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
来源：
SYNTHETIC COMMUNICATIONS | 2009年 / 39卷 / 21期
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
相关论文
共 50 条
  • [1] Towards the synthesis of fluoroquinolones via a nucleophilic aromatic substitution
    Sello, Thato
    Wagener, Carl
    van Otterlo, Willem
    JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2013, 56 : S156 - S156
  • [2] Synthesis of aminopyridines via an unprecedented nucleophilic aromatic substitution of cyanopyridines
    Penney, JM
    TETRAHEDRON LETTERS, 2004, 45 (12) : 2667 - 2669
  • [3] The synthesis of (±)-aminoglutethimide via vicarious nucleophilic aromatic substitution of hydrogen
    Bushell, SM
    Crump, JP
    Lawrence, NJ
    Pineau, G
    TETRAHEDRON, 1998, 54 (10) : 2269 - 2274
  • [4] Synthesis of quinoxaline derivatives via aromatic nucleophilic substitution of hydrogen
    Zasada, Aleksandra
    Brzeskiewicz, Jakub
    Antoniak, Damian
    Bechcicka, Malgorzata
    Loska, Rafal
    Makosza, Mieczyslaw
    ORGANIC & BIOMOLECULAR CHEMISTRY, 2023, 21 (05) : 994 - 999
  • [5] Synthesis of Emissive Heteroacene Derivatives via Nucleophilic Aromatic Substitution
    Hiscock, Lana K.
    Yao, Chengzhang
    Skene, W. G.
    Dawe, Louise N.
    Maly, Kenneth E.
    JOURNAL OF ORGANIC CHEMISTRY, 2019, 84 (23): : 15530 - 15537
  • [6] Microwave-assisted synthesis of azepines via nucleophilic aromatic substitution
    Bozinovic, Nina
    Solaja, Bogdan A.
    Opsenica, Igor M.
    JOURNAL OF THE SERBIAN CHEMICAL SOCIETY, 2016, 81 (11) : 1225 - 1230
  • [7] Preparation of Indolenines via Nucleophilic Aromatic Substitution
    Huber, Florian
    Roesslein, Joel
    Gademann, Karl
    ORGANIC LETTERS, 2019, 21 (08) : 2560 - 2564
  • [8] AROMATIC FLUOROALKOXYLATION VIA DIRECT AROMATIC NUCLEOPHILIC-SUBSTITUTION
    IDOUX, JP
    GUPTON, JT
    MCCURRY, CK
    CREWS, AD
    JURSS, CD
    COLON, C
    RAMPI, RC
    JOURNAL OF ORGANIC CHEMISTRY, 1983, 48 (21): : 3771 - 3773
  • [9] Synthesis of dye functionalized xerogels via nucleophilic aromatic substitution of fluoro aromatic compounds with aminosilanes
    Seifert, Andreas
    Ladewig, Katharina
    Schoenherr, Petra
    Hofmann, Katja
    Lungwitz, Ralf
    Roth, Isabelle
    Pohlers, Andreas
    Hoyer, Walter
    Baumann, Gisela
    Schulze, Steffen
    Hietschold, Michael
    Moszner, Norbert
    Burtscher, Peter
    Spange, Stefan
    JOURNAL OF SOL-GEL SCIENCE AND TECHNOLOGY, 2010, 53 (02) : 328 - 341
  • [10] Synthesis of dye functionalized xerogels via nucleophilic aromatic substitution of fluoro aromatic compounds with aminosilanes
    Andreas Seifert
    Katharina Ladewig
    Petra Schönherr
    Katja Hofmann
    Ralf Lungwitz
    Isabelle Roth
    Andreas Pohlers
    Walter Hoyer
    Gisela Baumann
    Steffen Schulze
    Michael Hietschold
    Norbert Moszner
    Peter Burtscher
    Stefan Spange
    Journal of Sol-Gel Science and Technology, 2010, 53 : 328 - 341
12345