10.6084/m9.figshare.1378839.v3
Song-Mei Wang
Song-Mei
Wang
Efficient Synthesis of (<i>S</i>)-3-(4-Fluorophenyl)morpholin-2-one, a Key Chiral Intermediate of Aprepitant
Taylor & Francis Group
2015
cyclization
ethyl
Key Chiral Intermediate
hydrogenation
Efficient Synthesis
method
antiemetic drug aprepitant
access
preparation
fluorophenyl
aprepitant
2015-07-20 18:00:46
Journal contribution
https://tandf.figshare.com/articles/journal_contribution/Efficient_Synthesis_of_i_S_i_3_4_Fluorophenyl_morpholin_2_one_a_Key_Chiral_Intermediate_of_Aprepitant/1378839
<div><p></p><p>A facile, economical, and practical method for the preparation of (<i>S</i>)-3-(4-fluorophenyl)morpholin-2-one [(<i>S</i>)-<b>9</b>] has been developed from ethyl 2-(4-fluorophenyl)-2-oxoacetate (<b>7</b>) in three steps through cyclization, hydrogenation, and resolution, providing a new and convenient access to the key intermediate of antiemetic drug aprepitant.</p></div>