- Synthesis method of 2-(1H-1,2,4-triazole-1-ethy)acetic acid
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The invention relates to a synthesis method of 2-(1H-1,2,4-triazole-1-ethy)acetic acid, and mainly solves the technical problem that no suitable industrial synthesis method exists at present. The preparation method comprises the following two steps: first
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Paragraph 0007; 0008; 0009
(2019/10/01)
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- Synthesis of N- and C-azolyl-substituted pyrazolo[1,5-a]pyrimidines by recyclization of pyrimidinium salts
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We studied the reaction of 2-(ethoxycarbonyl)methyl-1,4,6-trimethylpyrimidinium iodide with hydrazides of N-azolyl- and C-pyrazolyl-substituted carboxylic acids, which were synthesized by reacting the respective esters with hydrazine hydrate. This reaction was shown to result in recyclization and formation of ethyl 2-(pyrazolylalkyl)- and 2-(azolylalkyl)-5,7-dimethylpyrazolo[1,5-a]pyrimidine- 3-carboxylates. Besides pyrazolopyrimidines, the separation of reaction mixture provided in some cases also another recyclization product, 2-hydroxy-5,7-dimethylpyrazolo[1,5-a]pyrimidine.
- Danagulyan, Gevorg G.,Tumanyan, Araksya K.,Attaryan, Oganes S.,Tamazyan, Rafael A.,Danagulyan, Anna G.,Ayvazyan, Armen G.
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p. 483 - 490
(2015/10/19)
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- PROTEIN KINASE INHIBITORS
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A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
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Paragraph 0159
(2015/02/18)
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- PROTEIN KINASE INHIBITORS
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A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.
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Page/Page column 39
(2013/04/25)
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- Efficient synthesis and in vitro antifungal activity of 1H-benzimidazol-1-yl acetates/propionates containing 1H-1,2,4-triazole moiety
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A series of novel 1H-benzimidazol-1-yl acetates and 1H-benzimidazol-1-yl propionates containing 1H-1,2,4-triazole moiety were synthesized under microwave irradiation by multi-step reactions, in yields of 87-94%. Their in vitro antifungal activities against Botrytis cinerea and Sclerotinia sclerotiorum were evaluated by mycelial growth rate method. All the target compounds exhibit high activities against B. cinerea with the EC50 values of 7.96-21.74 μg/mL, higher than that of carbendazim.
- Zhang, Pei Zhi,Zhou, Shao Fang,Li, Tian Ren,Jiang, Lin
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p. 1381 - 1384
(2013/02/22)
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- Synthesis and properties of 1-dinitromethyl-3-R-1,2,4-triazoles
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Reductive denitration of 1-trinitromethyl-3-R-1,2,4-triazoles by KI or NH2OH followed by the treatment of the formed 1-dinitromethyl-3-R-1, 2,4-triazoles salts with sulfuric acid yielded dinitromethyl compounds (R = H, N3, Cl, NO2), sufficiently strong CH-acids (pKa 1.37-0.12) whose typical reactions are similar to those of gem-dinitrocompounds from the aliphatic series. The spectral data and the analysis of correlation relations between pKa of 1-dinitromethyl-3-R-1,2,4-triazoles and the substituent constants confirm that their structure is analogous to that of the majority of compounds belonging to the mentioned series. Nauka/Interperiodica 2007.
- Kofman,Trubitsyn,Dmitrienko,Glazkova,Tselinskii
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p. 758 - 764
(2008/02/08)
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- BIOMIMETIC, CHEMICAL, AND SPECTROSCOPIC EVALUATIONS FOR THE RADIOSENSITIZING POTENTIAL OF N1- AND N2-SUBSTITUTED DERIVATIVES OF 3-NITRO-1,2,4-TRIAZOLE TOWARD HYPOXIC CELLS IN THE RADIOTHERAPY: REMARKABLY DIFFERENT SUBSTITUTION EFFECT
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N1- and N2-derivatives of 3-nitro-1,2,4-triazole (3-NTR) were subjected to the non-biological evaluation methods involving biomimetic, chemical, and spectroscopic procedures for the radiosensitizing potential.Consequently, the N1-derivatives of 3-NTR were suggested to be more promising radiosensitizers to hypoxic cells in vivo than the N2-derivatives.
- Nagao, Yoshimitsu,Sano, Shigeki,Oxhiai, Masahito,Fujita, Eichi
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p. 3211 - 3232
(2007/10/02)
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