- Production process of 4, 6-dimethoxy-2-methylsulfonyl pyrimidine
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The invention belongs to the field of organic synthesis, and discloses a production process of 4, 6-dimethoxy-2-methanesulfonyl pyrimidine. According to the production process, dimethyl malonate, thiourea and sodium methoxide are used as raw materials, and cyclization, methylation, chlorination, methoxylation, oxidation and recrystallization are performed to prepare the product. According to the process provided by the invention, the yield of the 4, 6-dimethoxy-2-methylsulfonyl pyrimidine is greater than 90%. Compared with the prior art, methanol, phosphorus oxychloride, methylbenzene and sodium tungstate are repeatedly utilized, so that the wastewater treatment difficulty is reduced, and the production cost is reduced; moreover, sodium sulfate, hydrochloric acid, sodium phosphate and sodium chloride can be co-produced while 4, 6-dimethoxy-2-methylsulfonyl pyrimidine is produced, so that pollutants generated in the production process are greatly reduced, and the economic benefit and environmental benefit of the production process are further improved.
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Paragraph 0014-0015; 0020-0021; 0024
(2021/03/30)
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- NEW PYRIMIDINE DERIVATIVES FOR PREVENTION AND TREATMENT OF GRAM-NEGATIVE BACTERIAL INFECTION, CONTAMINATION AND FOULING
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New pyrimidine derivatives together with a membrane penetrating agent, optionally with a detectable isotope and pharmaceutical composition for use in treatment or prevention of Gram-negative bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of Gram-negative biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. New pyrimidine derivatives together with a membrane penetrating agent; for use as radiotracer in diagnosing or prognosing Gram-negative bacterial infection in a host mammal.
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Page/Page column 86
(2020/10/28)
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- Synthesis of ticagrelor analogues belonging to 1,2,3-triazolo[4,5-d]pyrimidines and study of their antiplatelet and antibacterial activity
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Based on the recent observation that the antiplatelet agent ticagrelor and one of its metabolite exert bactericidal activity against gram-positive bacteria, a series of 1,2,3-triazolo[4,5-d]pyrimidines structurally related to ticagrelor were synthesized and examined as putative antiplatelet and antibacterial agents. The aim was to assess the possibility of dissociating the two biological properties and to find novel 1,2,3-triazolo[4,5-d]pyrimidines expressing antiplatelet activity and devoid of in vitro antibacterial activity. The new compounds synthesized were known metabolites of ticagrelor as well as structurally simplified analogues. Some of them were found to express antiplatelet activity and to lose the antibacterial activity, supporting the view that the two activities were not necessarily linked.
- Goffin, Eric,Jacques, Nicolas,Lancellotti, Patrizio,Musumeci, Lucia,Nchimi, Alain,Pirotte, Bernard,Oury, Cécile
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- PYRIMIDINE DERIVATIVES FOR PREVENTION AND TREATMENT OF BACTERIAL INFECTIONS
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New pyrimidine derivatives of formula (I), optionally with a detectable isotope, pharmaceutical composition and method of preparation thereof. New pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or prevention and use as inhibitors of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers. New pyrimidine derivatives for use as radiotracer in diagnosing or prognosing bacterial infection in a host mammal.
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Page/Page column 74; 75
(2019/09/04)
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- Convenient synthesis of 2-(methylsulfonyl)pyrimidine derivatives
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An efficient and convenient approach for the preparation of functionalized 2-(methylsulfonyl)pyrimidine derivatives has been developed through cyclic condensation of malonate derivatives with S-methylisothiouronium sulfate followed by derivation and oxidation in water–acetone mixture using oxone as the oxidant. This synthetic strategy provides an efficient and environmentally friendly approach for easy access to 2-(methylsulfonyl)pyrimidine derivatives with considerable yields.
