Pd(II)-catalyzed, controllable C-H mono-/diarylation of aryl tetrazoles: concise synthesis of Losartan

被引:11
|
作者
Ding, Yan-Jun [1 ]
Li, Yan [1 ]
Dai, Sheng-Yu [1 ]
Lan, Quan [1 ]
Wang, Xi-Sheng [1 ]
机构
[1] Univ Sci & Technol China, Dept Chem, Hefei 230026, Anhui, Peoples R China
基金
中国博士后科学基金;
关键词
EFFICIENT CATALYTIC-SYSTEM; CROSS-COUPLING REACTIONS; ORTHO-ARYLATION; ANGIOTENSIN-II; DIRECTING GROUP; BOND FUNCTIONALIZATION; NATURAL-PRODUCTS; PALLADIUM; ACTIVATION; BROMIDES;
D O I
10.1039/c4ob02453b
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A palladium(II)-catalyzed C-H arylation directed by tetrazole, a metabolically stable surrogate for the carboxylic acid group in drug design, has been developed. Excellent mono-/di-selectivity was achieved through adjustment of the protecting site on the tetrazole ring. The synthetic utility of this new transformation was demonstrated in the concise total synthesis of Losartan.
引用
收藏
页码:3198 / 3201
页数:4
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