An efficient chiral resolution of racemic baclofen using 2-oxazolidinones as chiral auxiliaries
An efficient large-scale preparation of enantiomerically pure ( R )- and ( S )-baclofen hydrochloride is described. The principal feature of this approach is the practical resolution of N-Boc-protected baclofen using 2-oxazolidinones as chiral auxiliaries, resulting in the formation of diastereomers, followed by crystallization separation, cleavage of Evans' oxazolidinone and deprotection of N-Boc group to yield baclofen enantiomers.
Authors
- Katsuhisa Horimoto (ORCID: https://orcid.org/0000-0002-8328-6694)
- Dongyin Chen (ORCID: https://orcid.org/0000-0002-7978-7429)
- Junjie Zhu
- Lilin Wang (ORCID: https://orcid.org/0009-0000-5411-0545)
- Qian Ren
- Lili Yang
- Mengxin Zhang
- Pingping Sun
- Feng Zhang
Institutions
- Nanjing University of Chinese Medicine (CN)
- Soochow University (CN)
- Ministry of Education (KR)
- Koto Hospital (JP)
- Shanghai Center for Brain Science and Brain-Inspired Technology (CN)
- Nanjing Medical University (CN)
Publication Details
- Journal
- Results in Chemistry
- Published
- 2026-04-27
- DOI
- https://doi.org/10.1016/j.rechem.2026.103362
- Primary Topic
- Asymmetric Synthesis and Catalysis
- Type
- article
- Field-Weighted Citation Impact
- 0.00