- Huang, Tong-Hui,Zhou, Shan-Shan,Wu, Xin,An, Lin,Yin, Xiao-Xing
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supporting information
p. 714 - 720
(2018/02/16)
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- Facile synthesis of pyrido[2,3-d]pyrimidines via cyclocondensation of 4,6-dichloro-2-methylsulfanylpyrimidine-5-carbaldehyde with β-substituted β-aminoacrylic esters
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Abstract A new facile synthesis of pyrido[2,3-d]pyrimidin-4-ones via cyclocondensation of 4,6-dichloro-2-methylsulfanylpyrimidine-5-carbaldehyde with β-alkyl and β-aryl-β-aminoacrylic esters followed by hydrolysis of chlorine atom at position 4 of pyridopyrimidine ring has been developed. The cyclocondensation was found to be accelerated by acid.
- Chizhova, Maria E.,Bakulina, Olga Yu.,Ivanov, Alexander Yu.,Lobanov, Pavel S.,Dar'in, Dmitrii V.
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supporting information
p. 6196 - 6203
(2015/08/03)
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- Studies on the ATP Binding Site of Fyn Kinase for the Identification of New Inhibitors and Their Evaluation as Potential Agents against Tauopathies and Tumors
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Fyn is a member of the Src-family of nonreceptor protein-tyrosine kinases. Its abnormal activity has been shown to be related to various human cancers as well as to severe pathologies, such as Alzheimer's and Parkinson's diseases. Herein, a structure-based drug design protocol was employed aimed at identifying novel Fyn inhibitors. Two hits from commercial sources (1, 2) were found active against Fyn with Ki of about 2 μM, while derivative 4a, derived from our internal library, showed a Ki of 0.9 μM. A hit-to-lead optimization effort was then initiated on derivative 4a to improve its potency. Slightly modifications rapidly determine an increase in the binding affinity, with the best inhibitors 4c and 4d having Kis of 70 and 95 nM, respectively. Both compounds were found able to inhibit the phosphorylation of the protein Tau in an Alzheimer's model cell line and showed antiproliferative activities against different cancer cell lines. (Chemical Equation Presented).
- Tintori, Cristina,La Sala, Giuseppina,Vignaroli, Giulia,Botta, Lorenzo,Fallacara, Anna Lucia,Falchi, Federico,Radi, Marco,Zamperini, Claudio,Dreassi, Elena,Dello Iacono, Lucia,Orioli, Donata,Biamonti, Giuseppe,Garbelli, Mirko,Lossani, Andrea,Gasparrini, Francesca,Tuccinardi, Tiziano,Laurenzana, Ilaria,Angelucci, Adriano,Maga, Giovanni,Schenone, Silvia,Brullo, Chiara,Musumeci, Francesca,Desogus, Andrea,Crespan, Emmanuele,Botta, Maurizio
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p. 4590 - 4609
(2015/06/30)
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- PROCESSES FOR THE PREPARATION OF BISPYRIBAC SODIUM AND INTERMEDIATES THEREOF
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The present disclosure relates to a process for the preparation of Bispyribac-sodium by condensing 2,6-dihydroxy benzoic acid with 2-(alkyl sulfonyl)-4,6-dialkoxy pyrimidine in the presence of at least one base and at least one solvent. The present disclosure also relates to processes for the preparation of 2,6-dihydroxy benzoic acid and 2-(alkyl sulfonyl)-4,6- dialkoxy pyrimidine.
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Page/Page column 15-16
(2014/09/03)
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- Exploring the chemical space around the privileged pyrazolo[3,4-d] pyrimidine scaffold: Toward novel allosteric inhibitors of T315I-mutated Abl
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A library of pyrazolo[3,4-d]pyrimidines, endowed with a high level of molecular diversity, has been developed applying a synthetic sequence that allowed C3, N1, C4, and C6 substitution. The enzymatic screening of this "privileged scaffold"-based compound collection, validated the use of a diversity-oriented approach in a field characteristically explored by target-oriented synthesis. In fact, several compounds showed high activity against the selected kinases (i.e., Src, Abl wt, and T315I mutated-form), furthermore and interestingly a new compound has emerged as an allosteric inhibitor of the T315I mutated-form of Abl, opening up new opportunities for the development of a novel class of noncompetitive inhibitors of Abl (T315I).
