Transition metal free hydrolysis/cyclization strategy in a single pot: synthesis of fused furo N-heterocycles of pharmacological interest
Transition metal free hydrolysis/cyclization strategy in a single pot: synthesis of fused furo N-heterocycles of pharmacological interest
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DOI：
10.1039/c3ob41069b
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发表时间：
2013-08-14
影响因子：
3.2
通讯作者：
Pal, Manojit
中科院分区：
文献类型：
--
作者：
Nakhi, Ali;Rahman, Md. Shafiqur;Pal, Manojit
一种不含过渡金属的串联两步策略已经被开发出来，包括水解2-氯-3-炔基喹喔啉/吡嗪，然后在一锅中原位环化相应的2-羟基-3-炔基中间体，导致稠合呋喃并N-杂环作为潜在的sirtuins抑制剂。一种代表性化合物在体外和体内均显示出良好的药理学特性。
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.