期刊
ORGANIC LETTERS
卷 22, 期 20, 页码 8122-8126出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c03100
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 two-step flow asymmetric synthesis of chiral gamma-nitrobutyric acids as key intermediates of the GABA analogues baclofen, phenibut, and fluorophenibut is reported on a multigram scale. The telescoped process comprises an enantioselective Michael-type addition facilitated by a polystyrene-supported heterogeneous organocatalyst under neat conditions followed by in situ-generated performic acid-mediated aldehyde oxidation. Simple access to valuable optically active substances is provided with key advances in terms of productivity and sustainability compared to those of previous batch approaches.
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