期刊
TETRAHEDRON
卷 67, 期 52, 页码 10082-10088出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tet.2011.09.142
关键词
Lithiation-borylation; Escitalopram; Total synthesis; Carbamate; Boronic ester
资金
- EPSRC
- Royal society
- Engineering and Physical Sciences Research Council [EP/D501725/1, EP/E052185/1] Funding Source: researchfish
- EPSRC [EP/E052185/1] Funding Source: UKRI
The asymmetric synthesis of Escitalopram has been completed using a lithiation-borylation reaction as the key step. Suitably functionalized enantioenriched carbamate (er 98:2) and boronic ester coupling partners were prepared and following deprotonation with s-BuLi and borylation, the tertiary alcohol was obtained in 42% yield and 93:7 er. The lithiation-borylation reaction was found to tolerate nitrile, benzylic alcohol and N-Boc functionalities. The tertiary alcohol was converted to Escitalopram in three further steps. (C) 2011 Elsevier Ltd. All rights reserved.
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