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Process Development of the PDE IV Inhibitor 3-(Cyclopentyloxy)-N-(3, 5-dichloropyrid-4-yl)-4-methoxybenzamide

…, IM McFarlane, C Pemberton, AA Thatcher…

文献索引:Cook, David C.; Jones, Ronald H.; Kabir, Humayun; Lythgoe, David J.; McFarlane, Ian M.; Pemberton, Clive; Thatcher, Alan A.; Thompson, David M.; Walton, John B. Organic Process Research and Development, 1998 , vol. 2, # 3 p. 157 - 168

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被引用次数: 20

摘要

Development of an industrial process for 3-(cyclopentyloxy)-N-(3, 5-dichloropyrid-4-yl)-4- methoxybenzamide, a potent PDE IV type inhibitor, is described. The rapid identification of scalable reaction conditions allowed pilot-scale synthesis of kilogramme quantities for early clinical evaluation. However, as more compound was demanded, better reaction conditions were required in the interests of safety, economics, and environmental impact. This led to ...