Improved Synthesis of Valsartan via Nucleophilic Aromatic Substitution on Aryloxazoline

被引:9
|
作者
Ghosh, Samir [1 ]
Kumar, A. Sanjeev [1 ]
Soundararajan, R. [1 ]
Mehta, G. N. [1 ]
机构
[1] SVNIT, Dept Appl Chem, Surat 395007, India
关键词
Antihypertensive therapy; nucleophilic aromatic substitution; oxazoline; valsartan; II RECEPTOR ANTAGONISTS; POTENT; ANTIHYPERTENSIVES; DISCOVERY; BIARYLS; SERIES;
D O I
10.1080/00397910902840819
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A highly efficient approach to the synthesis of the angiotensin II receptor antagonist valsartan (Diovan), one of the most important agents used in antihypertensive therapy today is described. The formation of the aryl-aryl bond represents the key step of its synthesis, which has been done by simple nucleophelic aromatic substitution on aryloxazoline with good yield and purity.
引用
收藏
页码:3880 / 3887
页数:8
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