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Practical Asymmetric Fluorination Approach to the Scalable Synthesis of New Fluoroaminothiazine BACE Inhibitors
- Source :
- Organic Process Research & Development. 22:650-654
- Publication Year :
- 2018
- Publisher :
- American Chemical Society (ACS), 2018.
-
Abstract
- Here we report an optimized protocol for the asymmetric introduction of a fluorine atom into a quaternary center facilitated by d-proline, Selectfluor®, and trifluoroethanol. The synthesis proceeds over four steps starting from a chiral amino alcohol precursor and provides the desired enantiomer with no erosion of chiral purity and good diastereoselectivity. The process optimization allowed diastereoselective preparation of the key intermediate on a multigram scale.
Details
- ISSN :
- 1520586X and 10836160
- Volume :
- 22
- Database :
- OpenAIRE
- Journal :
- Organic Process Research & Development
- Accession number :
- edsair.doi...........605c2844dfb8d56a6a2a8fae33d2b3e2