40230-24-8Relevant academic research and scientific papers
Synthesis and biological evaluation of novel imidazopyrimidin-3-amines as anticancer agents
Mahdavi, Mohammad,Dianat, Shima,Khavari, Behnaz,Moghimi, Setareh,Abdollahi, Mohammad,Safavi, Maliheh,Mouradzadegun, Arash,Kabudanian Ardestani, Sussan,Sabourian, Reyhaneh,Emami, Saeed,Akbarzadeh, Tahmineh,Shafiee, Abbas,Foroumadi, Alireza
, p. 797 - 805 (2017)
Groebke–Blackburn–Bienayme reaction has been utilized for the synthesis of new imidazo[1,2-a]pyrimidine derivatives as novel anticancer agents. The cytotoxic activities of compounds were evaluated against human cancer cell lines including MCF-7, T-47D, an
Pyrimidin-6-yl Trifluoroborate Salts as Versatile Templates for Heterocycle Synthesis
Cousins, David L.,Fricero, Prisca,Kopf, Kenji P. M.,McColl, Elliot J.,Czechtizky, Werngard,Lim, Yee Hwee,Harrity, Joseph P. A.
, p. 9412 - 9415 (2021)
We report a novel and general method to access a highly under-studied privileged scaffold—pyrimidines bearing a trifluoroborate at C4, and highlight the broad utility of these intermediates in a rich array of downstream functionalization reactions. This chemistry is underpinned by the unique features of the trifluoroborate group; its robustness provides an opportunity to carry out chemoselective reactions at other positions on the pyrimidine while providing a pathway for elaboration at the C?B bond when suitably activated.
Synthesis and characterization of antitubercular triazine-chalcone hybrid molecules
Rawat, Aman,Kaur, Atinder,Surjit,Kaur, Harpreet
, p. 2084 - 2090 (2017)
A new series of 1,3,5-triazine-chalcone hybrid molecules have been synthesized and evaluated in vitro for Mycobacterium tuberculosis H37Rv inhibitory potency using Alamar blue assay and the activity expressed as the minimum inhibitory concentration (MIC)
Molecular docking, modeling, semiempirical calculations studies and in vitro evaluation of new synthesized pyrimidin-imide derivatives
Abdelmonsef, Aboubakr H.,Abo-Bakr, Ahmed M.,Alsoghier, Hesham M.
, (2021/10/05)
New pyrimidin-imide derivatives 2-7 were synthesized by a condensation reaction of 4,6-diphenylpyrimidin-2-amine 1 with different anhydrides. The synthesized compounds have been investigated and put under several studies suc as, in vitro and in silico techniques, Lipinski's rule of five (RO5), semiempirical (PM6) computational calculations in addition of some physicochemical parameters measurments to evaluate their biological effect against Penicillin-Binding Protein 3 (PBP3) from Escherichia coli. These studies revealed that the newly synthesized pyrimidin-imides have minimum binding energy and good affinity especialy for ligand molecule 5 which may be considered a promising inhibitor for the PBP3 protein. The structures of all newly derivatives were unambiguously confirmed by their elemental and spectral analyses IR, 1H NMR, 13C NMR, and MS.
Metal-free cascade synthesis of unsymmetrical 2-aminopyrimidines from imidazolate enaminones
Cui, Xue,Li, Youbin,Ma, Jianting,Wang, Xuesong,Xu, Junyu,Zeng, Tingting
, p. 24247 - 24253 (2021/07/29)
A convenient metal-free synthesis of unsymmetrical 2-aminopyrimidines from imidazolate enaminones has been developed. In this procedure, various structural 2-aminopyrimidines, as well as 4,5-dihydroisoxazol-5-ols and pyrazoles were synthesized in moderate to excellent yields. A plausible mechanism was also proposed for the cascade reaction. This method represents an effective strategy towards the synthesis of unsymmetrical 2-aminopyrimidines.
