Initial Process Development and Scale-Up of the Synthesis of a Triple Reuptake Inhibitor ALB 109780
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- 作者：Qiang Yang ; Luckner G. Ulysse ; Mark D. McLaws ; Daniel K. Keefe ; Brian P. Haney ; Congxiang Zha ; Peter R. Guzzo ; Shuang Liu
- 刊名：Organic Process Research & Development
- 出版年：2012
- 出版时间：March 16, 2012
- 年：2012
- 卷：16
- 期：3
- 页码：499-506
- 全文大小：356K
- 年卷期：v.16,no.3(March 16, 2012)
- ISSN：1520-586X
文摘
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鈥檚 reagent-mediated cyclization of a phenyl acetamide, copper-mediated Buchwald鈥揌artwig coupling to install a morpholine moiety, and palladium-catalyzed 伪-arylation of a dihydroisoquinolinone to construct the core structure.