A simple synthesis of substituted <i>N</i>-benzyl-3-pyrrolidinols
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An efficient synthesis of <i>N</i>-benzyl-3-hydroxypyrrolidines was achieved by the cyclodehydration of 4-amino-1,2-butanediols using thionyl chloride (SOCl<sub>2</sub>). The 4-amino-1,2-butanediols are readily accessible from aldehydes and ketones via homoallylic amines. While the cyclodehydration is non-stereoselective, the diastereomers are easily separated by column chromatography and the <i>N</i>-benzyl-3-pyrrolidinol enantiomers obtainable via <i>Aspergillus Oryzae</i> catalyzed transesterification.
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Taylor & Francis创建时间：
2025-08-22
