Fig. 5: Application of the pyridine-to-benzonitrile replacement strategy to the synthesis of drug analogues. | Nature Synthesis

Fig. 5: Application of the pyridine-to-benzonitrile replacement strategy to the synthesis of drug analogues.

From: A three-step strategy for the conversion of pyridines into benzonitriles

Fig. 5

a, Use of the methodology for the late-stage pyridine-to-benzonitrile ring replacement of drugs. b, Use of the method for the preparation of ‘unhappy water’ analogues of pyridine drugs. B(pin), pinacol boronic ester; HATU, hexafluorophosphate azabenzotriazole tetramethyl uronium; T3P, propylphosphonic anhydride; TMSN3, trimethylsilyl azide; TFA, trifluoroacetic acid. See Supplementary Information, section 11.5, for details of reaction conditions.

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