Large-scale Negishi coupling as applied to the synthesis of PDE472, an inhibitor of phosphodiesterase type 4D

…, M Acemoglu, W Marterer, W Pachinger

文献索引：Manley, Paul W.; Acemoglu, Murat; Marterer, Wolfgang; Pachinger, Werner Organic Process Research and Development, 2003 , vol. 7, # 3 p. 436 - 445

全文：HTML全文

被引用次数: 46

摘要

5-[2-Methoxy-5-(4-pyridinyl) phenyl]-2, 1, 3-benzoxadiazole (PDE472) is a selective inhibitor of the phosphodiesterase PDE4D isoenzyme, which is a recognised drug target for the treatment of asthma. Different synthetic routes to PDE472 were investigated, and the research synthesis was optimised to prepare a phase I batch on pilot-plant scale with the focus on the elimination or minimization of inherent process risks. An important refinement ...