CC BY 4.0 · Synlett
DOI: 10.1055/s-0036-1590920
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N1-Arylation of 1,4-Benzodiazepine-2-ones with Diaryliodonium Salts

Raysa Khana, Robert Felixb, Paul D. Kemmittc, Simon J. Colesd, Graham J. Tizzardd, John Spencer*a
  • aDepartment of Chemistry, School of Life Sciences, University of Sussex, Falmer, BN19QJ, UK   Email:
  • bTocris, Bio Techne, The Watkins Building, Atlantic Road, Bristol, BS11 9QD, UK
  • cIMED Oncology, AstraZeneca, 310 Cambridge Science Park, Milton Road, Cambridge CB4 0WG, UK
  • dUK National Crystallography Service, Chemistry, University of Southampton, Highfield, Southampton, SO17 1BJ, UK
R.K. is funded by an EPSRC/AZ funded PhD studentship (EP/M507568/1) with additional support from AstraZeneca [14550001 (SME)] and Tocris Biosciences. The EPSRC is also thanked for funding the UK ­National Crystallography Service
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Publication History

Received: 13 July 2017

Accepted after revision: 06 September 2017

Publication Date:
25 September 2017 (eFirst)


A library of N1-arylated 5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-ones has been synthesized starting with unsymmetrical diaryliodonium salts using aqueous ammonia as a base. This can also be applied to a similar 1,3,4-benzotriazepin-2-one derivative.

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