Solid‐Acid Catalyzed Continuous‐Flow Aminolysis of Epoxides
We report a solid-acid catalyzed aminolysis of epoxides under continuous-flow conditions. A titania-zirconia supported molybdenum oxide catalyst demonstrated exceptional substrate compatibility, enabling the synthesis of β-amino alcohols in excellent yields with high catalyst durability. Characterization of the catalyst revealed the crucial role of the titania-zirconia ratio in optimizing its performance. Furthermore, this method was applied to the efficient, sequential-flow synthesis of a rivaroxaban intermediate (an oral anticoagulant and the first direct factor Xa inhibitor), combining a hydrogenation step with the aminolysis reaction without the need for intermediate isolation.
Authors
- Yuki Saito (ORCID: https://orcid.org/0000-0002-4825-7783)
- Shu̅ Kobayashi (ORCID: https://orcid.org/0000-0002-8235-4368)
- Ken Nishizawa
Institutions
- The University of Tokyo (JP)
Publication Details
- Journal
- Chemistry - A European Journal
- Published
- 2024-09-17
- DOI
- https://doi.org/10.1002/chem.202403094
- Citations
- 2
- Primary Topic
- Chemical Synthesis and Reactions
- Type
- article
- Field-Weighted Citation Impact
- 0.50
Funders
- Japan Agency for Medical Research and Development
- University of Tokyo