- Synthesis of 1,3,5-triazinane-2-thiones and 1,3,5-oxadiazinane-4-thiones linked with isoxazoles
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Trimolecular condensation of N-(3,5-dimethyl-4-isoxazolyl)N′- arylthioureas 2 obtained from 1 by reaction with arylisothiocyanates, with aqueous formaldehyde and primary amines in toluene under reflux leads to 5-alkyl-1-(3,5-dimethyl-4-isoxazolyl)-3-aryl-hexahydro-1,3,5-triazinane-2- thiones 3 in excellent yields. Condensation of 2 with aqueous formaldehyde under similar condition provides isoxazolyl 1,3,5-oxadiazinane-4thiones 4.
- Rajanarendar,Siva Rami Reddy,Shaik, Firoz Pasha
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p. 119 - 122
(2010/04/29)
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- Imidazolo-5-YL-2anilino-pyrimidines as agents for the inhibition of the cell proliffration
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Compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, p, q, and n are as defined within and a pharmaceutically acceptable salts and in vivo hydrolysable esters are described. Also described are processes for their preparation and their use as medicaments, particularly medicaments for producing a cell cycle inhibitory (anti-cell-proliferation) effect in a warm-blooded animal, such as man.
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Page/Page column 39
(2010/02/05)
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- Medicament for viral diseases
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Isoxazoles are highly effective anti-viral agents. Combinations of isoxazoles, dihydropyrimidines and/or lamivudine and, optionally, interferon inhibit the proliferation of HBV viruses better than conventional agents.
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- Medicaments for viral diseases
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Chromanone derivatives are highly active antiviral agents. Combinations of chromanones and/or chromanols with HBV polymerase inhibitors, HBV DNA inhibitors or HBV core protein inhibitors and/or isoxazoles and, where appropriate, interferon inhibit the replication of HBV viruses better than agents disclosed previously.
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- Transformations in the isoxazole series: Synthesis of substituted 2-aminothiazoles
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Substitued N-(isoxazol-4-yl)thioureas 1 undergo a transformation in the presence of hexacarbonylmolybdenum and acid to yield functionalized thiazoles 3 in a one-pot reaction. In a few cases, 1,4,5-trisubstituted dihydroimidazoleth, iones 4 are also isolated as side products. Mechanistic considerations are outlined and scope and limitations of this new methodology discussed.
- Pascual, Alfons
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p. 531 - 542
(2007/10/02)
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