- A facile synthesis of 4(3H)-pyrimidinones via [4 + 2] cycloaddition utilizing trimethylsilylketene
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The [4+2]cycloaddition reaction utilizing trimethylsilylketene with 1,3-diaza-1,3-dienes smoothly proceeded to give the desired cycloadducts, 4(3H)-pyrimidinones, in moderate to high yields.
- Arai, Shigeru,Sakurai, Takuya,Asakura, Hitomi,Fuma, Shin-Ya,Shioiri, Takayuki,Aoyama, Toyohiko
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p. 2283 - 2287
(2007/10/03)
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- New 1,3-diazadienes used in heterocyclic synthesis
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The synthesis of dihydropyrimidines, dihydropyrimidinones and thiadiazine-1,1-dioxides starting from neutral or cationic 2-methylthio-1,3- diazadienes is described. Addition of H2S followed by loss of methanethiol led to the corresponding thiocarbonyl compounds.
- Friot, Celine,Reliquet, Alain,Reliquet, Francoise,Meslin, Jean Claude
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p. 695 - 702
(2007/10/03)
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- Synthesis and Biological Activity of 2,6-disubstituted 3-Aryl-4(3H)-pyrimidones as Potential CNS Agents
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The reaction of N-arylamidines (III) with appropriate 2-alkynoic ester gives 2,6-disubstituted 3-aryl-4(3H)-pyrimidones (IV) in one step except in the reaction of N-(2-trifluoromethylphenyl/biphenyl)-S-methylisothiourea with ethyl propiolate, where the required pyrimidones (IVa17/IVa20) along with the adduct (Va/Vb) have been isolated; these adducts on cyclisation yield the corresponding pyrimidinones (IVa17/IVa20). 2,3,6-Triphenyl-4(3H)-pyrimidone (IVh1) on treatment with P2S5 furnishes the corresponding thione (VI).Some of these compounds have shown significant central muscle relaxant, hypnotic, anticonvulsant, CNS depressant, antiinflammatory and diuretic activities.
- Gupta, K. A.,Saxena, Anil K.,Jain, Padam C.,Dua, P. R.,Prasad, C. R.,Anand, Nitya
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p. 789 - 794
(2007/10/02)
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