588-64-7Relevant articles and documents
Dual-parameter correlations on rate of dehydration step of a condensation reaction in aqueous solutions of ethanol, propan-2-ol and 2-methylpropan-2-ol
Habibi Yangjeh,Gholami,Mostaghim
, p. 884 - 889 (2001)
The reaction kinetics of the dehydration step of the condensation reaction between phenylhydrazine and benzaldehyde was studied spectrophotometrically in aqueous solutions of ethanol, propan-2-ol and 2-methylpropan-2-ol at pH 11.5 at 25 °C. The apparent second-order rate constants k2app of the reaction increase with mole fraction of water in all the aqueous solutions. Single-parameter correlations of log k2app versus π* (dipolarity/polarizability), α (hydrogen-bond donor acidity) and ETN (normalized polarity parameter) were obtained in all the aqueous solutions. In all cases, the correlations versus ETN and π* are acceptable, but correlations versus α are poor (e.g. in aqueous solutions of ethanol the correlation coefficients are 0.964, 0.967, and 0.751 respectively). The results of dual-parameter correlations of log k2app versus π* and α in all cases represent improvements with regard to the single-parameter models (in aqueous solutions of ethanol r = 0.995; s.e. = 0.038; n = 13). The apparent second-order rate constants of the reaction increase with α, π* and ETN. Increasing the hydrogen-bond donor acidity of the solvent stabilizes the activated complex of the reaction via hydrogen-bond formation with the intermediate. A dual-parameter equation of log k2app versus π* and α was obtained for the combined data set of aqueous solutions (n = 35, r = 0.989, s.e. = 0.062, F2.32 = 719.21), in which π* has the major effect on the reaction rate relative to α. Copyright
1, 3-diaryl-1, 2, 4-triazole compound as well as preparation method and application thereof
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Paragraph 0036-0038, (2021/01/29)
The invention discloses a 1, 3-diaryl-1, 2, 4-triazole compound, which has a novel structure shown in a structural general formula I and has better selective inhibition activity on HDAC6. The invention also discloses a preparation method of the compound, aryl groups and 4-amino-N-hydroxy-benzamide groups are introduced to a 1, 2, 4-triazole matrix for modification, a series of compounds with novelstructures are synthesized, and the method has the advantages of mild reaction conditions, simple operation, high yield and the like. The invention also discloses an application of the compound in preparation of a medicine for selectively inhibiting HDAC6. The compound provided by the invention can significantly inhibit HDAC6, the IC50 value of the compound is at a nanomole level, the dosage of apatient is favorably reduced, and the toxic and side effects of the medicine on a human body are reduced. The compound provided by the invention has high selectivity on subtype HDAC1, can effectivelyavoid toxic and side effects of a drug on normal tissues of a human body, and shows good development potential.
Mn(III)-mediated phosphinoylation of aldehyde hydrazones: Direct “one-pot” synthesis of α-iminophosphine oxides from aldehydes
Bian, Xue-Wei,Zhang, Ling,Shoberu, Adedamola,Zou, Jian-Ping
supporting information, (2021/04/02)
A “one-pot” strategy for the straightforward Mn(III)-mediated phosphinoylation of aldehyde hydrazones with diphenylphosphine oxide to furnish α-iminophosphine oxides is described. This mild and practical method allows the direct use of aldehydes as substrates in one pot to generate the hydrazones, which are then engaged “in situ” by the phosphorus reagent in the presence of Mn(OAc)3 oxidant. Thus, the requisite isolation of the hydrazones is not needed in this operation. Conducted mechanistic experiments implicate a pathway involving phosphorus-centered radicals.