Synthesis of an ORL-1 Receptor Antagonist via a Radical Bromination and Deoxyfluorination to Afford a gem-Difluorospirocycle
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- 作者：Amy C. DeBaillie ; Chauncey D. Jones ; Nicholas A. Magnus ; Carlos Mateos ; Alicia Torrado ; James P. Wepsiec ; Ramachandar Tokala ; Prasad Raje
- 刊名：Organic Process Research & Development
- 出版年：2015
- 出版时间：November 20, 2015
- 年：2015
- 卷：19
- 期：11
- 页码：1568-1575
- 全文大小：403K
- ISSN：1520-586X
文摘
The development of a synthesis of an ORL-1 receptor antagonist is described. The key process improvements in the synthetic sequence include a multikilogram bromination process and the development of a convergent coupling strategy. The process improvements resulted in the production of the active pharmaceutical ingredient (API) on a multikilogram scale.