Development an Efficient Route to the 5-Lipoxygenase Inhibitor PF-04191834

…, RA Vonder Embse, SA Kunda, W Kong

文献索引：De Koning, Pieter D.; Murtagh, Lorraine; Lawson, Jon P.; Vonder Embse, Richard A.; Kunda, Sastry A.; Kong, Wei Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1046 - 1051

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被引用次数: 5

摘要

A convergent six-step process for the synthesis of PF-04191834 (1), a potent and selective 5- lipoxygenase inhibitor, has been developed and used to deliver over 20 kg of API. The process uses the same bond-forming steps as the initial medicinal chemistry route, including the use of two consecutive Pd-catalyzed Ar–S couplings to form the key diaryl thioether linkage. The reaction conditions and downstream processing have been optimized to ...