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An Expedient Total Synthesis of Triciribine
Molecules ( IF 4.2 ) Pub Date : 2017-04-17 , DOI: 10.3390/molecules22040643
Chen Hu , Zhizhong Ruan , Haixin Ding , Yirong Zhou , Qiang Xiao

In the present paper, we report an expedient total synthesis of triciribine, a tricyclic 7-deazapurine nucleoside and protein kinase B (AKT ) inhibitor, in 35% overall yield. Our synthesis route features a highly regioselective substitution of 1-N-Boc-2-methylhydrazine and a trifluoroacetic acid catalyzed one-pot transformation which combined the deprotection of the tert-butylcarbonyl (Boc) group and ring closure reaction together to give a tricyclic nucleobase motif.

中文翻译:

曲西瑞滨的权宜全合成

在本论文中,我们报告了三环 7-脱氮嘌呤核苷和蛋白激酶 B (AKT) 抑制剂曲西瑞滨的权宜全合成,总产率为 35%。我们的合成路线以 1-N-Boc-2-甲基肼的高度区域选择性取代和三氟乙酸催化的一锅转化为特色,将叔丁基羰基 (Boc) 基团的脱保护和闭环反应结合在一起得到三环核碱基主题。
更新日期:2017-04-17
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