899167-26-1Relevant academic research and scientific papers
Integrated Ugi-Based Assembly of Functionally, Skeletally, and Stereochemically Diverse 1,4-Benzodiazepin-2-ones
Azuaje, Jhonny,Pérez-Rubio, José M.,Yaziji, Vicente,El Maatougui, Abdelaziz,González-Gomez, José Carlos,Sánchez-Pedregal, Vctor M.,Navarro-Vázquez, Armando,Masaguer, Christian F.,Teijeira, Marta,Sotelo, Eddy
, p. 1533 - 1549 (2015)
A practical, integrated and versatile U-4CR-based assembly of 1,4-benzodiazepin-2-ones exhibiting functionally, skeletally, and stereochemically diverse substitution patterns is described. By virtue of its convergence, atom economy, and bond-forming efficiency, the methodology documented herein exemplifies the reconciliation of structural complexity and experimental simplicity in the context of medicinal chemistry projects.
Multicomponent synthesis of diverse 1,4-benzodiazepine scaffolds
Huang, Yijun,Khoury, Kareem,Chanas, Tyler,D?mling, Alexander
supporting information, p. 5916 - 5919 (2013/02/22)
The 1,4-benzodiazepine (BDZ) scaffold is of particular interest in drug design due to a balanced ensemble of beneficial physicochemical properties including a semirigid and compact diazepine ring with spatial placements of several substituents, combined with low number of rotatable bonds, hydrogen bond donors and acceptors, and intermediate lipophilicity. As an alternative to traditional multistep sequential syntheses, we designed routes employing one-pot MCRs to accelerate access diverse BDZ scaffolds in two or three steps.
