- Regioselective S→N allylic transposition of 3-allylthio 1,2,4-triazinone without solvent, and catalyst under microwave irradiation
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The facile and regioselective cyclization of 3-allylsulfanyl-6-methyl-2H-[1,2,4-]triazin-5-one 2 to 3,6-dimethyl-2,3-dihydro-thiazolo [3,2-.b.][1,2,4] triazin-7-one 3has been performed by the catalytic action of H2SO4. Compound 2 underwent [3,3] sigmatropic shift under microwave irradiation to afford 4N allyl derivative 5 in fairly good yield. Treatment of 5 with cone, sulphuric acid afforded the corresponding 2-methyl thiazolo[2,3-c] triazinone 7.
- Heravi,Nooshabadi,Aghapoor
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- NEW SUBSTITUTED AZATHYMIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OF BACTERIAL INFECTIOUS DISEASES
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The invention relates to substituted azathymidines and related compounds of formula (I), wherein X is N or CH, and R1, R2 and R3 are as described in the specification, processes for the preparation thereof, pharmaceutical compositions containing the same, the use thereof optionally in combination with one or more other pharmaceutically active compounds as antibacterial agents for the therapy of infective diseases, and a method for the treatment of such diseases. The compounds of formula (I) are reducing selectively the pathogenicity of bacteria within the host, but without affecting the bacteria outside the host environment.
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Page/Page column 43; 48
(2008/06/13)
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- Palladium-Catalyzed Polyhetero-Claisen Rearragement of 3-(Allylthio)-1,2,4-triazin-5(4H)-ones
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The S -> N allylic transposition of 3-(allylthio)-1,2,4-triazin-5(2H)-ones (2) has been performed successfully by catalysis of a palladium(II) salt, where regioselectivities of the rearrangement (N-2 vs.N-4) are highly dependent on the substitution patter
- Mizutani, Masato,Sanemitsu, Yuzuru,Tamaru, Yoshinao,Yoshida, Zen-ichi
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p. 4585 - 4589
(2007/10/02)
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