10325-70-9Relevant articles and documents
A 2-amino-thiazole compounds (by machine translation)
-
Paragraph 0178-0180, (2016/10/08)
The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
PREPARATION METHOD OF DIHYDROINDENE AMIDE COMPOUNDS THEIR PHARMACEUTICAL COMPOSITIONS CONTAING COMPOUNDS THEREOF AND USE AS PROTEIN KINASES INHIBITOR
-
Page/Page column 18-19, (2011/11/13)
The invention provides a new kind of dihydroindene amide compounds of general formula I or their pharmaceutically acceptable salts or prodrug thereof which can be used as protein kinase inhibitor. The invention provides a preparation method of the kind of compounds, the pharmaceutical compositions containing the compounds, the method for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR, using them as protein kinase inhibitor, and their preparation use of drug used for preventing or curing the diseases related to the abnormity of activities of protein kinases, especially Abl, Bcr-Abl, c-Kit and PDGFR,
Synthesis and muscarinic activity of 1,2,3,4-tetrahydropyrimidine derivatives
Jung, Myung Hee,Park, Jewn-Giew,Yang, Kong Jae,Lee, Mi-Jeoung
, p. 79 - 85 (2007/10/03)
3-Methyl-1,2,3,4-tetrahydropyrimidine-5-carbaldehyde O-substituted oximes 4 and 1-(3-methyl-1,2,3,4-tetrahydropyrimidin-5-yl)ethanone O-substituted oximes 9 have been prepared as bioisosteric congeners of arecoline which is a muscarinic agonist for treatment of Alzheimer's disease. Starting from pyrimidine-5-carbaldehyde 1, formation of the 3-methylpyrimidinium salt and subsequent reduction afforded 1,2,3,4-tetrahydropyrimidine derivatives which were converted into oxalate salts in the interest of purity and stability. Binding affinities of prepared compounds for the cloned human muscarinic M1 receptor (h-M1) were determined by radioligand binding assay using [3H]-N-methylscopolamine (NMS).
ACIDIFYING EFFECTS OF AZA GROUPS IN THE NH ACIDITY OF AMINOAZINES AND THE CH ACIDITY OF ACETYLAZINES
Terekhova, M. I.,Petrov, E. S.,Mikhaleva, M. A.,Shkurko, O. P.,Mamaev, V. P.,Shatenshtein, A. I.
, p. 6 - 10 (2007/10/02)
The pK values for a series of aminoazines and acetylazines containing one, two, or three aza groups in the ring were determined in dimethyl sulfoxide.There is a good linear correlation between pK values of the investigated NH and CH acids.The acidifying effects (ΔpK) of the aza groups at positions 2, 3, or 4 in relation to the side chain were determined and had values of 3.1, 2.4, and 4.5 logarithmic units in the aminoazines and 3.5, 2.9 and 4.8 logarithmic units respectively in the acetylazines.Except in the case of two ortho-located aza groups the effects are additive.Compared with dimethyl sulfoxide water has a differentiating effect on the acidity of the aminoazines, and this is explained by the formation of hydrogen bonds between the molecules of the proton-donating solvent and the aza groups of the anions of the aminoazines.
PYRIMIDINES. 73. SYNTHESIS OF ACETYLPYRIMIDINES
Naumenko, I. I.,Mikhaleva, M. A.,Mamaev, V. P.
, p. 710 - 714 (2007/10/02)
It is shown that the use of benzene as the solvent in the preparation of 2- and 4-acetylpyrimidines from cyanopyrimidines via the Grignard reaction makes this reaction a practical method for the preparation of pyrimidinyl ketones.Preparatively convenient methods for the preparation of 4-acetylpyrimidine from 4-ethylpyrimidine through the α-oximino derivative and 5-acetylpyrimidine from 4,6-dichloro derivatives of pyrimidine are proposed.
