Transition metal free hydrolysis/cyclization strategy in a single pot: synthesis of fused furo N-heterocycles of pharmacological interest
作者:Ali Nakhi、Md. Shafiqur Rahman、Guru Pavan Kumar Seerapu、Rakesh Kumar Banote、Kummari Lalith Kumar、Pushkar Kulkarni、Devyani Haldar、Manojit Pal
DOI:10.1039/c3ob41069b
日期:——
A transition metal free tandem two-step strategy has been developed involving hydrolysis of 2-chloro-3-alkynyl quinoxalines/pyrazines followed by in situ cyclization of the corresponding 2-hydroxy-3-alkynyl intermediates in a single pot leading to fused furo N-heterocycles as potential inhibitors of sirtuins. A representative compound showed promising pharmacological properties in vitro and in vivo.
开发了一种无过渡金属的分段两步策略,该策略涉及2-氯-3-炔基喹喔啉/吡嗪的裂解,随后在单一反应容器中现场环化相应的2-羟基-3-炔基中间体,得到可能作为去乙酰化酶抑制剂的融合呋喃N-杂环化合物。其中一个代表性化合物在体外和体内均显示出有希望的药理学特性。