1,3‐Diazepine Derivatives: Strategies for Synthesis

Abstract

The present review describes the methodologies reported for the synthesis of 1,3‐diazepine derivatives. This heterocyclic moiety forms the core structure of many compounds with potent biological activities. Synthetic strategies by ring closure or ring transformation are discussed.

One-pot strategy to synthesize seven–membered 1,4-diazepine heterocyclic scaffolds assisted by zinc oxide nanoparticles as heterogeneous catalytic support system

“…[1][2][3][4][5][6][7][8][9][10] Diazepines are considered the biologically active epitope antigenic determinant and the useful building blocks in the construction of various pharmaceutically significant lead molecules. 11 Their derivatives are imperious types of compounds that have been widely explored for pharmacological activities such as antibacterial, antiviral, antioxidant, anticancer, antitumor [12][13] , antiparasitic 14 , antiemetic, antihistaminic, spasolytic 15 , antagonistic, anticonvulsive, anti-inflammatory and anti-fungicidal. [14][15][16] Some of them are an integral component of antimalarial drug therapy, anti-HIV, and other various pharmaceutical applications.…”

“…11 Their derivatives are imperious types of compounds that have been widely explored for pharmacological activities such as antibacterial, antiviral, antioxidant, anticancer, antitumor [12][13] , antiparasitic 14 , antiemetic, antihistaminic, spasolytic 15 , antagonistic, anticonvulsive, anti-inflammatory and anti-fungicidal. [14][15][16] Some of them are an integral component of antimalarial drug therapy, anti-HIV, and other various pharmaceutical applications. 17 Certain drugs embracing azepine nucleus are used for the treatment of Parkinson's and Alzheimer's disease since they exhibit anticonvulsant activity and may be used as tranquilizers.…”

2,2′‐Bis(arylamino)‐1,1′‐biaryls as Building Blocks for the Synthesis of Dibenzo[d,f][1,3]diazepines, Dibenzo[d,f][1,3]diazepinones, and Dibenzo[c,e][1,2,7]thiadiazepine 6‐Oxides

“…Although already described in 1929 by Le Fèvre, [11] only limited reports for the construction of 1,3‐diazepines are known. Despite considerable recent synthetic efforts in this area, [1d,3a,b,d,12–26] the synthesis of functionalized 1,3‐diazepine derivatives remains a challenging task. Therefore, better synthetic routes to the 1,3‐diazepine framework from readily available starting materials are desirable.…”