An efficient efficient preparation of 1,2-dihydropyridazines through a Diels-Alder/palladium-catalysed elimination sequence

TETRAHEDRON LETTERS

卷:60

Article

Britten, Thomas K.¹  Akien, Geoffrey R.¹  Kemmitt, Paul D.²  Halcovitch, Nathan R.¹  Coote, Susannah C.¹ 

[1] Univ Lancaster, Dept Chem, Lancaster LA1 4YB, England

[2] AstraZeneca, Oncol, IMED Biotech Unit, Cambridge CB10 1XL, England

关键词: Heterocycles;    Cycloadditions;    Dihydropyridazine;    Palladium;   

DOI  :  10.1016/j.tetlet.2019.04.054

来源: Elsevier

【 摘 要 】

A convenient, scalable synthesis of 1,2-dihydropyridazines is presented, based on the Diels-Alder cycloaddition of 1-acetoxy-1,3-butadiene with a variety of azo compounds, followed by a palladium-catalysed elimination. The products are produced on multigram scale and the new method is particularly efficient and atom-economical when compared with previous preparations of 1,2-dihydropyridazines. (C) 2019 Elsevier Ltd. All rights reserved.

【 授权许可】

Free