- cGAS ANTAGONIST COMPOUNDS
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Disclosed are novel compounds of Formula (I) that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.
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- Recyclization reactions of 1-alkylpyrimidinium salts
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The reaction of 4-amino-2-benzyl-1-methyl-5-ethoxycarbonylpyrimidinium iodide ( 3 ) with alcoholic methylamine resulted in the formation of the methylimine of 2-amino-4- hydroxy-6-methylamino-5-phenylpyridine-3-carbaldehyde ( 5 ). Heating of the same pyri
- Vardanyan, Ruben S.,Danagulyan, Gevork G.,Mkrtchyan, Armen D.,Hruby, Victor J.
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experimental part
p. 129 - 133
(2011/11/14)
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- Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity
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A series of pyrimidine derivatives bearing amine substituents at C-2 position were obtained from Biginelli 3,4-dihydropyrimidin-2(1H)-ones and the effect of structural variation on anti-TB activity against Mycobacterium tuberculosis H37Rv strai
- Singh, Kamaljit,Singh, Kawaljit,Wan, Baojie,Franzblau, Scott,Chibale, Kelly,Balzarini, Jan
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experimental part
p. 2290 - 2294
(2011/06/22)
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- Reaction of 2-Dimethylaminomethylene-1,3-diones with Dinucleophiles. VIII. Synthesis of Ethyl and Methyl 2,4-Disubstituted 5-Pyrimidinecarboxylates
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Reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates with N-C-N dinucleophiles such as guanidine, acetamidine or benzamidine afforded in high yields the relative esters of 4-substituted 2-amino-, 2-methyl- or 2-phenyl-5-pyrimidinecarboxylic acids, respectively.These esters were hydrolyzed to the corresponding carboxylic acids, which were converted by heating to 4-substituted 2-pyrimidinamines, 2-methyl or 2-phenylpyrimidines, respectively, generally in excellent yields.The 4-unsubstituted ethyl 2-amino-, 2-methyl- and 2-phenyl-5-pyrimidinecarboxylateswere obtained in moderate yields by reaction of the above dinucleophiles with ethyl 2,2-diformylacetate.These esters were hydrolyzed and the corresponding acids (with the exception of the 2-methyl derivative) were decarboxylated to give 2-pyrimidinamine and 2-phenylpyrimidine in satisfactory yields.
- Schenone, Pietro,Sansebastiano, Laura,Mosti, Luisa
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p. 295 - 305
(2007/10/02)
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- RECYCLIZATION OF 5-CARBETHOXY-4-METHYL-2-MERCAPTO(AMINO, HYDROXY) PYRIMIDINES TO GIVE 5-ACETYL-2-MERCAPTO(AMINO, HYDROXY)-4-HYDROXYPYRIMIDINES
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Conditions for the selective preparation of 5-carbethoxy-4-methyl-2-substituted pyrimidines or 5-acetyl-4-hydroxy-2-substituted pyrimidines by condensation of ethoxymethyleneacetoacetic ester with 1,3-binucleophiles are proposed.It is shown that under the influence of sodium ethoxide 5-carbethoxy-4-methyl-2-substituted pyrimidines undergo rearrangement to 5-acetyl-4-hydroxy-2-substituted pyrimidines.
- Vartanyan, R. S.,Kazaryan, Zh. V.,Vartanyan, S. A.
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p. 1212 - 1213
(2007/10/02)
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