期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 12, 期 5, 页码 884-887出版社
AMER CHEMICAL SOC
DOI: 10.1021/op8001195
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Linezolid, compound 1, is a member of the oxazolidinone class of antibacterials and has had recent clinical interest due to its potential use as a long-term treatment for bacterial infection. Detailed herein are improvements to the original synthesis to enable phase I clinical trials. Of particular interest is the preparation of a key oxindole subunit utilizing a Pd-mediated cyclization. Optimization of the synthesis of the oxindole included the use of trifluorotoluene as the solvent.
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