123044-27-9Relevant academic research and scientific papers
Expedient Synthesis of Biginelli-Type Dihydropyrimidinones Using α-(Benzotriazolyl)alkyl Urea Derivatives
Abdel-Fattah, Ashraf A. A.
, p. 2358 - 2362 (2003)
Reaction of readily available α-(benzotriazolyl)alkyl urea derivatives (derived from aromatic, heteroaromatic, and aliphatic aldehydes) with β-keto esters resulted in 3,4-dihydropyrimidin-2(1H)-ones in good to excellent yields.
Highly regioselective addition of organozinc reagents to 2-Oxo-1,2-dihydropyrimidine-5-carboxylates activated by BF3· OEt2: Synthesis of 2-Oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates
Singh, Kamaljit,Chopra, Rakesh
, p. 6124 - 6129 (2013)
The incorporation of alkyl as well as phenyl groups at C-4, a key position of 2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylates, responsible for antagonist/agonist switching of the calcium channel blocking activity of these compounds, has been achieved by the addition of organozinc reagents to the corresponding 2-oxo-1,2-dihydropyrimidine-5-carboxylate derivatives catalysed by BF3OEt2. An efficacious diversification of the key C-4 position of 2-oxo-1,2-dihydropyrimidine-5-carboxylates has been achieved through the addition of organozinc reagents.
A highly regio- and chemoselective addition of carbon nucleophiles to pyrimidinones. A new route to C4 elaborated Biginelli compounds
Singh, Kamaljit,Arora, Divya,Singh, Sukhdeep
, p. 1349 - 1352 (2007)
Ethyl 6-methyl-pyrimidine-2-one-5-carboxylates react with C-nucleophiles in a diversity oriented synthetic sequence to afford C4 substituted congeners of medicinally potent Biginelli dihydropyrimidinones, in a highly regioselective manner.
Halogenated macroporous sulfonic resins as efficient catalysts for the Biginelli reaction
Shen, Pengfei,Xu, Mancai,Yin, Dulin,Xie, Shaoan,Zhou, Chan,Li, Fada
, p. 18 - 21 (2016)
A series of halogenated macroporous sulfonic resins A-15-Cl, A-15-Br and A-15-I were synthesized from the precursor Amberlyst 15 by a typical halogenation reaction, and they were evaluated for the catalytic activities of the halogenated macroporous sulfon
Enantioselective N-Acylation of Biginelli Dihydropyrimidines by Oxidative NHC Catalysis
Brandolese, Arianna,Ragno, Daniele,Leonardi, Costanza,Di Carmine, Graziano,Bortolini, Olga,De Risi, Carmela,Massi, Alessandro
, p. 2439 - 2447 (2020/04/30)
The oxidative N-acylation reaction of 3,4-dihydropyrimidin-2-(1H)-ones (DHPMs) with enals and N-heterocyclic carbene (NHC) catalysts is described. The reaction proceeds in the presence of quinone oxidant without additional acyl transfer agents and in the
Quinolinium Chlorochromate: An Excellent Reagent for N3-C4 Dehydrogenation of Dihydropyrimidinones and their Antifungal Evaluation
Kaur, Jaspal,Utreja, Divya,Verma, Vibha
, p. 11 - 20 (2021/06/12)
To enhance the efficacy of 3,4-dihydropyrimidin-2-ones (DHPMs) as an antifungal agent, their dehydrogenated derivatives, i.e., pyrimidin-2-ones were synthesized employing quinolinium chlorochromate as an oxidizing agent. The synthesized compounds were scr
Synthesis and anticancer activity of new dihydropyrimidinone derivatives
Mostafa, Amany S.,Selim, Khalid B.
, p. 304 - 315 (2018/07/25)
A series of dihydropyrimidinone derivatives bearing various N-heterocyclic moieties was designed and synthesized. Twelve new compounds were screened for their cytotoxic activity using 60 cancer cell lines according to NCI (USA) protocol. Compound 19 showe
(C5H6N4O)(C5H5N4O)3(C5H4N4O)[Bi2Cl11]Cl2 as a simple and efficient catalyst in Biginelli reaction
Zhang, Xiang,Gu, Xiaoyu,Gao, Yuhua,Nie, Shipeng,Lu, Hongfei
, (2017/03/24)
A highly efficient and facile procedure for the one-pot three-component synthesis of 3,4-dihydropyrimidin-2-(1H)ones/thiones from the one-pot condensation of aldehyde, β-dicarbonyl compound and urea/thiourea was developed. The methodology is applicable to
Synthesizing method for 3,4-dihydropyrimidinone derivative
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Paragraph 0055; 0056; 0057; 0058; 0059, (2016/10/24)
The invention discloses a synthesizing method for a 3,4-dihydropyrimidinone derivative.The synthesizing method comprises the specific steps that (C5H6N4O)(C5H5N4O)3(C5H4N4O)[Bi2Cl11]Cl2 serves as a catalyst, ethyl alcohol serves as a solvent, a reaction i
Targeting the Hsp90 C-terminal domain by the chemically accessible dihydropyrimidinone scaffold
Strocchia, Maria,Terracciano, Stefania,Chini, Maria G.,Vassallo, Antonio,Vaccaro, Maria C.,Dal Piaz, Fabrizio,Leone, Antonietta,Riccio, Raffaele,Bruno, Ines,Bifulco, Giuseppe
supporting information, p. 3850 - 3853 (2015/03/30)
Hsp90 C-terminal ligands are potential new anti-cancer drugs alternative to the more studied N-terminal inhibitors. Here we report the identification of a new dihydropyrimidinone binding the C-terminus, which is not structurally related to other well-known natural and nature-inspired inhibitors of this second druggable Hsp90 site.
