Polyfunctional pyrazoles. 4. Synthesis of 3-[3-aryl-1-(2-ethoxycarbonyl)-4-pyrazolyl]acrylic and-propionic acids

3-(3-Aryl-4-formyl-1-pyrazolyl)propionic acids are converted by Knoevenagel condensation under conditions of microwave activation into 3-[3-aryl-1-(2-ethoxycarbonyl)-4-pyrazolyl]acrylic acids. Reduction of the latter with hydrazine hydrate in the presence of Raney nickel gives 3-[3-aryl-1-(2-ethoxycarbonyl)-4-pyrazolyl]propionic acids. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 686–690, May, 2006.     

2-(1-苯基-3-芳基吡唑-4-基)-3-芳酰氨基-4-噻唑啉酮的合成

1-苯基-3-芳基-4-甲酰基吡唑与芳酰肼在乙醇中回流,缩合所得的腙在巯基乙酸作用下,合环得到2-(1-苯基-3-芳基吡唑-4-基)-3-芳酰氨基-4-噻唑啉酮类化合物,其结构经IR,MS,1HNMR谱和元素分析确证。     

Synthesis and Anticholinesterase Activity of 3-{[4-Methyl-3-(4-methylpiperazin-1-yl)]pent-1-en-1-yl}-4H-chromen-4-ones

Russian Journal of General Chemistry - A procedure has been developed and optimized for the synthesis of 3-{[4-methyl-3-(4-methylpiperazin-1-yl)]pent-1-en-1-yl}-4H-chromen-4-ones (as...     

1-Ethyl-1,4-dihydro-4-oxo-7-(pyridinyl)-3-quinolinecarboxylic acids. I. Synthesis of 3- and 4-(3-aminophenyl)pyridine intermediates

A series of substituted 3- and 4-(3-aminophenyl)pyridines has been prepared as intermediates for the synthesis of some 1-alkyl-1,4-dihydro-4-oxo-7-pyridinyl-3-quinolinecarboxylic acids. The Hantzsch, Hauser and other pyridine syntheses were used. 4-(3-Aminophenyl)pyridine was prepared via 3-(4-pyridinyl)-2-cyclohexen-1-one using the Semmler-Wolff reaction.     

Laser photolysis of 1-(4-nitrophenyl)-3-methylpyrazole and 1-ethyl-3-(4-nitrophenyl)-5-chloropyrazole

The spectral kinetic characteristics of the triplet states of 1-(4-nitrophenyl)-3-methylpyrazole (1) and 1-ethyl-3-(4-nitrophenyl)-5-chloropyrazole (2) were studied by the laser nanosecond photolysis technique in different solvents. The triplet lifetimes (τ_T) of molecules 1 and 2 were found to depend strongly on the solvent nature. An increase in τ_T by approximately two orders of magnitude on going from nonpolar and polar aprotic solvents (τ_T ≤ 15 ns) to aqueous-acetonitrile solutions (τ_T = 1100 ns for a volume acetonitrile to water ratio of 1 : 3) was analyzed, taking into account the influence of the medium on the relative contribution of the n,π*- and π,π*-configurations to the lowest triplet state. __________ Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1115–1119, May, 2005.     

Synthesis of blood group Forssman pentasaccharide GalNAcα1-3GalNAcβ1-3Galα1-4Galβ1-4Glcβ–R

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Synthesis of 1-(3',4'-dihydroxyphenyl)-7-(4"-hydroxyphenyl)- 4hepten-3-one

Natural diarylheptanoids have significant bioactivities. Some of them are potent inhibitors against prostaglandin biosynthesizing enzyme (PG synthetase) and 5-lipoxygenase (LT synthetase)1-2. Compound 1 was firstly isolated from Alnus rubra bark3. So far its synthesis has not been reported yet. Herein, we report the synthesis of compound 1. Meantime, compound 24 was also obtianed as an intermediate. Compound 7 and 16 were converted to compound 10 and 18 respectively, because compound 1…     

Molecular and Crystal Structure of 1-(4-Chlorophenyl)- 3- (4-Nitrophenyl)- 1-Triazene

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4-(4-氟苯基)-3-丁炔-1-醇的催化合成

设计合成了一种水溶性好、结构简单、性质稳定、安全无毒的高效含氮钯配合物催化剂[(NH2CH2COOH)2Pd Cl2],以对氟碘苯与3-丁炔-1-醇为起始原料,考察了溶剂、催化剂的用量、温度、时间和碱对Sonogashira偶联反应的影响,确定了最优反应条件,目标化合物分离产率高达96%。     

Unconventional nucleotide analogues. 3. 4-(N1-pyrimidyl)-2-aminobutyric acids

Alkylation of 4-ethoxy-2-hydroxypyrimidines (10a, b), via their anions, provides a convenient procedure for preparing N₁-substituted derivatives. Reaction of 10a, b with t-butyl 4-bromo-2-benzyloxycarbamidobutyrate (17) gives good yields of the N₁-alkylated products 18a, b. The latter have been converted to uracil- (20a), thymine- (20b) and cytosine- (21) substituted -aminobutyric acids.     

Synthesis of some new pyrazolyl-thiazolidinone derivatives starting from 1-(3-chlorophenyl)-3-(4-methoxyphenyl)-1H-pyrazole-4-carboxaldehyde

Russian Journal of General Chemistry - A novel synthetic approach to (E)-1-{[1-(3-chlorophenyl)-3-[(4-methoxyphenyl-1H-pyrazol-4-yl)- methylene]hydrazono}-3-phenylthiazolidin-4-one starting from...     

Microwave-assisted synthesis and antibacterial activity of derivatives of 3-[1-(4-fluorobenzyl)-1H-indol-3-yl]-5-(4-fluorobenzylthio)-4H-1,2,4-triazol-4-amine

Herein, an excellent method for the synthesis of twelve novel Schiff base derivatives containing indole and triazole assisted by microwave irradiation is reported. Compared with the conventional method, the yields increased from 59–84 % to 85–96 % and the reaction time was reduced from 24–30 h to 4–8 min. Moreover, all series of the newly synthesized Schiff bases were evaluated for their antibacterial activity. The values of minimum inhibitory concentration (MIC) and IC50 indicated that many target compounds possessed excellent antibacterial activity against Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Bacillus subtilis.