59607-60-2Relevant academic research and scientific papers
Nebivolol nanoparticles: A first catalytic use in Biginelli and Biginelli-like reactions
Khaskel, Anamika,Barman, Pranjit,Maiti, Subir Kumar,Jana, Utpal
, p. 1021 - 1025 (2018/11/24)
Herein, we report the catalytic activity of nebivolol nanoparticles a novel organocatalyst for the synthesis of DHPMs and DHPM-5-carboxamides. The nanoparticles are confirmed by DSC, TEM, AFM, and IR spectroscopy. The catalyst can be readily recovered and
A General, Efficient and Green Procedure for Synthesis of Dihydropyrimidine-5-carboxamides in Low Melting Betaine Hydrochloride/Urea Mixture
Liu, Peng,Hao, Jianwu,Zhang, Zhanhui
, p. 637 - 645 (2016/07/06)
A simple, facile and convenient strategy has been developed for the synthesis of dihydropyrimidine-5-carboxamides in low melting mixture of betaine hydrochloride/urea. In this procedure, the low melting mixture of betaine hydrochloride/urea plays a triple
Synthesis of pyrimidine carboxamide derivatives catalyzed by uranyl nitrate hexa hydrate with their antibacterial and antioxidant studies
Venkatesan,Satyanarayana,Sivakumar
, p. 119 - 128 (2016/02/12)
An efficient and simple method was developed for the synthesis pyrimidine-5-carboxamides using UO2(NO3)2.6H2O catalyst under conventional and microwave irradiation. The synthesis of dihydropyrimidine using urany
Targeting dormant tuberculosis bacilli: Results for molecules with a novel pyrimidone scaffold
Joshi, Rohit R.,Barchha, Avinash,Khedkar, Vijay M.,Pissurlenkar, Raghuvir R. S.,Sarkar, Sampa,Sarkar, Dhiman,Joshi, Rohini R.,Joshi, Ramesh A.,Shah, Anamik K.,Coutinho, Evans C.
, p. 201 - 207 (2015/01/30)
Our inability to completely control TB has been due in part to the presence of dormant mycobacteria. This also renders drug regimens ineffective and is the prime cause of the appearance of drug-resistant strains. In continuation of our efforts to develop novel antitubercular agents that especially target dormant mycobacteria, a set of 55 new compounds belonging to the pyrimidone class were designed on the basis of CoMFA and CoMSIA studies, and these were synthesized and subsequently tested against both the dormant and virulent BCG strain of M. tuberculosis. Some novel compounds have been identified which selectively inhibit the dormant tuberculosis bacilli with significantly low IC50 values. This study reports the second molecule after TMC-207, having the ability to inhibit tuberculosis bacilli exclusively in its dormant phase. The synthesis was accomplished by a modified multicomponent Biginelli reaction. A classification model was generated using the binary QSAR approach - recursive partitioning (RP) to identify structural characteristics related to the activity. Physicochemical, structural, topological, connectivity indices, and E-state key descriptors were used for generation of the decision tree. The decision tree could provide insights into structure-activity relationships that will guide the design of more potent inhibitors. This paper reports the second molecule after TMC-207, with the ability to inhibit tuberculosis bacilli in its dormant phase. The paper reports molecules with a novel Pyrimidone Scaffold, the synthesis of which was accomplished with a modified multi-component Biginelli reaction. A classification model was generated using recursive partitioning (RP) technique to identify structural characteristics of the molecules with their varying activities.
Iron-catalyzed four-member multicomponent reaction for assembly of (E)-6-arylvinyl-3,4-dihydropyrimidin-2(1H)-ones
Zhang, Zhiguo,Zhang, Lianqiang,Duan, Xinyu,Yan, Xiangqian,Yan, Yan,Liu, Qingfeng,Liu, Tongxin,Zhang, Guisheng
, p. 7745 - 7751 (2015/09/07)
A novel iron-catalyzed one-pot multi-component tandem reaction of acetoacetamide, urea, and two molecules of aryl aldehydes has been developed. This reaction provides a general, straightforward, practical and useful method for the preparation of potential
2-acylthioacetamides in the biginelli reaction
Kurmach,Ryabitskiy,Britsun
, p. 1770 - 1776 (2014/05/06)
We have demonstrated for the first time a Biginelli reaction of 2-acylthioacetamides with aromatic aldehydes and ureas or thioureas, leading to N-Ar1-4-Ar2-6-R1-1-R2-2-oxo(thioxo)- 1,2,3,4-tetrahydro-pyrimidine-5-carbothioamides. The regioselectivity of this process matched the concept of hard/soft Lewis acids and bases. It was established that nitrous acid or other oxidants converted the synthesized compounds into N-Ar1-4-Ar2-6-R1-1-R 2-2-oxo(thioxo)-1,2,3,4-tetrahydropyrimidine-5-carboxamides, and not the expected 4-Ar2-6-R1-1-R2-5-(1,3- benzothiazol-2-yl)-1,2,3,4-tetrahydropyrimidin-2-ones(thiones).
Ultrasound-assisted synthesis of 6-methyl-1,2,3,4-tetrahydro-N-aryl-2-oxo/ thio-4-arylpyrimidine-5-carboxamides catalyzed by uranyl nitrate hexahydrate
Venkatesan,Satyanarayana,Sivakumar
, p. 624 - 630 (2014/06/24)
An efficient and simple method developed for the synthesis of 6-methyl-1,2,3,4-tetrahydro-N-aryl-2-oxo/thio-4-arylpyrimidine-5-carboxamide derivatives (4a-o) using UO2(NO3)2.6H 2O catalyst under conventional and
In vitro anti-inflammatory potential and QSAR analysis of oxazolo/thiazolo pyrimidine derivatives
Sawant, Ramesh L.,Bansode, Charusheela A.,Wadekar, Jyoti B.
, p. 1884 - 1892 (2013/07/26)
Twenty-six different benzylidene oxazolo/thiazolo (3,2-a)-pyrimidine-6- carboxamide derivatives were synthesized and evaluated for their anti-inflammatory potential by protein denaturation method. The structures of title compounds were characterized by IR and NMR spectral data. The SAR studies reveal that compounds containing electron withdrawing polar group at para position of 5-phenyl ring and electron withdrawing non-polar group at para position of 2-benzylidene moiety of thiazolo pyrimidine nucleus have better anti-inflammatory potential. The 2D-QSAR studies were performed on VLife MDS software which reveals that anti-inflammatory potential of benzylidene-3-oxo-5H- oxazolo/thiazolo (3,2-a)-pyrimidine-6-carboxamides is dependent on estate contribution, alignment independent, individual and path count descriptors.
Three-component synthesis of 6-aryl-4-methyl-2-oxo-1,2,3,6- tetrahydropyrimidine-5-(N-aryl)carboxamides
Gein,Zamaraeva,Kurbatova,Vakhrin
experimental part, p. 856 - 858 (2011/07/08)
A three-component synthesis using acetoacetanilides and a mixture of an aromatic aldehyde and urea yields 6-aryl-4-methyl-2-oxo-1,2,3,6- tetrahydropyrimidine-5-(N-aryl)carboxamides.
Synthesis of 3,4-Dihydropyrimidin-2(1H)-one-5-carboxamides
Soleymani, Mousa,Memarian, Hamid Reza
experimental part, p. 485 - 492 (2010/10/02)
The synthesis of various dihydropyrimidinone derivatives bearing carbamoyl moieties in 5-position under reflux conditions and microwave irradiation is described. An efficient three-component Biginelli reaction using catalytic amounts of zirconium(IV) chlo
