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

Julien R.C. Prevost, Arina Kozlova, Bouazza Es Saadi, Esra Yildiz, Sara Modaffari, Didier M. Lambert, Lionel Pochet, Johan Wouters, Eduard Dolušić, Raphaël Frédérick

Research output: Contribution to journalArticle

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 μM range.

Original languageEnglish
Pages (from-to)4315-4319
Number of pages5
JournalTetrahedron Letters
Volume59
Issue number49
DOIs
Publication statusPublished - 5 Dec 2018

Keywords

  • Electrophilic aromatic substitution
  • Halogenation
  • Monoacylglycerol lipase
  • Oxidation
  • Thiazoles

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