254982-97-3

Upstream product

• 32315-10-9 bis(trichloromethyl) carbonate 
• 190839-39-5 diphenyl [(amino)(p-chlorophenyl)methyl]phosphonate 
• 106787-29-5 diphenyl [(amino)(p-chlorophenyl)methyl]phosphonate hydrobromide 
• 104-88-1 4-chlorobenzaldehyde 
• 164065-24-1 [benzyloxycarbonylamino-(4-chloro-phenyl)-methyl]-phosphonic acid diphenyl ester 
• 101-02-0 triphenyl phosphite 

Relevant academic research and scientific papers

A convenient and efficient synthesis of novel 1-ethoxycarbonylmethyl-3-ethyl-1,2,3,4-tetrahydro-4-oxo- 1,3,2-benzodiazaphosphorin-2-carboxamide 2-oxides

Some novel 1-ethoxycarbonylmethyl-3-ethyl-1,2,3,4-tetra- hydro-4-oxo-1,3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-amino acid ester or α -aminophosphonate groups have been designed incorporating the proximate carbonyl and phosphoryl groups into the benzoannulated phosphidiamide heterocycle and synthesized by a convenient one-pot procedure in good yields, in which the hydrochlorides of α-amino acid esters or hydrobromides of α -aminophosphonates reacted smoothly with bis(trichloromethyl) carbonate with the help of four molar equivalents of triethylamine to give the corresponding isocyanates that then formed the products by the addition with the phosphorus reagent containing a P-H bond.

A convenient synthesis of N-t-butyl-N′-aminocarbonyl-N-(substituted)benzoylhydrazine containing α-aminoalkylphosphonate groups in a one-pot procedure

A variety of novel N-t-butyl-N′-aminocarbonyl-N-(substituted)benzoylhydrazines containing α-aminoalkylphosphonate groups were synthesized. Treatment of α-aminoalkylphosphonates with triphosgene yielded α-isocyanatoalkylphosphonates, and subsequent addition with N-t-butyl-N-substituted benzoylhydrazines provided the title compounds in a one-pot procedure with good yields. The triphosgene-mediated reaction for the synthesis of α-isocyanatoalkylphosphonates enjoys a number of advantages: the reaction is carried out under mild condition in good yield, triphosgene is relatively safe to handle because of its low vapor pressure and high stability, and the experimental procedure is simple. This method can be applicable to the synthesis of other α-isocyanatoalkyl-phosphonates and urylenediphosphonates. The structures of all of the products and by-products were confirmed by 1H NMR, 31P NMR, IR and mass spectroscopy, and elemental analysis. We also found that some of the compounds possess potential anti-tobacco mosaic virus (TMV) activities and anticancer activities.

Synthesis and bioactivities of 1,3,2-benzodiazaphosphorin-2-carboxamide 2-oxides containing α-aminophosphonate groups

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.

New and effective synthesis of unsymmetrical α-ureidoalkylphosphonates

An efficient synthesis of substituted α-ureidoalkylphosphonates 3 was reported. The method involves the conversion of α-aminoalkylphosphonates 1 to α-isocyanatoalkylphosphonates 2 by treating with triphosgene and followed by addition of substituted amine to 2. A new kind of cyclic α-ureidoalkylphosphonates 5 was also obtained by treating 2 with ?-aminobenzoic acid, followed by intramolecular cyclization of intermediate 4.