Bioorganic & medicinal chemistry letters

A concise route to triazolobenzodiazepine derivatives via a one-pot alkyne-azide cycloaddition reaction

AW Thomas

Index: Thomas, Andrew W Bioorganic and medicinal chemistry letters, 2002 , vol. 12, # 14 p. 1881 - 1884

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Citation Number: 40

Abstract

A new and efficient one-pot synthesis of [1, 2, 3] triazolo [1, 5-a][1, 4] benzodiazepin-6 (4H)- ones is described starting from readily available anthranilic acids. A small array of the title compounds were assembled via a four-step sequence involving diazotisation, azide addition followed by amide bond formation employing polymer supported carbodiimide and subsequent 1, 3-dipolar cycloaddition reaction.