Initial process development and scale-up of the synthesis of a triple reuptake inhibitor ALB 109780

…, MD McLaws, DK Keefe, BP Haney, C Zha…

Index: Yang, Qiang; Ulysse, Luckner G.; McLaws, Mark D.; Keefe, Daniel K.; Haney, Brian P.; Zha, Congxiang; Guzzo, Peter R.; Liu, Shuang Organic Process Research and Development, 2012 , vol. 16, # 3 p. 499 - 506

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Citation Number: 8

Abstract

Early process development toward a triple reuptake inhibitor is described. Three different routes were evaluated; one of them was optimized and scaled up to generate 470 g of API as this route minimized the formation of undesired side products. The selected route featured Eaton's reagent-mediated cyclization of a phenyl acetamide, copper-mediated Buchwald–Hartwig coupling to install a morpholine moiety, and palladium-catalyzed α- ...