32618-85-2Relevant academic research and scientific papers
Synthesis, spectroscopic characterization and x-ray analysis of 6-nitroquinazoline-2,4(1H,3H)-dione
Kesternich, Victor,Perez-Fehrmann, Marcia,Ortiz, Sergio,Verdugo, Felipe,Brito, Ivan,Bolte, Michael,Cardenas, Alejandro
, p. 1817 - 1819 (2013)
In this work, 6-nitroquinazoline-2,4(1H,3H)-dione was obtained in two step with good yields using a facile synthetic method. Its structure was characterized by X-ray single crystal diffraction technique (XRD), IR, 1D-NMR (1H-NMR and 13C-NMR) and 2D-NMR (H-H COSY and H-C HMBC) spectroscopy. All N and O carbonyl atoms are involved in hydrogen bonding, with an average HO distance of 1.89(2) A and N-HO angles in the range 169.5(2)-177.2(2). In the crystal packing the molecules are associated by two strong intermolecular N-HO hydrogen bonds forming centrosymmetric ring with graph-set motif R22(8), which are linked by N-HO hydrogen bonds.
Transition metals in organic synthesis, part 111: 1 first total synthesis and structural revision of antipathine A
Berndt, Andreas,Gruner, Margit,Schmidt, Arndt W.,Kn?lker, Hans-Joachim
, p. 2102 - 2106 (2013)
We describe the first total synthesis of antipathine A and a revision of the original structural assignment. Georg Thieme Verlag Stuttgart, New York.
Synthesis and Anti-Proliferation Activity Evaluation of Novel 2-Chloroquinazoline as Potential EGFR-TK Inhibitors
Zheng, Quan,Xu, Xuan-Bo,Jin, Hao,Zhang, Wen,Rao, Guo-Wu
, (2021/10/23)
A novel series of 2-chloroquinazoline derivatives had been synthesized and their anti-proliferation activities against the four EGFR high-expressing cells A549, NCI-H1975, AGS and HepG2 cell lines were evaluated. The preliminary SAR study of the scaffold of new compounds showed that the compounds with a chlorine substituent on R3 had a better anti-proliferation activity than those substituted by hydrogen atom or vinyl group. Among them, 2-chloro-N-[2-chloro-4-(3-chloro-4-fluoroanilino)quinazolin-6-yl]acetamide (10b) had the best activity, and the corresponding IC50 were 3.68, 10.06, 1.73 and 2.04 μM, respectively. And compound 10b had better or equivalent activity against four cell lines than Gefitinib. The activity of the compound 10b on the EGFR enzyme was subsequently tested. The Wound Healing of A549, AGS and HepG2 cells by this compound showed that the compound can inhibit the migration of cancer cells. Finally, the action channel of the compound 10b was supported by western blotting experiments. It provides useful information for the design of EGFR-TK inhibitors.
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
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Page/Page column 1301, (2021/07/02)
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
3-benzyl-6-amido-2, 4-(1H, 3H)-quinazolinedione derivatives and synthesis method and application thereof
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Paragraph 0014; 0018; 0020; 0021, (2019/06/12)
The present invention relates to 3-Benzyl-6-Amido-2, 4-(1H,3H)-quinazolinedione derivatives and synthesis methods and application thereof, belongs to the technical field of medicine, and relates to ageneral formula (I), wherein R1, R2 and R3 are different
CO2 transformation under mild conditions using tripolyphosphate-grafted KCC-1-NH2
Sadeghzadeh, Seyed Mohsen,Zhiani, Rahele,Moradi, Marjan
, p. 535 - 544 (2018/04/26)
Fibrous nanosilica (KCC-1) as a catalyst support was investigated in terms of stability, recycling, and reusability. For the first time, CO2 transformation was performed via the synthesis and application of KCC-1 together with sodium tripolyphosphate (STPP) and 3-aminopropyltriethoxysilane (APTES) as its functionalized derivative. To this goal, KCC-1/STPP NPs were applied to act as a nanocatalyst with excellent catalytic activities under green reaction conditions.
4-AMINO-2-PYRIDO-BICYCLIC PYRIMIDINES AND USE THEREOF AS TOPOISOMERASE II INHIBITORS
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Page/Page column 22; 52-53, (2018/07/29)
The present invention concerns 4-amino-2-pyrido-bicyclic pyrimidines as type II topoisomerase inhibitors and use thereof as medicaments especially in the treatment of cancer. The invention also provides a method for the manufacture of 4- amino-2-pyrido bicyclic pyrimidines.
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Fukase, Yoshiyuki,Sato, Ayumu,Tomata, Yoshihide,Ochida, Atsuko,Kono, Mitsunori,Yonemori, Kazuko,Koga, Keiko,Okui, Toshitake,Yamasaki, Masashi,Fujitani, Yasushi,Nakagawa, Hideyuki,Koyama, Ryoukichi,Nakayama, Masaharu,Skene, Robert,Sang, Bi-Ching,Hoffman, Isaac,Shirai, Junya,Yamamoto, Satoshi
, p. 721 - 736 (2018/02/07)
Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for the treatment of inflammatory and autoimmune diseases. A hit compound, 1, was discovered by high-throughput screeni
A 2, 4 - quinazoline dione compound preparation method
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Paragraph 0120; 0121, (2017/10/31)
The invention belongs to the field of organic chemistry, and concretely relates to a preparation method of benzoyleneurea compounds. The preparation method comprises the following steps: a 2-aminobenzonitrile compound and carbon dioxide are used as raw materials, preferably a reaction employs acylamino divalent rare earth metal amides and DBU as catalysts at 50-150 DEG C under a normal pressure, the reaction is carried out in an aprotic polar solvent for 4-40 hours, and the benzoyleneurea compounds are obtained with a high yield. The method has the advantages of mild reaction condition, few catalyst amount, simple separation and purification, high yield and wide substrate application range.
Bifunctional Ionic Liquids Derived from Biorenewable Sources as Sustainable Catalysts for Fixation of Carbon Dioxide
Saptal, Vitthal B.,Bhanage, Bhalchandra M.
, p. 1145 - 1151 (2017/03/27)
A series of highly efficient, bifunctional ionic liquids containing a quaternary alkyl ammonium cation and an amine anion were prepared from choline and amino acids, respectively. Nine ILs were synthesized, characterized, and applied as organocatalysts for the chemical fixation of carbon dioxide to form cyclic carbonates and quinazoline-2,4(1 H,3 H)-diones. A binary mixture of an IL and a co-catalysts generates deep eutectic solvents (DESs) and accelerates the rate of the cycloaddition reaction at atmospheric pressure and low temperature (70 °C). The presence of the hydroxyl functional group of choline and the free amine group of the amino acids in the ILs has a synergistic effect on the activation of the epoxide and carbon dioxide towards the cycloaddition reactions. These ILs are biodegradable and are synthesized from easily available biorenewable sources. Additionally, this catalytic method demonstrates ultimate environmental benignity because of the mild metal- and solvent-free conditions as well as the recyclability of the catalyst and co-catalyst.
