Efficient Synthesis of (S)-3-(4-Fluorophenyl)morpholin-2-one,a Key Chiral Intermediate of Aprepitant |
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| Authors: | Song-Mei Wang |
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| Affiliation: | 1. School of Environment, Jiangsu University, Zhenjiang, Chinablueyhz@126.com |
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| Abstract: | A facile, economical, and practical method for the preparation of (S)-3-(4-fluorophenyl)morpholin-2-one [(S)-9] has been developed from ethyl 2-(4-fluorophenyl)-2-oxoacetate (7) in three steps through cyclization, hydrogenation, and resolution, providing a new and convenient access to the key intermediate of antiemetic drug aprepitant. |
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| Keywords: | Aprepitant chiral intermediate DBTA resolution |
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