- Vignaroli, Giulia,Mencarelli, Martina,Sementa, Deborah,Crespan, Emmanuele,Kissova, Miroslava,Maga, Giovanni,Schenone, Silvia,Radi, Marco,Botta, Maurizio
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supporting information
p. 168 - 175
(2014/05/06)
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- BICYCLIC CARBOXAMIDE INHIBITORS OF KINASES
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The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X1, X2, X3, X4, R1, R2, R3, A, B, Z, n, and m are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
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Page/Page column 58-59
(2012/08/07)
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- PYRIMIDINE SUBSTITUTED MACROCYCLIC HCV INHIBITORS
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Compounds of the Formula (I) including a stereoisomer thereof, or an N-oxide, a pharmaceutically acceptable addition salt, or a pharmaceutically acceptable addition solvate thereof; useful as HCV inhibitors; processes for preparing these compounds as well as pharmaceutical compositions comprising these compounds as active ingredient.
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Page/Page column 96
(2008/12/08)
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- 7-(4,6-dimethoxypyrimidinyl)oxy- and -thiophthalides as novel herbicides: Part 1. CGA 279 233: A new grass-killer for rice
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A series of novel types of 7-(4,6-dimethoxypyrimidin-2-yl)oxy - and -thio-3-methyl-1 (3H)-isobenzofuranones were discovered at Dr R Maag AG. From the thio-isobenzofuranyl series, CGA 279 233 - BSI-proposed common name pyriftalid - was chosen for further development as a grass herbicide for use in rice. General synthetic approaches to these new phthalic acid-derived compounds are given, with emphasis on the synthesis of pyriftalid and its physico-chemical behaviour.
- Luethy, Christoph,Zondler, Helmut,Rapold, Thomas,Seifert, Gottfried,Urwyler, Bernhard,Heinis, Thomas,Steinruecken, Hans Christian,Allen, James
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p. 205 - 224
(2007/10/03)
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- Triazolo[4,5-D]pyrimidinyl derivatives and their use as medicaments
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The invention relates to triazolo[4,5-d]pyrimidin-3-yl derivatives which are useful in the treatment of platelet aggregation disorders.
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- Novel pyrimidine and 1,3,5-triazine hypolipidemic agents
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New compounds were synthesized by changing the substituents of a trisubstituted pyrimidine, i.e., [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]acetic acid, a potent hypolipidemic agent, impaired, however, by a marked hepatomegaly-inducing effect. The structural variations led to the subsidence (14b, i.e., 4-chloro-2-(dimethylamino)-6-[(2,3-dimethylphenyl)amino]pyrimidine) or to the reduction (18b, [[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]amino]acetic acid) of said untoward effect but still maintained the hypolipidemic effect that, although markedly decreased, still proves significant for serum cholesterol and triglycerides (18b) or for serum triglycerides only (14b).
- d'Atri,Gomarasca,Resnati,Tronconi,Scolastico,Sirtori
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p. 1621 - 1629
(2007/10/02)
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- Pyrimidine (4,6)diyl-bis-(thiono)(thiol)-phosphoric(phosphonic)acid esters
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Pyrimidine (4,6)diyl-bis-(thiono)(thiol)-phosphoric (phosphonic) acid esters of the formula STR1 in which R is alkyl with 1 to 6 carbon atoms, R1 is alkyl, alkoxy or alkylmercapto each with 1 to 6 carbon atoms or phenyl, R2 is alkyl, alkoxy or alkylmercapto each with 1 to 5 carbon atoms, hydrogen or phenyl, R3 is hydrogen, alkyl with 1 to 4 carbon atoms or halogen, and X is oxygen or sulfur, Which possess insecticidal and acaricidal properties.
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- Substituted 6-hydroxy pyrimidines
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The present invention concerns novel 4-hydroxypyrimidine derivatives of the formula: SPC1 Wherein R1 is a substituent, e.g., alkyl, R2 is hydrogen or a substituent, e.g., alkyl R3 is amino unsubstituted or substituted by alkyl, a nitrogen heterocycle, alkoxy or alkylthio, which are used as intermediates in the production of useful insecticides.
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