Development of a New Synthesis for the Large-Scale Preparation of Triple Reuptake Inhibitor (−)-GSK1360707

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• 作者：Vassil I. Elitzin ; Kimberly A. Harvey ; Hyunjung Kim ; Matthew Salmons ; Matthew J. Sharp ; Elie A. Tabet ; Matthew A. Toczko
• 刊名：Organic Process Research & Development
• 出版年：2010
• 出版时间：July 16, 2010
• 年：2010
• 卷：14
• 期：4
• 页码：912-917
• 全文大小：228K
• 年卷期：v.14,no.4(July 16, 2010)
• ISSN：1520-586X

文摘

The triple reuptake inhibitor, GSK1360707, was synthesized via an efficient, scalable route, which features a vinyl triflate Suzuki coupling followed by a single-step, double alkylative cyclopropanation with a dihalomethane. Also, a mechanistic understanding of the Suzuki reaction (as it relates to the control of a polychlorinated biphenyl impurity) is discussed.