6843-45-4Relevant academic research and scientific papers
Synthesis of glycolurils and hydantoins by reaction of urea and 1, 2-dicarbonyl compounds using etidronic acid as a “green catalyst”
Bakibaev, Abdigali A.,Uhov, Artur,S. Malkov, Victor,Yu. Panshina, Svetlana
, p. 4262 - 4270 (2020/10/02)
Most of the known methods for the synthesis of heterocyclic compounds have disadvantages, such as a long reaction time and aggressive conditions. We have developed a new, rather simple and efficient method for the synthesis of a number of glycoluryls and hydantoins in water using a etidronic acid (HEDP) as “Green catalyst.” So, for the first time, the condensation reaction of ureas with 1, 2-dicarbonyl compounds was carried out in the presence of HEDP. Also based on NMR studies, a chemism of these reactions, which is stepwise, is proposed. It has been established that the optimal conditions for the synthesis of glycoluryls and hydantoins using HEDP are: temperature 80°C-90°C, 40-20 minutes, and the ratio of urea and HEDP is 1:1. In all cases, the remaining aqueous filtrate containing HEDP after the reaction can be reused for other cycles synthesis of glycoluril and other compounds, because HEDP is not converted during the reaction.
2,4-Imidazolinedione heterocyclic derivative, and preparation method and use thereof
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Paragraph 0081; 0082; 0083, (2017/07/01)
The invention belongs to the field of chemical medicines, and concretely relates to a 2,4-imidazolinedione heterocyclic derivative, and a preparation method and a use thereof. The structure of the 2,4-imidazolinedione heterocyclic derivative is represented by formula I. The invention also provides the preparation method and the use of the 2,4-imidazolinedione heterocyclic derivative. The 2,4-imidazolinedione heterocyclic derivative has a good inhibition effect on Pim-1 protein kinase micro-molecules, and has important exploitation application prospect.
IDENTIFICATION AND TREATMENT OF VULNERABLE PLAQUES
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Paragraph 0149, (2016/11/28)
A method of detecting an atherosclerotic plaque vulnerable to rupture in a subject comprises providing to the subject a labelled necrostatin or a derivative thereof, and visualizing the label, wherein a localization of the label in a plaque indicates the plaque is vulnerable to rupture. A method of detecting and treating an atherosclerotic plaque vulnerable to rupture comprises providing to the subject a labelled necrostatin or a derivative thereof, visualizing the label, wherein a localization of the label in a plaque indicates the plaque is vulnerable to rupture; and providing a necroptosis inhibitor or derivative thereof to the subject when the visualizing indicates that the plaque is vulnerable to rupture. The necroptosis inhibitor may comprise a necrostatin, such as Nec-1. The label may be a radiolabel such as 123I. By visualizing plaques vulnerable to rupture, atherosclerotic plaques may be identified and treated in advance of rupture.
NOVEL AMIDE DERIVATIVE AND USE THEREOF AS MEDICINE
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Paragraph 0780; 0781; 0782, (2013/03/26)
Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.
AMINOMETHYL BIARYL BENZOTRIAZOLE DERIVATIVES
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Page/Page column 29, (2012/11/14)
The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
Facile synthesis of hydantoins and thiohydantoins in aqueous solution
Baccolini, Graziano,Boga, Carla,Delpivo, Camilla,Micheletti, Gabriele
experimental part, p. 1713 - 1717 (2011/05/05)
A series of hydantoins and thiohydantoins have been synthesized in water at room temperature from urea (or N-methylurea, or thiourea) and simple aldehydes (as glyoxal, and its simple derivatives) in the presence of phosphoric anhydride. The reaction time is 10 min using an equimolar amount of P 4O10 with respect to the other reagents, but the reaction occurs also, even if with longer reaction times, with very small amounts of P4O10. In addition, this method provides a clean and 'green' approach to hydantoins, compounds of great interest in biological and pharmacological fields.
Synthesis of imidazol[1,5-a]indole-1,3-diones from imidazolidene-2,4-diones
Akeng'a,Read
, p. 11 - 16 (2008/09/16)
Copper and tributyltin hydride catalysed cyclization, through the N-aryl bond formation, of imidazolidine-2,4-diones (11-16,18) yielded imidazo[1,5-a]indole-1,3-diones (5-10) in high yields (72-100%). The ease of cyclization was found to be consistent with the normal halogen reactivity and the type of substituents. The highly substituted imidazole-2,4-dione 15 gave brominated 19 and tin incorporated heterocycles 20 when treated with copper bromide and tributyltin hydride, respectively.
Unusual oxidation behaviour of a propargylic alcohol
Porter, Michael J.,White, Nicola J.,Howells, Garnet E.,Laffan, David D.P.
, p. 6541 - 6543 (2007/10/03)
Attempts to convert a propargylic alcohol bearing an imidazolone substituent to the corresponding aldehyde under Parikh-Doering conditions gave an α,β-unsaturated-β-methylsulfanyl aldehyde, which cyclised under mildly acidic conditions. Attempts to convert a propargylic alcohol bearing an imidazolone substituent to the corresponding aldehyde under Parikh-Doering conditions gave an α,β-unsaturated-β- methylsulfanyl aldehyde, which cyclised under mildly acidic conditions.
Methyl orthocarboxylates as methylating agents of heterocycles
Janin, Yves L.,Huel, Christiane,Flad, Genevieve,Thirot, Sylvie
, p. 1763 - 1769 (2007/10/03)
Methylation reactions occurring between trimethyl orthocarboxylates or N,N-dimethylcarboxamide dimethyl acetals and various hydroxylated heterocycles, involving a lactam-lactim tautomeric equilibrium, were investigated as an alternative to classic methyla
A New Method of Synthesis of 3-Monosubstituted-2-thiohydantoins and -Hydantoins
Ryczek, J.
, p. 2599 - 2604 (2007/10/02)
A new method of synthesis of 3-monosubstituted derivatives of 2-thiohydantoin and hydantoin in reaction of isothiocyanate or isocyanate glycin ethyl ester with primary aliphatic and aromatic amines has been described. Crude products were obtained with high yield and purity. The structure of these compounds was confirmed by spectral methods. Key words: 2-thiohydantoin, hydantoin, isothiocyanate glycin ethyl ester, isocyanate glycin ethyl ester
