A new method for the synthesis of 2-aminomethyl functionalized 1,4-benzodiazepin-5-ones is presented. The benzodiazepine core is well-known to interact with biological receptors and many pharmaceutical drugs are derived from this structure. The alkene diamination strategy is employed for the first time for the synthesis of 1,4-benzodiazepinones. In this reaction, copper(2-ethylhexanoate) serves as promoter and a range of external amines can be coupled with 2-sulfonamido--allyl benzamides to generate the 1,4-benzodiazepinones in good yields.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4448762 | PMC |
| http://dx.doi.org/10.1016/j.tetlet.2015.01.171 | DOI Listing |
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