A Simple and Efficient Approach for the Synthesis of 1,3-Oxazolidines from β-Amino Alcohols Using Grinding Technique

摘要

An environment-friendly and efficient method for synthesis of 1,3-oxazolidines from β-amino alcohols has been developed using paraformaldehyde in the presence of 10 mol% alkali as a green reaction medium.The method is concise,simple,transition metal free,and high yielding at room temperature with wide substrate scope and functional group compatibility.The optimized method can be used for the synthesis of 1,3-oxazolidines intermediates,which are used as prodrug moieties to improve therapeutic potential of the parent drug.Structure and formation of the synthesized compounds has been characterized and confirmed through conventional spectroscopic techniques,such as ~1H nuclear magnetic resonance (NMR),~(13)C NMR,and mass spectroscopy.