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

TETRAHEDRON LETTERS

卷:54

Article

Abed, Hassen Bel¹  Bande, Omprakash¹  Mammoliti, Oscar²  Van Lommen, Guy²  Herdewijn, Piet¹ 

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

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

关键词: Phthalazine;    Aryne;    Pyridazine;    Diaza-Wittig;   

DOI  :  10.1016/j.tetlet.2013.10.075

来源: Elsevier

【 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.

【 授权许可】

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