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Design and synthesis of 3-acyl-2(3H)-benzoxazolone and 3-acyl-2(3H)-benzothiazolone derivatives |
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| Authors: | Faouzi Guenadil Hocine Aichaoui Coco N Kapanda Didier M Lambert Christopher R McCurdy and Jacques H Poupaert |
| Institution: | (1) Laboratoire de Chimie Pharmaceutique, D?partement de Chimie, Facult? des Sciences, Universit? de Badji-Mokhtar, 23000, BP 12, Annaba, Algeria;(2) Louvain Drug Research Institute, D?partement de Chimie Pharmaceutique (CMFA-Cannabinoid and Endocannabinoid Research Group), Universit? Catholique de Louvain, 1200 Brussels, Belgium;(3) Department of Medicinal Chemistry, School of Pharmacy, University of Mississippi, University, MS 38677, USA; |
| Abstract: | AbstractA simpler and efficient “green” method using solid sodium hydroxide in a solvent mixture of acetone/water was found to catalyze N-acylation of 2(3H)-benzoxazolones and 2(3H)-benzothiazolones for facile and rapid synthesis of N-acyl derivatives in excellent yields. This method was applied to the synthesis of a series of 132 compounds employing a variety of acyl chlorides. |
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