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One-pot synthesis of quinoline-based tetracycles by a tandem three-component reaction
被引:57
|作者:
Che, Chao
Xiang, Jing
Wang, Guo-Xin
Fathi, Reza
Quan, Jun-Min
Yang, Zhen
[1
]
机构:
[1] Peking Univ, Minist Educ, Key Lab Bioorgan Chem & Mol Engn, Shenzhen Grad Sch,Lab Chem Genom, Beijing 100871, Peoples R China
[2] Peking Univ, Sch Pharmaceut Sci, State Key Lab Nat & Biomimet Drugs, Coll Chem,BNLMS, Beijing 100871, Peoples R China
[3] XTL Biopharmaceut Inc, New York, NY 10989 USA
来源:
关键词:
D O I:
10.1021/cc070058a
中图分类号:
O69 [应用化学];
学科分类号:
081704 ;
摘要:
A practical one-pot synthetic strategy for the efficient synthesis of a range of structurally interesting and bioactive quinoline-based tetracycles has been developed. A key step in the synthesis is a tandem three-component reaction of heteroaromatic amine, methyl 2-formylbenzoate and (t)butyl isonitrile, followed by TFA-mediated lactamization via intramolecular aminolysis of an adjacent ester. Results related to a kinase-panel screening for several selected compounds are also discussed in this article.
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页码:982 / 989
页数:8
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