期刊
CHEMICAL SCIENCE
卷 10, 期 48, 页码 11141-11146出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c9sc04752b
关键词
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资金
- Austrian Science Fund (FWF) [M 2413-B21]
- Austrian Science Fund (FWF) [M2413] Funding Source: Austrian Science Fund (FWF)
The catalytic enantioselective synthesis of the chiral key intermediate of the antidepressant (-)-paroxetine is demonstrated as a continuous flow process on multi-gram scale. The critical step is a solvent-free organocatalytic conjugate addition followed by a telescoped reductive amination-lactamization-amide/ester reduction sequence. Due to the efficient heterogeneous catalysts and the solvent-free or highly concentrated conditions applied, the flow method offers key advances in terms of productivity and sustainability compared to earlier batch approaches.
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