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

作　　者：Abed Al Aziz Al Quntar Hasan Dweik Ahmad Jabareen Tatyana A. Gloriozova Valery M. Dembitsky Abed Al Aziz Al Quntar;Hasan Dweik;Ahmad Jabareen;Tatyana A. Gloriozova;Valery M. Dembitsky(Department of Material Engineering, Faculty of Engineering, Al-Quds University, Jerusalem, Palestine;Faculty of Chemistry and Chemical Technology, Al-Quds University, Jerusalem, Palestine;Institute of Biomedical Chemistry, Moscow, Russia;Centre for Applied Research and Innovation, and Entrepreneurship, Lethbridge College, Lethbridge, Canada)

机构地区：[1]Department of Material Engineering, Faculty of Engineering, Al-Quds University, Jerusalem, Palestine [2]Faculty of Chemistry and Chemical Technology, Al-Quds University, Jerusalem, Palestine [3]Institute of Biomedical Chemistry, Moscow, Russia [4]Centre for Applied Research and Innovation, and Entrepreneurship, Lethbridge College, Lethbridge, Canada

出　　处：《International Journal of Organic Chemistry》2020年第4期170-181,共12页有机化学国际期刊（英文）

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.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.

关 键 词：Alkynylphosphonates CYCLIZATION PYRROLIDINE β-Aminophosphonates Amine Addition ANTIBIOTICS 

分 类 号：O62[理学—有机化学]