52421-75-7Relevant academic research and scientific papers
SUBSTITUTED TETRAHYDROQUINOLINONE COMPOUNDS AS ROR GAMMA MODULATORS
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Page/Page column 73; 74, (2016/12/07)
The present invention provides substituted tetrahydroquinolinone and related compounds of formula (I), which are therapeutically useful as modulators of Retinoic acid receptor-related orphan receptors (RORs), more particularly as RORγ modulators. These co
Process for preparing 4-hydroxypyrimidine
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, (2008/06/13)
A process for preparing a 4-hydroxypyrimidine of Formula III: STR1 wherein R1 and R2 each represent a hydrogen atom, an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 2 to 10 carbon atoms, and R4 represents hydrogen an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms, an aralkyl group having 7 to 10 carbon atoms or an aryl group having 6 to 10 carbon atoms, which comprises subjecting a 3-amino-2-unsaturated carboxylate of Formula I: STR2 wherein R1 and R2 are as defined above and R3 represents an alkyl group having 1 to 10 carbon atoms, a cycloalkyl group having 3 to 10 carbon atoms or an aralkyl group having 7 to 10 carbon atoms, and a carboxylic acid amide of Formula II: wherein R4 is as defined above, to reaction with each other in the presence of a base.
Synthesis of β-Ketocarboxamide Derivatives Using 2,2-Dimethyl-2H,4H-1,3-dioxin-4-ones
Sato, Masayuki,Ogasawara, Hiromichi,Komatsu, Sachiko,Kato, Tetsuzo
, p. 3848 - 3856 (2007/10/02)
Thermal reaction of 2,2-dimethyl-2H,4H-1,3-dioxin-4-ones (1) with amines was studied.Acylketenes 2, generated by heating of 1, reacted with anilines and benzylamine to give the corresponding β-ketocarboxamides (3,4, and 5) in good yields.The reaction of 1 with ammonia gave 3-amino-2-alkenamides (7), which were hydrolyzed to β-ketocarboxamides (6).The former products 7 were readily transformed to the 6-substituted 2-methyl-3H-pyrimidin-4-ones (9) via the 3-acetamido-2-alkenamides (8).Acylation of O-benzylhydroxylamine with 1 gave the β-ketohydroxamic acids 10.Debenzylation of 10 followed by cyclization gave rise to 5-alkyl-3-hydroxyisoxazoles (12).The reaction of 1 with amides gave the corresponding N-acetylated amides (13). Keywords --- 2H,4H-1,3-dioxin-4-one; thermal fragmentation; acylketene; acylation; carboxamide; hydroxamic acid; 3-hydroxyisoxazole; 3H-pyrimidin-4-one
Studies on Pyrimidine Derivatives. XXXII. Reaction of 4-Substituted 2,6-Dimethylpyrimidine 1-Oxides with Phosphoryl Chloride
Sakamoto, Takao,Yoshizawa, Hiroshi,Kaneda, Sohichi,Hama, Yoshiaki,Yamanaka, Hiroshi
, p. 4533 - 4538 (2007/10/02)
The reaction of 2,6-dimethyl-4-phenylpyrimidine 1-oxide with phosphoryl chloride gave 4-chloromethyl-2-methyl-6-phenylpyrimidine exclusively.In contrast, 2,6-dimethyl-4-methoxy-pyrimidine 1-oxide and 2,6-dimethyl-4-dimethylaminopyrimidine 1-oxide reacted with the same reagent to give the corresponding 2-chloromethylpyrimidines predominantly.Keywords - pyrimidine N-oxide; chloromethylpyrimidine; phosphoryl chloride; siteselective reaction; substituent effect
