Development of a Large-Scale Route to an MCH1 Receptor Antagonist: Investigation of a Staudinger Ketene鈥揑mine Cycloaddition in Batch and Flow Mode
详细信息 查看全文
- 作者：Staffan Karlsson ; Rolf Bergman ; Christian L枚fberg ; Peter R. Moore ; Fritiof Pont茅n ; Joakim Tholander ; Henrik S枚rensen
- 刊名：Organic Process Research & Development
- 出版年：2015
- 出版时间：December 18, 2015
- 年：2015
- 卷：19
- 期：12
- 页码：2067-2074
- 全文大小：430K
- ISSN：1520-586X
文摘
A practical large-scale route to an MCH1 receptor antagonist is described. A Staudinger 尾-lactam synthesis of an imine and an in situ generated ketene was utilized as a key step for the preparation of a spiro-azetidine building block. The reaction was demonstrated in both batch and flow mode and a comparison of these techniques is described.