1,3,2-二氮杂磷杂环戊烯（N-杂环磷）介导的碳-磷键形成的一锅串联反应：合成α-氨基膦酸酯的途径。
1,3,2-Diazaphospholidine (N-Heterocyclic Phosphine)-Mediated Carbon-Phosphorus Bond-Forming, One-Pot Tandem Reaction: A Route to α-Amino Phosphonates.
机构信息
Department of Chemistry and Biochemistry, University of Nevada Las Vegas , 4505 S. Maryland Parkway, Las Vegas, Nevada 89154-4003, United States.
出版信息
J Org Chem. 2016 Jun 3;81(11):4550-8. doi: 10.1021/acs.joc.6b00326. Epub 2016 May 20.
A novel 1,3,2-diazaphospholidine (N-heterocyclic phosphine)-thiourea-mediated phospha-Mannich/intramolecular nucleophilic substitution reaction has been developed for the construction of an N-C-P bond unit. This transformation enabled a rapid access to cyclic tertiary α-amino phosphonates in one-pot procedure under additive-free mild reaction conditions. This study revealed the critical role of thiourea moiety of the N-heterocyclic phosphine-thiourea in the sequential intramolecular nucleophilic substitution reaction of the phosphonylation.
一种新型的 1,3,2-二氮杂膦（N-杂环磷）-硫脲介导的磷-Mannich/分子内亲核取代反应已被开发出来，用于构建 N-C-P 键单元。这种转化在无添加剂的温和反应条件下，通过一锅法快速构建了环状叔α-氨基膦酸酯。该研究揭示了 N-杂环磷-硫脲中的硫脲部分在膦酰化的顺序分子内亲核取代反应中的关键作用。
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