Department of Natural Medicine, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai 201203, China.
School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, 333 Longteng Road, Shanghai, 201620 China.
Org Biomol Chem. 2022 Aug 24;20(33):6571-6581. doi: 10.1039/d2ob01196d.
A practical approach to α-aminophosphonates has been developed through an In(OTf)-catalyzed -α phosphonylation of ,-acetals with triethyl phosphite 7. Indoline and isoindoline ,-acetals 6a-6j and 9a-9j and chain ,-acetals 11a-11p were subjected to a Lewis acid catalyzed -α phosphonylation process. As a result, the desired α-aminophosphonates 8a-8j, 10a-10j and 12a-12p were obtained in moderate to good yields.
已经开发出一种实用的α-氨基膦酸酯方法，通过三乙基亚膦酸酯 7 与 In(OTf)催化的 -α膦酰化 -，-缩醛反应实现。吲哚啉和异吲哚啉，-缩醛 6a-6j 和 9a-9j 以及链，-缩醛 11a-11p 都经过路易斯酸催化的 -α膦酰化过程。结果，所需的α-氨基膦酸酯 8a-8j、10a-10j 和 12a-12p 以中等至良好的产率得到。
