Efficient and Scalable Enantioselective Synthesis of a CGRP Antagonist
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- 作者：David K. Leahy ; Yu Fan ; Lopa V. Desai ; Collin Chan ; Jason Zhu ; Guanglin Luo ; Ling Chen ; Ronald L. Hanson ; Masano Sugiyama ; Thorsten Rosner ; Nicolas Cuniere ; Zhiwei Guo ; Yi Hsiao ; Qi Gao
- 刊名：Organic Letters
- 出版年：2012
- 出版时间：September 21, 2012
- 年：2012
- 卷：14
- 期：18
- 页码：4938-4941
- 全文大小：242K
- 年卷期：v.14,no.18(September 21, 2012)
- ISSN：1523-7052
文摘
An enantioselective synthesis of the CGRP antagonist BMS-846372, amenable to large scale preparation, is presented. This new synthesis showcases a chemo- and enantioselective reduction of a cyclohepta[b]pyridine-5,9-dione as well as a Pd-catalyzed alpha-arylation reaction to form the key carbon鈥揷arbon bond and set the absolute and relative stereochemistry.