期刊
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
卷 2019, 期 41, 页码 6973-6982出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201901389
关键词
Paroxetine; Femoxetine; Total synthesis; Organocatalysis; Flow Chemistry; Immobilised Catalysts
资金
- Polish National Science Centre [DEC-2015/16/S/ST5/00440]
- Foundation for Polish Science [TEAM/2017-4/38]
Total, asymmetric synthesis of (+)-Paroxetine and (+)-Femoxetine, selective serotonin reuptake inhibitors, used for the treatment of depression, anxiety, and panic disorders is reported. The key step is organocatalytic Michael addition of aldehydes to trans-nitroalkenes realized in bath or continues flow. High efficiency and selectivity in the Michael addition was achieved by application of Wang resin-supported Hayashi-Jorgensen catalyst.
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