- PROCESS FOR THE PREPARATION OF 1-(ARYLMETHYL)QUINAZOLINE-2,4(1H,3H)-DIONES
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This disclosure provides a process for preparing 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones, specially provides a method for preparing the compound of Formula I, and the method comprises the step of reacting the compound of Formula II with the compound o
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Paragraph 0119-0120
(2019/04/29)
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- Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation
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The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various q
- Wang, Peng-Xu,Wang, Ya-Nan,Lin, Zi-Yun,Li, Gang,Huang, Hai-Hong
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supporting information
p. 1183 - 1189
(2018/04/02)
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- NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS AND ORGANIC ELECTROLUMINESCENCE DEVICES CONTAINING THEM
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The present invention relates to compounds of the general formula (11), to a material for an organic electroluminescence device comprising ot least one of these compounds, to an organic electroluminescence device comprising at least one of these compounds
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Paragraph 0449
(2017/07/14)
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- Carbon Dioxide Mediated Novel Synthesis of Quinazoline-2,4(1H,3H)-dione in Water
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A novel, efficient, and scalable CO2 mediated synthesis of quinazoline-2,4(1H,3H)-dione was developed by a simple cyclization of 2-aminobenzonitrile with DMF in water as the solvent. This is the first report of its kind. DMF was used as the necessary carbon source in the synthesis of quinazoline-2,4(1H,3H)-dione. This synthetic protocol is very efficient; it gives >99% conversion with excellent selectivity. The product was isolated by filtration because of the highly insoluble nature of quinazoline-2,4(1H,3H)-dione in water. The co-product, dimethyl amine, also has industrial importance, and the CO2 that is used can be recycled. This protocol has wide-spread applications in the syntheses of benzimidazole and benzothiazole.
- Rasal, Kalidas B.,Yadav, Ganapati D.
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p. 2067 - 2073
(2016/12/24)
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- La-Mg mixed oxide as a highly basic water resistant catalyst for utilization of CO2 in the synthesis of quinazoline-2,4(1H,3H)-dione
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The synthesis of quinazoline-2,4(1H,3H)-dione was done by direct utilization of CO2 in the cyclization of 2-aminobenzonitrile (2-ABN) using lanthanum magnesia mixed oxide (La-Mg MO) as a strong basic catalyst under mild reaction conditions in water. It gave a conversion of ~92% with 100% selectivity at 140 °C in 14 h. La-Mg MO was prepared by hydrothermal method using urea as homogeneous precipitating agent. The catalyst was characterized by different analytical techniques like BET, XRD, FT-IR, SEM, and TGA, and the basicity by CO2-TPD and acidity by NH3 TPD. Various reaction parameters were studied to predict the reaction mechanism and kinetics. The reaction follows the Langmuir-Hinshelwood-Hougen-Watson (LHHW) type kinetics model with an apparent activation energy of 23.3 kcal mol-1. The catalyst was recycled three times with an insignificant change in activity. The overall process is clean and green.
- Rasal,Yadav, Ganapati D.
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p. 111079 - 111089
(2016/12/03)
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- Discovery of 1-substituted benzyl-quinazoline-2,4(1H,3H)-dione derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors
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Poly(ADP-ribose)polymerase-1 (PARP-1) has emerged as a promising anticancer drug target due to its key role in the DNA repair process. In this work, a novel series of 1-benzyl-quinazoline-2,4(1H,3H)-dione derivatives were designed and synthesized as human PARP-1 inhibitors, structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values of single or double digit nanomolar level. Compound 7j was a potent PARP-1 and PARP-2 inhibitor and it could selectively kill the breast cancer cells MX-1 and MDA-MB-468 with mutated BRCA1/2 and PTEN, respectively, in comparison with homologous recombination proficient cell types such as breast cancer cells MDA-MB-231. In addition, compound 7j displayed the strongest potentiation effect on temozolomide in MX-1 cells (PF50 = 3.77) in this series of PARP-1 inhibitors.
- Yao, Haiping,Ji, Ming,Zhu, Zhixiang,Zhou, Jie,Cao, Ran,Chen, Xiaoguang,Xu, Bailing
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p. 681 - 693
(2015/02/19)
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- Synthesis of 5-and 7-fluoroquinazolin-4(1H)-ones
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5-Fluoroquinazoline-2,4-diones and their 2-thio analogs were obtained from 6-fluoroanthranilic acid. Two convenient routes to 5-fluoroquinazolin-4-ones involved cyclocondensation of 6-fluoroanthranilamide with acid chlorides (anhydrides) or with aromatic (heterocyclic) aldehydes. A method for the synthesis of 7-fluoroquinazolin-4-one from 2,4-difluorobenzoic acid was proposed.
- Layeva,Nosova,Lipunova,Trashakhova,Charushin
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p. 1821 - 1827
(2008/09/19)
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- Tripler stability of oligodeoxynucleotides containing substituted quinazoline-2,4-(1H,3H)-dione
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Triple helical structures can be observed between double-stranded nucleic acids and a third strand through the formation of Hoogsteen hydrogen bond. We report here the use of quinazoline-2,4-dione derivatives as substitutes for thymine in TA*T triplets. The synthesis and the characterization of monochloro derivatives of quinazoline-2,4-dione as well as 5-fluoro and 6-nitro substituted quinazoline rings are described. The ability of the various modified bases to promote the formation of triplexes was reached by thermal denaturation studies.
- Michel, Justine,Gueguen, Genevieve,Vercauteren, Joseph,Moreau, Serge
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p. 8457 - 8478
(2007/10/03)
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