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Development and Proof of Concept for a Large-Scale Photoredox Additive-Free Minisci Reaction
- Source :
- Organic Process Research & Development; January 2021, Vol. 25 Issue: 1 p57-67, 11p
- Publication Year :
- 2021
-
Abstract
- New route development activities toward ceralasertib (AZD6738) have resulted in the discovery of an efficient, acid additive-free, photoredox Minisci reaction. Mechanistic understanding resulting from LED-NMR reaction profiling, quantum yield measurements, and Stern–Volmer quenching studies have enabled optimization of the catalyst system, resulting in a significant enhancement in the rate of reaction. A large-scale continuous photoflow process has been developed, providing encouraging proof-of-concept data for the future application of this technology in the clinical manufacture of ceralasertib.
Details
- Language :
- English
- ISSN :
- 10836160 and 1520586X
- Volume :
- 25
- Issue :
- 1
- Database :
- Supplemental Index
- Journal :
- Organic Process Research & Development
- Publication Type :
- Periodical
- Accession number :
- ejs54880836
- Full Text :
- https://doi.org/10.1021/acs.oprd.0c00483