Heteroaryl Ethers by Oxidative Palladium Catalysis of Pyridotriazol-1-yloxy Pyrimidines with Arylboronic Acids

被引:13
作者
Bardhan, Sujata [1 ]
Wacharasindhu, Sumrit [1 ]
Wan, Zhao-Kui [1 ]
Mansour, Tarek S. [1 ]
机构
[1] Wyeth Res, Chem Sci, Pearl River, NY 10965 USA
关键词
ARYL BORONIC ACIDS; C-O BOND; BASE-FREE; COUPLING REAGENTS; SNAR REACTIONS; AMINO-ACIDS; EFFICIENT; DERIVATIVES; HETEROCYCLES; ACTIVATION;
D O I
10.1021/ol900592b
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The oxidative palladium-catalyzed cross-coupling of pyrimidines containing pyridotriazol-1-yloxy (OPt) as either a urea or an amide functional group with arylboronic acids in the presence of CS2CO3 in DME containing 0.6-1.0% H2O is described for the preparation of heteroaryl ethers. The bromo substitution in the case of 3-(5-bromo-pyrimidin-2-yloxy)-3H-[1,2,3]triazolo[4,5-b]pyridine 1 could serve as a handle for further elaborations such as Suzuki coupling for attaching varied aryl groups.
引用
收藏
页码:2511 / 2514
页数:4
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