145084-44-2

Basic information

• Product Name: 1-(2-Oxo-2-o-tolyl-ethyl)-5-phenyl-1H-benzo[e][1,4]diazepine-2,3-dione 3-oxime
• Synonyms: 1-(2-Oxo-2-o-tolyl-ethyl)-5-phenyl-1H-benzo[e][1,4]diazepine-2,3-dione 3-oxime
• CAS NO: 145084-44-2
• Molecular Weight: 397.433
• Mol File: 145084-44-2.mol
• Article Data: 1

Chemical Properties

• CAS DataBase Reference: 1-(2-Oxo-2-o-tolyl-ethyl)-5-phenyl-1H-benzo[e][1,4]diazepine-2,3-dione 3-oxime(CAS DataBase Reference)
• NIST Chemistry Reference: 1-(2-Oxo-2-o-tolyl-ethyl)-5-phenyl-1H-benzo[e][1,4]diazepine-2,3-dione 3-oxime(145084-44-2)
• EPA Substance Registry System: 1-(2-Oxo-2-o-tolyl-ethyl)-5-phenyl-1H-benzo[e][1,4]diazepine-2,3-dione 3-oxime(145084-44-2)

Safety Data

• Hazardous Substances Data: 145084-44-2(Hazardous Substances Data)

Upstream product

• 2898-08-0 2,3-dihydro-5-phenyl-1H-1,4-benzodiazepin-2-one 
• 51012-65-8 2-bromo-1-o-tolylethanone 
• 145084-43-1 1,3-dihydro-1-(2'-methylphenacyl)-5-phenyl-2H-1,4-benzodiazepin-2-one 

Downstream Products

• 174276-57-4 (S)-2-amino-N-<(R)-2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl>benzenepropanamide 
• 174391-10-7 (S)-2-amino-N-<(S)-2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl>benzenepropanamide 
• 145084-28-2 (R)-1-[2,3-dihydro-1-(2'-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-3-(3-tolyl)urea 
• 145084-28-2 (S)-YM 022 
• 145084-28-2 1-<2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl>-3-(3-methylphenyl)urea 
• 145084-87-3 (R)-3-amino-1,3-dihydro-1-(2-methylphenacyl)-5-phenyl-2H-1,4-benzodiazepin-2-one 
• 145084-89-5 (S)-3-amino-1,3-dihydro-1-(2-methylphenacyl)-5-phenyl-2H-1,4-benzodiazepin-2-one 
• 145084-42-0 (RS)-3-amino-1,3-dihydro-1-(2-methylphenacyl)-5-phenyl-2H-1,4-benzodiazepin-2-one 

Relevant articles and documents

New 1,4-benzodiazepin-2-one derivatives as gastrin/cholecystokinin-B antagonists

A novel series of 1-aroylmethyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one derivatives was prepared and evaluated for activity as gastrin/cholecystokinin (CCK)-B receptor antagonists. In vitro binding studies showed that some derivatives exhibited potent affinity for gastrin/CCK-B receptor and high selectivity over peripheral CCK (CCK-A) receptor. Furthermore, these compounds potently inhibited pentagastrin- induced gastric acid secretion upon intravenous administration in an in vivo model in rats. Structure-activity relationship studies of this series suggested that 1-[(R)-2,3-dihydro-1-(2-methylphenacyl)-2-oxo-5-phenyl-1H- 1,4-benzodiazepin-3-yl]-3-(3-methylphenyl)urea (35b, YM022) was the optimal compound with IC50 values of 0.17, 0.11 and 150 nM for gastrin, CCK-B and CCK-A receptors, respectively, and an ED50 value of 9.5 nmol/kg (i.v.) in rats. The absolute configuration of the precursor of YM022, an (R)-3-amino- 1,3-dihydro-2H-1,4-benzodiazepin-2-one derivative ((R)-25), was determined by X-ray crystallographic analysis of its (S)-mandelate. It would be expected thai YM022, a potent and selective gastrin/CCK-B receptor antagonist, inhibits gastric acid secretion without inducing gastrin-mediated side- effects such as hypergastrinemia and hyperplasia of oxyntic mucosa.