A green approach for the synthesis of benzazolyl pyrimidinyl carbamothioates under ultrasonication and their antimicrobial activity
Kayathi, Narendra Babu,Panga, Siva Sankar,Adivireddy, Padmaja,Venkatapuram, Padmavathi
, p. 2931 - 2943 (2021/07/26)
A library of benzazolyl pyrimidinyl carbamothioates were prepared by the reaction of benzazolyl carbonothioates with pyrimidinyl-2-amine in the presence of an ionic liquid- 1-butyl-3-methylimidazolium hydroxide ([bmim]OH) under ultrasonication at a frequency of 35?kHz and tested for antimicrobial activity. Chloro- and nitro-substituted benzothiazolyl/benzimidazolyl pyrimidinyl carbamothioates displayed prominent antibacterial activity against Bacillus subtilis, while nitro-substituted benzothiazolyl/benzimidazolyl pyrimidinyl carbamothioates showed excellent antifungal activity against Aspergilus niger. Graphic abstract: [Figure not available: see fulltext.].
Iron-Catalyzed Alkyne-Based Multicomponent Synthesis of Pyrimidines under Air
Chakraborty, Gargi,Guin, Amit Kumar,Mondal, Rakesh,Paul, Nanda D.,Sarkar, Susmita
, p. 13186 - 13197 (2021/10/01)
An iron-catalyzed sustainable, economically affordable, and eco-friendly synthetic protocol for the construction of various trisubstituted pyrimidines is described. A wide range of trisubstituted pyrimidines were prepared using a well-defined, easy to prepare, bench-stable, and phosphine-free iron catalyst featuring a redox-noninnocent tridentate arylazo pincer under comparatively mild aerobic conditions via dehydrogenative functionalization of alcohols with alkynes and amidines.
Copper-catalyzed three-component formal [3 + 1 + 2] annulations for the synthesis of 2-aminopyrimidines fromO-acyl ketoximes
Chen, Hongbiao,Deng, Guo-Jun,Huang, Huawen,Xu, Zhenhua
supporting information, p. 8706 - 8710 (2021/10/22)
A copper-based catalytic system has been developed to enable formal [3 + 1 + 2] annulations of ketoxime acetates, aldehydes, and cyanamides. This protocol offers a new strategy for the synthesis of highly substituted 2-aminopyrimidine compounds, and more importantly, pyrimidines have now been included in the N-heterocycle family constructed usingO-acyl ketoximes as N-C-C synthons.
Direct access to 2-(N-alkylamino)pyrimidines via ruthenium catalyzed tandem multicomponent annulation/N-alkylation
Borthakur, Ishani,Guria, Saikat,Kundu, Sabuj,Maji, Milan,Singha, Suman
, p. 37 - 51 (2021/08/25)
2-(N-alkylamino)pyrimidines are important heterocycles widely found in various pharmaceutically important drugs. Here, we have disclosed a new cooperative ruthenium complex catalyzed tandem multicomponent synthesis of 2-(N-alkylamino)pyrimidines directly from guanidine salt and alcohols. The reactions proceeded through the dehydrogenation of alcohols, followed by C[sbnd]C coupling and sequential C[sbnd]N coupling with guanidine and primary alcohol, with the elimination of three equivalents of hydrogen gas. In this work, application of both the acceptorless dehydrogenative coupling (ADC) and borrowing hydrogen (BH) strategies were accomplished in a single reaction. This catalytic method tolerated a wide range of substrates. The viability of the current method was demonstrated by preparative scale synthesis of a few products. A plausible catalytic cycle was proposed based on various control experiments, mechanistic studies and DFT calculations. Remarkably, 42 new 2-(N-alkylamino)pyrimidines were synthesized following this catalytic protocol.
Design and synthesis of quinoline-pyrimidine inspired hybrids as potential plasmodial inhibitors
Kayamba, Francis,Malimabe, Teboho,Ademola, Idowu Kehinde,Pooe, Ofentse Jacob,Kushwaha, Narva Deshwar,Mahlalela, Mavela,van Zyl, Robyn L.,Gordon, Michelle,Mudau, Pertunia T.,Zininga, Tawanda,Shonhai, Addmore,Nyamori, Vincent O.,Karpoormath, Rajshekhar
, (2021/03/22)
Presently, artemisinin-based combination therapy (ACT) is the first-line therapy of Plasmodium falciparum malaria. With the emergence of malaria parasites that are resistant to ACT, alternative antimalarial therapies are urgently needed. In line with this
