Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
5266634 | Tetrahedron Letters | 2013 | 6 Pages |
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 100Â 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.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Sandra Malaquin, Mouhamad Jida, Justin Courtin, Guillaume Laconde, Nicolas Willand, Benoit Deprez, Rebecca Deprez-Poulain,