6623-81-0Relevant articles and documents
Preparation method of 2-chloro-5-methoxypyrimidine
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Paragraph 0014-0017, (2019/10/23)
The invention relates to the field of compound preparation methods, and in particular relates to a preparation method of 2-chloro-5-methoxypyrimidine, which is prepared by taking methyl methoxyacetateas a raw material. The product prepared by the preparation method has high purity, the catalyst and the solvent can be recycled, the reaction is mild, the control is easy, and the method is suitablefor industrial production.
NOVEL PYRIMIDINE COMPOUNDS AS MTOR AND P13K INHIBITORS
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Page/Page column 109, (2011/07/30)
The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.
Falcipain inhibitors: Optimization studies of the 2-pyrimidinecarbonitrile lead series
Coterón, Jose M.,Catterick, David,Castro, Julia,Chaparro, María J.,Díaz, Beatriz,Fernández, Esther,Ferrer, Santiago,Gamo, Francisco J.,Gordo, Mariola,Gut, Jiri,De Las Heras, Laura,Legac, Jennifer,Marco, Maria,Miguel, Juan,Mu?oz, Vicente,Porras, Esther,De La Rosa, Juan C.,Ruiz, Jose R.,Sandoval, Elena,Ventosa, Pilar,Rosenthal, Philip J.,Fiandor, Jose M.
experimental part, p. 6129 - 6152 (2010/10/21)
Falcipain-2 and falcipain-3 are papain-family cysteine proteases of the malaria parasite Plasmodium falciparum that are responsible for host hemoglobin hydrolysis to provide amino acids for parasite protein synthesis. Different heteroarylnitrile derivatives were studied as potential falcipain inhibitors and therefore potential antiparasitic lead compounds, with the 5-substituted-2- cyanopyrimidine chemical class emerging as the most potent and promising lead series. Through a sequential lead optimization process considering the different positions present in the initial scaffold, nanomolar and subnanomolar inhibitors at falcipains 2 and 3 were identified, with activity against cultured parasites in the micromolar range. Introduction of protonable amines within lead molecules led to marked improvements of up to 1000 times in activity against cultured parasites without noteworthy alterations in other SAR tendencies. Optimized compounds presented enzymatic activities in the picomolar to low nanomolar range and antiparasitic activities in the low nanomolar range.
Experimental measurement and correlation of the solubilities of 2,4-dichloro-5-methoxypyrimidine in ethyl ethanoate, methanol, ethanol, acetone, tetrachloromethane, and heptane at temperatures between (295 and 320) K
Liu, Yong-Jie,Luo, Ting-Liang,Yao, Xin-Ding,Mao, Zhi-Bo,Liu, Guo-Ji
body text, p. 1402 - 1404 (2010/09/04)
The solid-liquid equilibrium of 2,4-dichloro-5-methoxypyrimidine was first determined in this article. Using a laser monitoring observation technique, the solubilities of 2,4-dichloro-5-methoxypyrimidine in ethyl ethanoate, methanol, ethanol, acetone, tetrachloromethane, and heptane have been determined experimentally from (295.60 to 316.39, 302.37 to 316.95, 299.44 to 316.61, 297.35 to 311.37, 298.60 to 312.15, and 298.10 to 320.08) K, respectively. The results are correlated with λ-h equation and Apelblat equation. The calculated results show that the correlation of the Apelblat model for six measured systems has less deviation than that of the λ-h equation.
ANTHRANILAMIDE INHIBITORS OF AURORA KINASE
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Page/Page column 15, (2008/12/07)
The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; where R1, R2, R3, R4, r and s are as previously defined. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.
Reactions of benzonitrile oxide with methoxypyrimidines and pyrimidones
Corsaro, Antonino,Pistara, Venerando,Rescifina, Antonio,Chiacchio, Maria A.,Piperno, Anna,Romeo, Giovanni
, p. 1079 - 1097 (2007/10/03)
Methoxypyrimidines preferentially add to benzonitrile oxide to give cycloadducts to their C=N double bonds. These, however, lose benzonitrile affording the corresponding pyrimidones. Cycloadditions to their C=C double bonds take place to a very low extent, and products generally undergo a ring opening process which affords the corresponding oximes. Pyrimidones preferentially give addition products to their nitrogen atoms, and only in the case of 4-pyrimidone, the cycloadduct to its C=C double bond was isolated.
Simultaneous determination of five oxidative DNA lesions in human urine
Ravanat, Jean-Luc,Guicherd, Pascale,Tuce, Zorana,Cadet, Jean
, p. 802 - 808 (2007/10/03)
A method, involving a HPLC prepurification followed by a GC/MS analysis, has been set up for the measurement of nucleic acid oxidation products in human urine. For this purpose, isotopically labeled internal standards have been prepared and used for isotope dilution mass spectrometric detection. Using this approach, four oxidized DNA bases, i.e., 5-hydroxyuracil, 5- (hydroxymethyl)uracil, 8-oxo-7,8-dihydroadenine, and 8-oxo-7,8- dihydroguanine, together with 8-oxo-7,8-dihydro-2'-deoxyguanosine have been simultaneously quantified in human urine samples. The levels of the oxidized nucleic acid constituents, as expressed in picomoles per milliliter, were determined to be, in decreasing order: 8-oxo-7,8-dihydroguanine (583 ± 376) > 5-(hydroxymethyl)uracil (121 ± 56) > 5-hydroxyuracil (58 ± 23) > 8-oxo- 7,8-dihydro-2'-deoxyguanosine (30 ± 15) > 8-oxo-7,8-dihydroadenine (7 ± 4). Attempts to determine the amount of 5,6-dihydroxy-5,6-dihydrothymine, 5- hydroxycytosine, and 2,6-diamino-4-hydroxy-5-formamidopyrimidine using the above HPLC-GC/MS method were unsuccessful.
Phenylation of pyrimidinones using diphenyliodonium salts
Jacobsen, Stig Andre,Rodbotten, Synne,Benneche, Tore
, p. 3265 - 3268 (2007/10/03)
Pyrimidinones 1 have been phenylated under basic conditions using diphenyliodonium salts, and the effect of substituents on the yield and regiochemistry has been studied. The Royal Society of Chemistry 1999.