One pot Solvent-free synthesis of 1,5-benzodiazepine derivatives

Benzodiazepines are biologically active compounds with anti-inflammatory, antianxiety, anticonvulsant, and hypnotic activity. Due to its wide biological utility, the syntheses of these types of compounds have gained much importance in last few years. Benzadiazepines have been synthesized by the condensation of ophenylenediamines with α,β-unsaturated Diffpounds, β-haloketones or ketones. is conrs have been used for this type of condensation which majorly includes like lead nitrate, L-proline, BF3-etherate, polyphosphoric acid, NaBH4, SiO2, MgO/POCl3, acetic acid under microwave conditions and in ionic liquids. Many of these processes suffer from one or more limitations, such as long reaction times, occurrence of several side reactions, drastic reaction conditions, low yields, and tedious work-up procedure. Therefore, the search continues for a better catalyst for the synthesis of 1,5-benzadiazepines in terms of mild reaction conditions, operational simplicity, economic viability and selectivity.


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  1. Z-360 is a selective and orally available 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity. Z-360

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