779309-80-7Relevant academic research and scientific papers
Discovery of Irbesartan Derivatives as BLT2 Agonists by Virtual Screening
Hernandez-Olmos, Victor,Heering, Jan,Bischoff-Kont, Iris,Kaps, Alexander,Rajkumar, Rinusha,Liu, Ting,Fürst, Robert,Steinhilber, Dieter,Proschak, Ewgenij
supporting information, p. 1261 - 1266 (2021/07/28)
Leuktriene B4 receptor 2 (BLT2) is a G-protein coupled receptor modulation of which is discussed to be a therapeutic option for healing of intestinal lesions. In this work, new BLT2 agonists were identified by a virtual screening of a repurposing library and in vitro assay of the most promising compounds. Irbesartan, an approved type-1 angiotensin II receptor (AT1) antagonist, was identified as a moderate BLT2 agonist. An initial SAR study on the irbesartan scaffold was performed resulting in the discovery of a new potent BLT2 agonist (8f, EC50 = 67.6 nM). Irbesartan and 8f were shown to promote proliferation of epithelial colon cells, an effect which was reversible by a BLT2 antagonist.
OMS-2 nanorod-supported cobalt catalyst for aerobic dehydrocyclization of vicinal diols and amidines: Access to functionalized imidazolones
Xie, Feng,Chen, Xiuwen,Zhang, Xiangyu,Luo, Chujun,Lin, Shizhuo,Chen, Xiaoyong,Li, Bin,Li, Yibiao,Zhang, Min
, p. 192 - 197 (2021/05/17)
The development of reusable base metal catalysts for innovative catalytic transformations is a key technology toward sustainable production of fine chemicals, pharmaceuticals, and other function products. Herein, we report the preparation of a new highly dipersed manganese oxides of octahedral molecular sieve (OMS-2) nanorod-supported cobalt catalyst, which is successfully applied for aerobic dehydrocyclization of vicinal diols and amidines to access structurally diverse imidazolones, a class of valuable compounds found in numerous natural and biomedical products. The developed catalytic transformation proceeds with broad substrate scope, good functional group compability, the use of green molecular oxygen and reusable cobalt catalyst, which offers an important platform for the conversion of abundant and sustainable alcohol resources into functional N-heterocycles. The strategy combining nanocatalyst design with aerobic dehydrocoupling is anticipated to achieve other challenging catalytic transformations.
Synthetic method of imidazolinone derivative
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Paragraph 0069-0076, (2021/07/10)
The invention discloses a synthesis method of an imidazolinone derivative. According to the method, amidine compounds and polyhydric alcohol compounds are taken as raw materials, high-value conversion of polyhydric alcohol is catalyzed by a cobalt catalyst to form a series of imidazolinone derivatives, a novel and green synthesis path meeting the sustainable chemical principle is developed, high-value conversion of renewable resources is achieved, and the method is suitable for industrial production. Therefore, the synthesis requirements on the imidazolinone derivative are met. The synthesis method has the advantages of wide substrate applicability, good functional group compatibility and use of a reusable cheap metal catalyst and air as an oxidant, has potential to prepare the imidazolinone derivative in one step on a large scale, and also provides an important way for converting biomass resources into high-value functional molecules.
4. 4 - Disubstituted - 4, 5 - dihydro - 1H - imidazole -5 - ketone, derivative and its synthesis method
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Paragraph 0086; 0106-0108, (2018/10/19)
The invention relates to a 4, 4-disubstituted-4, 5-dihydro-1H-imidazole-5-one and derivatives thereof as well as a synthesis method thereof. The synthesis method adopts the technical scheme that amidine compounds and ketones are converted into imidazolone and derivatives thereof in the absence of catalysts just under the action of alkali by using air or oxygen as an oxidant and pyridine, quinoline, triethylamine, NMP, DMA, DMSO, 1, 4-dioxane, toluene and the like as an organic solvent. The synthesis method overcomes the difficulties of the existing method for synthesizing imidazolone compounds of complicated synthesis steps, multi-step synthesis processes as well as the use of metal catalysts, metal oxidants or peroxides of chemical equivalent; and 4, 4-disubstituted-4, 5-dihydro-1H-imidazole-5-one and the derivatives thereof are suitably used as multifunctional materials, and are important raw materials especially for producing the medicine Avapro for treating high blood pressure.
Efficient 4,5-dihydro-1H-imidazol-5-one formation from amidines and ketones under transition-metal free conditions?
Xie, Yanjun,Cheng, Xiufang,Liu, Saiwen,Chen, Hui,Zhou, Wang,Yang, Luo,Deng, Guo-Jun
supporting information, p. 209 - 213 (2018/04/16)
An efficient procedure for 4,5-dihydro-1H-imidazol-5-one preparation from aryl amidines and ketones under transition-metal free conditions is described. When cyclic ketones were employed, various spiro-fused 4,5-dihydro-1H-imidazol-5-ones were formed in h
Oxidation of substituted imidazolidin-4-ones: New alternative method preparation of 4,5-dihydro-1H-imidazol-5-ones
Panov, Illia,Drabina, Pavel,Padelkova, Zdenka,Hanusek, Jiri,Sedlak, Milos
experimental part, p. 1356 - 1360 (2011/01/05)
The reaction of aldehydes (pentanal, benzaldehyde, 4-methoxybenzaldehyde, 4-nitrobenzaldehyde, salicylaldehyde, pyridin-2-carbaldehyde) with 1-aminocyclopentancarboxamide or (S)-2-amino-2,3-dimethylbutanamide has been used to prepare substituted imidazolidin-4-ones 1a-g (a: R1 = CH 3(CH2)3; b: R1 = C6H 5; c: R1 = 4-CH3OC6H4; d: R1 = 4-NO2C6H4; e: R1 = 2-HOC6H4; f: R1 = 2-pyridyl; for R2 = R3 = (CH2)4), and g: R1 = 2-pyridyl; for R2 = CH3; R3 = CH(CH 3)2) in the yields of 53-83%. Subsequent oxidations with various reagents gave the corresponding 4,5-dihydro-1H-imidazol-5-ones 2a-g: Pd/C (72-93%), DDQ (25-80%), and MnO2 (30-77%). Structure of the prepared compounds 1a-g and 2a-g was verified by 1H NMR and 13C NMR spectroscopy, EI-MS and elemental analysis. X-ray diffraction was performed in the case of compounds 1e and 2e.
