Abstract

A synthesis of 11-(piperazin-1yl)-5 H-dibenzo[b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. Key steps involved are Ullmann condensation, catalytic hydrogenation, and catalyzed cyclization.

Highlights

  • Dibenzodiazepine derivatives have attracted much attention from the medicinal chemistry community owing to their potential use in the treatment of psychiatric disorders

  • In past years large number of derivatives from this class have been synthesized and tested for their pharmacological actions like muscarinic agonistic and dopamine antagonistic activities1-7. 11-(Piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine is a structural analogue of clozapine, an important atypical antipsychotic

  • We report a simple and high yielding method for kilo scale synthesis of 11(piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine

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Summary

Introduction

Dibenzodiazepine derivatives have attracted much attention from the medicinal chemistry community owing to their potential use in the treatment of psychiatric disorders. Abstract: A synthesis of 11-(piperazin-1yl)-5H-dibenzo[b,e][1,4]diazepine on kilo scale without any chromatographic purification step is reported. The drugs in current clinical use from this class are few in number.

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