Novel 2-alkyl/arylcarbamato-6-(1,1-dimethylethyl)-3-cyclohexyl-3,4-dihydro-2H-1,3,2-benzoxazaphosphorine-2-oxides (IV) have been synthesized from reactions of 2-cyclohexylaminomethyl-4-t-butylphenol I [8c] with various dichlorophosphinyl carbamates (III) [8a-b] in dry toluene in the presence of triethylamine at 40-50 °C. All the title compounds (IVa-j) at reflux temperature are degraded to 2-amino-6-(1,1-dimethylethyl)-3-cyclohexyl-3,4-dihydro-2H-1,3,2-benzoxazaphosphorine-2-oxide (IVk) exclusively. The structures are determined by ir, nmr and mass spectral studies. They were screened for antifungal activity against Penicillium notatum, Aspergillus niger and Helminthosporium sps, and antibacterial activity on Escherchia coli, Staphylococcus aureus and Pseudomonas aeruginosa. A few of them possess significant activity.
Some novel 2-(heterylcarboxamido)-2,3-dihydro-1H-1,2,5-oxadiazolo [3,4-c][1,3,2]diazaphosphole-2-oxides (4-13) have been synthesized from reaction of 3,4-diamino-1,2,5-oxadiazole (3) with various dichlorophosphinylcarboxamides (2), which were prepared by C-acylation of electron-rich heterocyclic compounds with dichloro isocyanato phosphine oxide (Kirsanov isocyanate) (1) in dry octane, in the presence of triethylamine at 50-60 °C. Their structures were determined by IR, 1 H, 13 C, 31 P NMR and mass spectral (MS) studies. They were screened for antifungal and antibacterial activity against Curvularia lunata / Aspergillus niger and Staphylococcus aureus / Escherichia coli, respectively. Most of these compounds exhibited moderate activity in the assays.
Syntheses of 2-aryloxy/2-chloro ethoxy-
2, 3-dihydro-5-benzoyl-1H-1, 3, 2-benzodiaza-phosphole 2-oxides 3a-h were accomplished by reactions of equimolar quantities of 3,4-diaminobenzophenone (1) with various aryl/chloroethoxy phosphorodichloridates 2a-g and 2h in the presence of triethylamine at 50-60• C. Compounds 3i-k were prepared by reacting 3,4-diaminobenzophenone (1) with aryl thiophosphorodichloridates 2i-k under similar conditions. They were characterized by IR,
Organo-phosphorus compoundsOrgano-phosphorus compounds S 0080
Synthesis and Antimicrobial Activity of Novel 2-Alkyl/Arylcarbamato-6-(1,1-dimethylethyl)-3-cyclohexyl-3,4-dihydro-2H-1,3,2-benzoxazaphosphorine-2-ox-ides. -Some of the compounds presented show significant antibacterial and antifungal activity. -(BABU, Y. H.; REDDY, P. V. G.; REDDY*, C. S.; REDDY, C. D.; DEVI*, P. U. M.; J.
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