An Aminopyrrolidinyl Phosphonates—A New Class of Antibiotics: Facile Synthesis and Predicted Biological Activity

• 作者: Abed Al Aziz Al Quntar Ahmad Jabareen Hasan Dweik Tatyana A. Gloriozova Valery M. Dembitsky
• 来源期刊: 有机化学国际期刊(英文)
• 学科: 化学
• 关键词: Alkynylphosphonates CYCLIZATION PYRROLIDINE β-Aminophosphonates Amine Addition ANTIBIOTICS
• 年，卷（期）: yjhxgjqkyw_2020,（4）
• 页码范围: 170-181
• 页数: 12页
• 分类号: O62

摘要

A novel class of aminopyrrolidinyl phosphonates was synthesized in 74% - 80% isolated yield by the addition of three-fold excess of primary amines to diethyl 4-chloro-1-butynylphosphonates. The reaction was carried out at room temperature and in the absence of solvent or catalyst to give solely compounds which showed predicted biological activity based on PASS program. Some of the synthesized derivatives of antibiotics exhibit properties for the treatment of stroke, the treatment of acute neurological disorders, and can also be acetyl esterase inhibitors.