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A high‐yielding procedure for the synthesis of isatins has been developed. Sequential Pd‐catalyzed double carbonylation of 2‐iodoanilines with near stoichiometric amounts of CO followed by acid‐promoted cyclization readily affords an array of isatins. The conversion of 2‐iodoanilines to isatins in good to excellent yields was found to proceed with good functional group tolerance. This protocol proved adaptable to 13C‐isotope labeling of isatins, which was extended to the synthesis of the 13C‐isotope labeled antiviral drug metisazone and the experimental anti‐schizophrenia drug ML137.
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Laursen et al. (2016) studied this question.
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