Efficient Synthesis of (<i>S</i>)-3-(4-Fluorophenyl)morpholin-2-one, a Key Chiral Intermediate of Aprepitant

2015-07-20T18:00:46Z (GMT) by Song-Mei Wang
<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>