containing amino acids. In addition to this synthesis, of unsymmetrical bisindolylmethane (BIM)‐containing amino acids is also reported. These symmetrical and unsymmetrical BIM‐containing amino acids are reported first time and are considered as bishomotryptophan derivatives, a biologically important homolog of tryptophan. These important monomers may serve as important tools for peptide design and engineering.
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