A convenient synthesis of novel complex morpholines was achieved by a two-step process involving a Petasis three-component coupling reaction of glycolaldehyde, organoboronic acid and different amines, followed by an acid- or base-mediated intramolecular cyclization. The use of threonine derivatives with glycolaldehyde in the Petasis reaction has been studied and successfully applied in the process, achieving morpholines with a higher fraction of sp³ carbon atoms compared to blockbuster drugs.

中文翻译：

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富含sp ³的多苏氨酸衍生吗啉骨架的短合成

通过两步过程可轻松合成新型复杂的吗啉，该过程涉及乙醇醛，有机硼酸和不同胺的Petasis三组分偶联反应，然后进行酸或碱介导的分子内环化反应。已经研究了苏氨酸衍生物和乙醇醛在Petasis反应中的应用，并成功地应用于该过程中，与重磅炸弹药物相比，吗啉具有更高的sp ³碳原子分数。