One pot synthesis of dibenzodiazepinones via CuI catalysis in ethylene glycol |
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| Authors: | Qing-Yang Zhang Xiao-Jian Wang Yu-Lin Tian Jian-Guo Qi Chun Li Da-Li Yin |
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| Affiliation: | State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Peking Union Medical College and Chinese Academy of Medical Sciences, Beijing 100050, China |
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| Abstract: | A one pot protocol for the synthesis of dibenzodiazepinones was developed. The substituted ethyl 2-halobenzoates are cross-coupled with o-phenylenediamine utilizing a ligand-free, CuI catalyzed system, which spontaneously undergo an intramolecular N-acylation in ethylene glycol to give the corresponding products in high yields. This synthetic protocol provides a concise and efficient access to a wide variety of dibenzodiazepinone, including biologically active molecules. |
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| Keywords: | One pot Copper Cyclization Dibenzodiazepinone |
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