Synthesis, Crystal Structures and Cytotoxic Activity of New 1,3,4,5-tetrahydro-2H-1,5-benzodiazepine Derivatives

Abstract

The synthesis of a series of 1,3,4,5-tetrahydro-2H-1,5-benzodiazepine has been achieved by reaction of DHA (dehydroacetic acid), o-PDA (o-phenylenediamine) and aromatic aldehydes in the presence of a catalytic amount of TFA (trifluoroacetic acid). Four molecules were crystallised and their structures determined using single crystal X-ray crystallography The 15-benzodiazepines derivatives were evaluated for their in vitro cytotoxic effects.

Atom‐economical Approaches to 1,5‐Benzodiazepines Containing Indole Ring via Fe3O4@SiO2‐PTSA‐catalyzed Multi‐component Domino Reactions

“…[14] Moreover, 1,5benzodiazepine derivatives are also involved in industry for the synthesis of some photosensitive materials. [15] Consequently, the development of methods to prepare novel structures of 1,5-benzodiazepines is important for medicinal chemistry and industrial production, and represents a worthwhile goal in organic synthesis.…”