134653-70-6Relevant articles and documents
Simple access toward 3-halo- and 3-nitro-pyrazolo[1,5-a] pyrimidines through a one-pot sequence
Castillo, Juan-Carlos,Rosero, Hernán-Alejandro,Portilla, Jaime
, p. 28483 - 28488 (2017)
Herein, a regioselective, time-efficient and one-pot route for the synthesis of diversely substituted 3-halo- and 3-nitropyrazolo[1,5-a]pyrimidines in good to excellent yields through a microwave-assisted process is provided. The reaction features a sequential cyclocondensation reaction of β-enaminones with NH-5-aminopyrazoles, followed by a regioselective electrophilic substitution with easily available electrophilic reagents. This methodology is distinguished by its short reaction times, high-yield, operational simplicity, broad substrate scope and pot-economy. Furthermore, these 3-functionalized heterocycles have been successfully used in the synthesis of 3-alkynyl and 3-aminopyrazolo[1,5-a]pyrimidines in yields up to 92%.
A facile, regioselective synthesis of pyrazolo[1, 5-a]pyrimidine analogs in the presence of KHSO4 in aqueous media assisted by ultrasound and their anti-inflammatory and anti-cancer activities
Kaping, Shunan,Kalita, Utpalparna,Sunn, Melboureen,Singha, Laishram Indira,Vishwakarma, Jai Narain
, p. 1257 - 1276 (2016)
Abstract: An environmentally benign, simple, efficient, and convenient route is described for the synthesis of novel pyrazolo[1,5-a]pyrimidine derivatives under ultrasound irradiation assisted by KHSO4 in aqueous medium. 3-(4-Methoxyphenyl)-3-o
Pyrimidine-based pyrazoles as cyclin-dependent kinase 2 inhibitors: Design, synthesis, and biological evaluation
Vekariya, Mayur K.,Vekariya, Rajesh H.,Brahmkshatriya, Pathik S.,Shah, Nisha K.
, p. 1683 - 1691 (2018)
A series of new pyrimidine-pyrazole hybrid molecules were designed as inhibitors of cyclin-dependent kinase 2. Designed compounds were docked using Glide and the compounds showing good score values and encouraging interactions with the residues were selected for synthesis. They were then evaluated using CDK2-CyclinA2 enzyme inhibition by a luminescent ADP detection assay. We show that of the 26 compounds synthesized and evaluated, at least 5 compounds were found to be highly potent (IC50??20?nm); which can be further optimized to have selectivity over other kinase isoforms.
A facile synthesis of 2,2-disubstituted 5-carbethoxy-2,3-dyhydro-4H-pyran-4-ones
Totah, Nancy I.,Chen, Deqi
, p. 213 - 216 (1998)
A facile synthesis of 5-carbethoxy-2,3-dihydropyran-4-ones is described via the condensation of ethyl 2-formyl-3-oxobutanoate with various ketones.
Synthesis method of 1, 3-dimethyl-1H-pyrazole-4-carboxylic acid
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Paragraph 0025; 0032; 0037, (2021/03/13)
The invention relates to a synthesis method of 1, 3-dimethyl-1H-pyrazole-4-carboxylic acid, and the method comprises the following steps: 1, carrying out condensation reaction on N, N-dimethylamino ethyl acrylate, triethylamine and acetyl chloride to generate ethyl 2-dimethylamino-3-oxobutyrate and triethylamine hydrochloride; 2, carrying out a cyclization reaction on 2-dimethylamino ethyl-3-oxobutyrate and methylhydrazine to generate 1, 3-dimethyl-1H-pyrazole ethyl-4-formate and a dimethylamine aqueous solution; 3, carrying out a reaction on formic acid, ethyl acetoacetate and dimethylamine generated in the step 2 cyclization reaction to generate 2-dimethylamino ethyl-3-oxobutyrate and water, wherein the ethyl 2-dimethylamino-3-oxobutyrate generated in the step 3 is recycled as a reactantin the step 2; 4, hydrolyzing the ethyl 1, 3-dimethyl-1H-pyrazole-4-formate to obtain the 1, 3-dimethyl-1H-pyrazole-4-carboxylic acid. The 1, 3-dimethyl-1H-pyrazole-4-carboxylic acid has the advantages of few synthesis steps, safe reaction process and no three-waste pollution, and is suitable for industrial batch large-scale preparation.
Fused tetracyclic compounds and application thereof in medicines
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Paragraph 0512; 0530-0532, (2020/04/17)
The invention relates to fused tetracyclic compounds and an application thereof in medicines, and in particular, relates to the application of the fused tetracyclic compounds as medicines for treatingand/or preventing hepatitis B. Specifically, the invention relates to the compounds represented by a general formula (I) or stereoisomers, tautomers, nitrogen oxides, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, wherein the variables are defined in the specification. The invention further relates to the application of the compounds represented by the general formula (I) or the stereoisomers, the tautomers, the nitric oxides, the solvates, the metabolites, the pharmaceutically acceptable salts or the prodrugs thereof as medicines, and in particular, relates tothe application of the compounds as the medicines for treating and/or preventing hepatitis B.
