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A concise, protecting-group-free synthesis of the antipsychotic agent (+)-nemonapride has been achieved featuring a europium(III) trifluoromethanesulfonate (Eu(OTf) 3 )-catalyzed C4 selective aminolysis of a 3,4-epoxy alcohol by benzylamine and an expedient use of the resulting 4-benzylamino-1,3-diol product for constructing the pyrrolidine skeleton.

chemical and pharmaceutical bulletin/chemical and pharmaceutical bulletin

Concise, Protecting-Group-Free Synthesis of (+)-Nemonapride &lt;i&gt;via&lt;/i&gt; Eu(OTf)&lt;sub&gt;3&lt;/sub&gt;-Catalyzed Aminolysis of 3,4-Epoxy Alcohol