The Synthesis of a 5HT2C Receptor Agonist
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- 作者：Lindsay A. Hobson ; William A. Nugent ; Stephen R. Anderson ; Subodh S. Deshmukh ; James J. Haley III ; Pingli Liu ; Nicholas A. Magnus ; Patrick Sheeran ; James P. Sherbine ; Benjamin R. P. Stone ; Jiang Zhu
- 刊名：Organic Process Research & Development
- 出版年：2007
- 出版时间：November 2007
- 年：2007
- 卷：11
- 期：6
- 页码：985 - 995
- 全文大小：200K
- 年卷期：v.11,no.6(November 2007)
- ISSN：1520-586X
文摘
This report describes the large-scale synthesis of 1 that features a Fischer indole strategy to form an advanced intermediate followed by reduction to the indoline to construct the tetracyclic core of the molecule. Resolution using dibenzoyl-D-tartaric acid affords access to a single enantiomer, from which a Suzuki coupling builds in the biaryl functionality. Deprotection followed by salt formation furnishes the desired target molecule.