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

…, IM McFarlane, C Pemberton, AA Thatcher…

Index: 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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Citation Number: 20

Abstract

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 ...