5496-93-5Relevant articles and documents
Synthesis method of 6-chloro-3-alkyl uracil
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Paragraph 0056-0057, (2019/12/02)
The invention relates to a synthesis method of 6-chloro-3-alkyl uracil, which is characterized by comprising the following steps: by using malonic acid and N-alkyl urea as raw materials, carrying outthe cyclization reaction to generate alkyl tripyrimidone; and then carrying out chlorination on the alkyl tripyrimidone to generate the 6-chloro-3-alkyl uracil. Compared with an existing method, the method is mild in reaction and low in cost, high-cost and high-risk raw materials such as high-toxicity and high-boiling phosphorus oxychloride are not used, and industrial large-scale production is facilitated; meanwhile, the chemical purity obtained by the method is high, the yield is good, and the economic benefit is good.
A facile synthesis of 5-acylbarbituric acids under microwave irradiations
Singh, Palwinder,Paul, Kamaldeep
, p. 1105 - 1108 (2007/10/03)
N-Monosubstituted and N,N'-disubstituted barbituric acids on treatment with benzoic anhydride/acetic anhydride under microwave irradiations without using any solvent provide a convenient methodology for the synthesis of 5-benzoyl/ acylbarbituric acids in moderate to high yields.
Synthesis of Paraxanthine Analogs (1,7-Disubstituted Xanthines) and Other Xanthines Unsubstituted at the 3-Position: Structure-Activity Relationships at Adenosine Receptors
Mueller, Christa E.,Shi, Dan,Manning, Malcolm,Daly, John W.
, p. 3341 - 3349 (2007/10/02)
Synthetic procedures for the preparation of various 3-unsubstituted xanthines, including paraxanthine analogs (1,7-disubstituted xanthines) and 1,8-disubstituted xanthines, were developed.Sylylation of 1-substituted xanthines followed by alkylation at the 7-position provides a facile route to paraxanthine analogs.Regioselective alkylation of tris(trimethylsilyl)-6-aminouracil provides 3-substituted 6-aminouracils, which are converted to 1,8-disubstituted xanthines by standard procedures.The ring closure of 3-substituted 5-cyclopentanecarboxamido- and 5-(benzoylamino)-6-aminouracils requires drastic reaction conditions.Affinity for brain A1 and A2 adenosine receptors was determined in binding assays for these and other xanthines with substituents in 1-, 3-, 7-, 8-, and 9-positions.Substitution at the 1-position was necessary for high affinity at adenosine receptors. 1,3-Disubstituted xanthines generally had higher affinity than 1,7-disubstituted xanthines. 1,8-Disubstituted xanthines had high affinity for adenosine receptors; some were highly selective for A1 receptors.