65164-85-4Relevant academic research and scientific papers
Synthesis of phosphonodipeptide conjugates of ursolic acid and their homologs
Deng, Sheng-Lou,Baglin, Isabelle,Nour, Mohammed,Cave, Christian
, p. 55 - 65 (2008/04/05)
To prepare novel derivatives of naturally bioactive 3β-hydroxy-urs-12- en-28-oic acid (ursolic acid) with unusual properties and broad spectrum of activities, a number of chemical reactions were conducted. First, a variety of a-aminophosphonates were prepared by a series of reactions involving the three-component Mannich type reaction as a key step. Second, an array of phosphonodipeptides and their homologs was synthesized through multistep reactions including condensation of phthalic anhydride with glycine or β-alanine, chlorination of N-blocked amino acids, coupling of acid chloride with α-aminophosphonates and sequential hydrazinolysis. Finally, new classes of phosphonodipeptide conjugates of ursolic acid and their homologs were obtained by condensation of 3β-acetoxy-urs-12-en-28-oyl chloride with phosphonodipeptides and their homologs.
Synthesis and bioactivities of 1,3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-aminophosphonate groups
Huang, Junmin,Chen, Ruyu
, p. 97 - 101 (2007/10/03)
In order to search for novel antitumor and antiviral agents with high activity and low toxicity, a series of 1-ethoxycarbonylmethyl-3-ethyl-1,2,3,4-tetrahydro-4-oxo-1, 3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-aminophosphonate groups have been designed and synthesized by a convenient one-pot procedure in good yields. The structures of products were confirmed by 1H NMR, 31P NMR, IR spectra, and elemental analyses. The bioassay results showed that some of them possess excellent anti-tobacco mosaic virus activities and exhibit higher inhibitory effects compared with that of the contrast drug 2,4-dioxyhexahydro-1,3,5-triazine.
