Convenient one-pot formation of highly functionalized 5-bromo-2-aminothiazoles, potential endocannabinoid hydrolase MAGL inhibitors
作者:Julien R.C. Prevost、Arina Kozlova、Bouazza Es Saadi、Esra Yildiz、Sara Modaffari、Didier M. Lambert、Lionel Pochet、Johan Wouters、Eduard Dolušić、Raphaël Frédérick
DOI:10.1016/j.tetlet.2018.10.055
日期:2018.12
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
带有各种取代基的高度官能化的5-溴-2-氨基-1,3-噻唑可以通过快速有效的一锅法轻松制备,使用简单的起始原料和温和的条件,同时避免使用金属催化剂或不方便的试剂,例如作为元素卤素。这些有用的产物可以用作其他反应的起始原料或用作药理学上有意义的化合物。在我们的工作中,我们证明了所产生的5-溴噻唑化合物可能导致μM范围内的单酰基甘油脂酶(MAGL)抑制。