Water-based conditions for the microscale parallel synthesis of bicyclic lactams |
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Authors: | Sandra Malaquin Mouhamad Jida Justin Courtin Guillaume Laconde Nicolas Willand Benoit Deprez Rebecca Deprez-Poulain |
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Institution: | Biostructures and Drug Discovery, INSERM U761, Institut Pasteur de Lille, Université Lille Nord de France, Lille F-59006, France;PRIM, Lille F-59000, France |
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Abstract: | We report efficient miniaturized conditions to prepare arrays of bicyclic lactams for screening. The nature of the solvent is usually an important factor of reactivity. At a small synthesis scale, when automated pipetting devices are required, physical properties of the solvent, such as surface tension and vapor pressure also become very important. After having shown that a complete evaporation of a solution of reagents in water or a mixture of ethanol and water yields the expected lactams, we exemplified the reaction and procedure with the preparation of a library of 80 members. Our synthesis scheme is validated for synthesis scales from 1 to 100 mg. Therefore, it can be used both to produce rapidly test samples for HTS as well as to prepare intermediates for the synthesis of more elaborated nature-inspired compounds. |
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