A novel and convenient strategy for the synthesis of phthalazines from an aryne precursor

被引：9

作者：

Abed, Hassen Bel ^{[1
]}

Bande, Omprakash ^{[1
]}

Mammoliti, Oscar ^{[2
]}

Van Lommen, Guy ^{[2
]}

Herdewijn, Piet ^{[1
]}

机构：

[1] Katholieke Univ Leuven, Med Chem Lab, Rega Inst Med Res, B-3001 Louvain, Belgium

[2] Galapagos, Med Chem Lab, B-2800 Mechelen, Belgium

来源：

TETRAHEDRON LETTERS | 2013年 / 54卷 / 51期

关键词：

Phthalazine; Aryne; Pyridazine; Diaza-Wittig; DIELS-ALDER REACTIONS; CHEMISTRY; CYCLOADDITION; DIENOPHILES; PYRIDAZINES; AZAMERONE; BENZYNES; ESTERS;

D O I：

10.1016/j.tetlet.2013.10.075

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A novel three-step entry toward phthalazine derivatives has been elaborated. A strategy based on a sequential acyl-alkylation/diazo transfer reaction/Diaza-Wittig reaction led to the desired analogues in moderate to good yields from an aryne precursor. Various aryl groups were introduced on the annulated pyridazine, moreover the presence of an ester group allows further modifications. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：7056 / 7058

页数：3

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