1041191-00-7Relevant academic research and scientific papers
Late Stage C-H Activation of a Privileged Scaffold; Synthesis of a Library of Benzodiazepines
Khan, Raysa,Felix, Robert,Kemmitt, Paul D.,Coles, Simon J.,Day, Iain J.,Tizzard, Graham J.,Spencer, John
, p. 98 - 109 (2016)
A library of over twenty 5-(2-arylphenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-ones has been formed by a microwave-mediated late-stage palladium-catalysed arylation of 1,4-benzodiazepines using diaryliodonium salts. This can also be applied to nordazepam (7-chloro-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one), the active metabolite of diazepam, and subsequent N-alkylation and/or H/D exchange allows further diversification towards elaborated pharmaceuticals and their 3,3′-deuterated analogues.
C-H activations on a 1H-1,4-benzodiazepin-2(3H)-one template
Spencer, John,Chowdhry, Babur Z.,Mallet, Anthony I.,Rathnam, Rajendra P.,Adatia, Trushar,Bashall, Alan,Rominger, Frank
, p. 6082 - 6089 (2008/09/21)
Air stable benzodiazepine containing palladacycles were synthesized by a C-H activation reaction and studied by mass spectrometry and X-ray crystallography. Catalytic C-H functionalizations of 1-methyl-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one with diphenyliodonium hexafluorophosphate led to a mixture, which included the starting material and the expected product 1-methyl-5-(2′-biphenyl)-1H-1,4-benzodiazepin-2(3H)-one.
