A short and efficient synthesis of valsartan via a Negishi reaction

被引：15

作者：

Ghosh, Samir ^{[1
]}

Kumar, A. Sanjeev ^{[1
]}

Mehta, G. N. ^{[1
]}

机构：

[1] SV Natl Inst Technol, Dept Appl Chem, Surat 395007, India

来源：

BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY | 2010年 / 6卷

关键词：

antihypertensive therapy; aryl bromide; Negishi coupling; tetrazole; valsartan; CROSS-COUPLING REACTIONS; II RECEPTOR ANTAGONISTS; POTENT; ANTIHYPERTENSIVES; DISCOVERY; BIARYLS; SERIES;

D O I：

10.3762/bjoc.6.27

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan (R)) is presented. Directed ortho-metalation of 5-phenyl-1trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previously reported syntheses.

引用

页数：4

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