1352344-86-5Relevant articles and documents
Enantioenriched synthesis of Escitalopram using lithiation-borylation methodology
Partridge, Benjamin M.,Thomas, Stephen P.,Aggarwal, Varinder K.
supporting information; experimental part, p. 10082 - 10088 (2012/02/05)
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.