Development of a Practical Process for the Synthesis of PDE4 Inhibitors
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- 作者：Rogelio P. Frutos ; Thomas G. Tampone ; Jason A. Mulder ; Sonia Rodriguez ; Nathan K. Yee ; Bing-Shiou Yang ; Chris H. Senanayake
- 刊名：Organic Process Research & Development
- 出版年：2016
- 出版时间：May 20, 2016
- 年：2016
- 卷：20
- 期：5
- 页码：982-988
- 全文大小：316K
- 年卷期：0
- ISSN：1520-586X
文摘
A practical, safe, and efficient process for the synthesis of PDE4 (phosphodiesterase type 4) inhibitors represented by 1 and 2 was developed and demonstrated on a multi-kilogram scale. Key aspects of the process include the regioselective synthesis of dihydrothieno[3,2-d]pyrimidine-2,4-diol 9 and the asymmetric sulfur oxidation of intermediate 11.