Palladium-Catalyzed Direct Benzylation of Xanthines

被引:26
作者
Sahnoun, Sophian [1 ]
Messaoudi, Samir [1 ]
Brion, Jean-Daniel [1 ]
Alami, Mouad [1 ]
机构
[1] Univ Paris 11, BioCIS, Chim Therapeut Lab, Fac Pharm,UMR 8076, F-92296 Chatenay Malabry, France
关键词
C-H activation; chemoselectivity; heterocycles; inhibitors; palladium; INTERMOLECULAR DIRECT ARYLATION; C-H BONDS; HETEROAROMATIC-COMPOUNDS; BREAST-CANCER; ARYL HALIDES; DIHYDROFOLATE-REDUCTASE; PNEUMOCYSTIS-CARINII; AROMATASE INHIBITORS; COUPLING REACTION; ALKYL FORMATES;
D O I
10.1002/cctc.201000439
中图分类号
O64 [物理化学(理论化学)、化学物理学];
学科分类号
070304 ; 081704 ;
摘要
An efficient and versatile synthetic palladium-catalyzed sp(2) C-H bond activation approach for the preparation of a series of C8-benzyl xanthines has been developed using benzyl chlorides as coupling partners. The reactions take place rapidly in 1,4-dioxane and proceed in the presence of [PdCl2(MeCN)(2)]/P(o-tolyl)(3) as a catalyst system and Cs2CO3 as a base to afford good to excellent yields of the corresponding C8-benzylated xanthines of biological interest.
引用
收藏
页码:893 / 897
页数:5
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