78438-75-2

Upstream product

• 1670-14-0 benzamidine monohydrochloride 
• 78438-91-2 5-ethoxycarbonyl-4-(2-methylaminoanilino)-2-phenylpyrimidine 
• 434933-18-3 4-(dimethylamino)-1,3-dihydro-1-methyl-2H-1,5-benzodiazepin-2-one 
• 62537-60-4 2-(Dimethylamino)-1,3-dihydro-2H-1,5-benzodiazepin-2-one 

Downstream Products

• 78438-63-8 11-chloroacetyl-6-methyl-2-phenyl-5,6-dihydropyrimido[4,5-b][1,5]benzodiazepin-5-one 

Relevant academic research and scientific papers

1,5-Benzodiazepines. Part XII. Synthesis and biological evaluation of tricyclic and tetracyclic 1,5-benzodiazepine derivatives as nevirapine analogues

A number of properly substituted 5H-pyrimido[4,5-b][1,5]benzodiazepines (2) and pyrazolo[3,4-b][1,5]benzodiazepines (3 and 4), as well as compounds 5-7, which are derivatives of new tetracyclic systems, were prepared as nevirapine analogues through multistep synthetic routes. The cytotoxic and anti-HIV-1 properties of compounds 2-7 were evaluated in cell-based assays, together with their inhibitory activity against the HIV-1 recombinant reverse transcriptase (rRT) in enzyme assays. The modifications introduced into nevirapine heterocyclic skeleton proved to have a negative effect for the anti-HIV-1 activity. It is worth noting that some of the new derivatives proved to be cytotoxic in the low micromolar range.

Pyrimidobenzodiazepinones, their use and medicaments containing them

11-Acyl-2-phenyl- and 11-acyl-5,6-dihydropyrimido[4,5-b][1,5]benzodiazepin-5-ones, their acid-addition salts and their N-oxides provide protective action for the stomach and intestines of warm-blooded animals and inhibit the formation of gastric and intestinal ulcers.