ZrCl₄ as a new catalyst for ester amidation: an efficient synthesis of h-P2X7R antagonists

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• 作者：Germain Homerin^a ; ^b ; Davy Baudelet^a ; ^b ; Pierrick Dufré ; noy^a ; ^b ; Benoî ; t Rigo^a ; ^b ; Emmanuelle Lipka^a ; ^d ; Xavier Dezitter^a ; ^c ; Christophe Furman^a ; ^c ; Ré ; gis Millet^a ; ^c ; Alina Ghinet^a ; ^b ; ^e ; ^{alina.ghinet@hei.fr" class="auth_mail" title="E-mail the corresponding author}
• 关键词：ZrCl4 ; Aminolysis ; Pyroglutamide ; P2X7R ; IBD ; Inflammation
• 刊名：Tetrahedron Letters
• 出版年：2016
• 出版时间：9 March 2016
• 年：2016
• 卷：57
• 期：10
• 页码：1165-1170
• 全文大小：1179 K

文摘

The catalytic activity of zirconium (IV) chloride (ZrCl₄) versus conventional catalysts (PTSA or HCl) for the amidation of methyl-pyroglutamate derivatives was investigated. In this study of the synthesis of P2X7 receptor (P2X7R) antagonists, ZrCl₄ was the best catalyst for the synthesis of pyroglutamides substituted in position 1. Four new pyroglutamides have shown good antagonistic properties on the human P2X7 receptor (h-P2X7R).