Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors

Prevost, Julien R.C.;Kozlova, Arina;Es Saadi, Bouazza;Yildiz, Esra;Frédérick, Raphaël;et.al.
(2018) Tetrahedron Letters — Vol. 59, n° 49, p. 4315-4319 (2018)

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Abstract
Highly functionalized 5-bromo-2-amino-1,3-thiazoles bearing various substituents could be easily prepared by a rapid and efficient one-pot method, using simple starting materials and mild conditions while avoiding the use of metal catalysts or inconvenient reagents such as elemental halogens. These useful products can serve as starting materials for other reactions or as pharmacologically interesting compounds. In our work we have shown that the resulting 5-bromothiazole compounds could lead to monoacylglycerol lipase (MAGL) inhibition in the lM range.
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Prevost, J. R. C., Kozlova, A., Es Saadi, B., Yildiz, E., Modaffari, S., Lambert, D., Pochet, L., Wouters, J., Dolušić, E., & Frédérick, R. (2018). Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors. Tetrahedron Letters, 59(49), 4315-4319. https://doi.org/10.1016/j.tetlet.2018.10.055 (Original work published 2018)