5-methyl-4-nitrosopyrazoles and synthesis method thereof

FIELD: chemistry.

SUBSTANCE: 3-methyl-4-nitrosopyrazoles are obtained via cyclocondensation of hydrazine salts with a nitrosation product obtained from 4,4-dimethoxybutan-2-one held in aqueous hydrochloric acid first. The obtained compounds can be used as modifiers and stabilisers of rubber mixtures, particularly during vulcanisation of butadiene-nitrile rubber and as fungicides.

EFFECT: novel method of producing 3-methyl-4-nitrosopyrazoles and obtaining novel 3-methyl-4-nitrosopyrazoles.

2 cl, 4 ex

 

The invention relates to the field of organic chemistry, in particular 3-methyl-4-nitrosophenol and the way they are received, which can be used as compounds with fungicidal activity, and as modifiers and stabilizers rubber compounds.

Analogues of substances not. So far, these substances are not known.

Known compounds of a number of 4-nitrosophenol with methyl(aryl) substituents in the 3 and 5 position of the pyrazol ring.

Known methods to obtain 3-methyl-4-nitrosophenol impossible. Direct nitrotyrosine 3-methyl-4-nitrosophenol could not be obtained, despite the fact that the reaction of electrophilic substitution (for example, halogenation) pyrazoles are light and the Deputy is in position 4, whereas nitrous acid has no significant effect on the pyrazoles, and enter nitrosourea in the 4 position is not possible. [Elderfield, Heterocyclic compounds, M.: publishing house of foreign literature, 1961. Volume 5, p.77.]

Cyclocondensation substituted hydrazine with 3-hydroximino-2,4-pentanedione obtained only 3,5-dimethyl-4-nitrosophenol, and 3-methyl-4-nitrosophenol thus not possible to obtain. [Patent 2,827,415 USA, W.A.Freeman, .Barnet, D.L.Pain, Rainham, R.Slack. Heterocyclic compounds, Appl. 13.08.1956, publ. 18.03.1958.]

Closest to the proposed method of obtaining 3-methyl-4-nitrosobis is Solow is the way to obtain 3,5-dimethyl-4-nitrosophenol structure

where R = cyclopentyl, cyclohexyl, cycloheptyl.

3,5-Dimethyl-4-nitrosophenol get cyclocondensation 3 hydroximino-2,3-pentanedione with salts of substituted hydrazines. In this way produce 3,5-dimethylsiloxane 4-nitrosophenol aqueous solution of 3-hydroximino-2,4-pentanedione add to hydrochloridum of cycloalkylation (cyclopentyl, cyclohexyl, cycloheptyl), then the reaction mass is stirred for 2 hours, fell 3,5-dimethyl-4-nitrosophenol filtered.

The disadvantage of this method is:

For the cyclocondensation is used only 1,3-diketone, namely 3-hydroximino-2,4-pentandiol, making this method suitable for obtaining dimethyl derivatives of pyrazole.

In the cyclocondensation used only cycloalumination that does not allow unsubstituted on indielisboa the nitrogen atom of the 3-methyl-4-nitrosophenol and his phenyl derivative.

By a known method to obtain 3-methyl-4-nitrosophenol not possible due to the presence of two metal groups in the 1,3-diketone, which during the test form is only 3,5-dimethyl-4-nitrosophenol.

The unique way of getting there.

The invention solves the single task of creating a new method for the preparation of 3-methyl-4-nitrosophenol.

The technical result of the conclusion which is to create a new way to obtain 3-methyl-4-nitrosophenol and retrieving previously unknown 3-methyl-4-nitrosophenol.

This technical result is achieved by the fact that the previously unknown 3-methyl-4-nitrosophenol get cyclocondensation salts of hydrazines of the formula NH2Other, where R=H, Ph, product nitrosation of an aqueous solution of sodium nitrite, pre-stored in an aqueous solution of hydrochloric acid 4,4-diethoxybutane-2-it, when the molar ratio of 4,4-diethoxybutane-2-it-to-hydrazine 1:0,5-1,8.

where R=H, Ph; X=Cl, ASO.

This method first obtained 3-methyl-4-nitrosophenol:

3-Methyl-4-nitrosophenol

Crystalline substance, blue-green, T. pl. 134-135º (ethanol),1H NMR spectrum (CDCl3), d, ppm: 2.95 (ush. C., 3H, CH3), 7.77 (ush. C. 1H arene.).13The NMR spectrum (CDCl3), d, ppm: 10.78, 29.81, 161.71. Soluble in ethanol, chloroform, ethyl acetate, diethyl ether.

3-Methyl-4-nitroso-1-phenylpyrazol

Crystalline substance, green, T. pl. 106-107°C (ethanol),1H NMR spectrum (CDCl3), d, ppm: 2.70 (ush. C., 3H, CH3), 7.43-7.46 (m, N arene.), 7.53-7.55 (m, 2H arene.), 7.77-7.79 (m, 2H arene.), 8.54 (ush. S. N. arene.).13The NMR spectrum (CDCl3), d, ppm: 12.75, 119.82, 128.45, 129.79, 138.55, 162.44. Soluble in ethanol, ethyl acetate, chloroform, diethyl ether.

The method of obtaining 3-methyl-4-nitrosophenol is as clicks the zoom. 1 N. hydrochloric acid is added 4,4-diethoxybutane-2-he and the reaction mass is stirred for 30 minutes. Then added dropwise an aqueous solution of sodium nitrite, otdovat oxides of nitrogen. To a solution of nitroso compounds obtained was added a freshly prepared solution of salt (acetic or hydrochloric acids) hydrazine (NH2-Other, R=H, Ph) and stirred for 2-3 hours at a molar ratio of 4,4-diethoxybutane-2-it-to-hydrazine 1: 0,5-1,8 (more or fewer salts of hydrazine leads to the decrease of the yield of the desired 3-methyl-4-nitrosophenol). 3-Methyl-4-nitrosophenol allocate by filtration or extraction with an organic solvent.

Example 1. Obtaining 3-methyl-4-nitrosophenol.

4,4-Diethoxybutane-2-he (1.32 g, 10 mmol) dissolved in 1 N. hydrochloric acid (10 ml), for 30 minutes, stirred at 20°C, cooled to 0°C and added dropwise a solution of sodium nitrite (0.76 g, 11 mmol) in 4 ml of water for 30 minutes. From the reaction mixture otdovat oxides of nitrogen in a water-jet vacuum pump, and then add a mixture of 10 ml of 1 N. hydrochloric acid (10 ml, 10 mmol) and hydrazine hydrate is added (0.5 ml, 9 mmol). Stirred for 10 minutes at 20°C, the precipitated crystals blue-green color filter. Yield 0.30 g, 30%. T square 134-135°C (ethanol).1H NMR spectrum (CDCl3), d, ppm: 2.95 (ush. C., 3H, CH3), 7.77 (ush. C. 1H arene.).13The NMR spectrum (CDCl3), d, ppm: 10.78, 29.81, 161.71.

Example 2. Obtaining 3-methyl-4-nitrosophenol.

4,4-Diethoxybutane-2-he (1.32 g, 10 mmol) dissolved in 1 N. hydrochloric acid (10 ml) and stirred for 30 minutes at 20°C, then cooled to 0°C and added dropwise a solution of sodium nitrite (0.76 g, 11 mmol) in 4 ml of water for 30 minutes. From the reaction mixture otdovat oxides of nitrogen under a water-jet vacuum pump, and then add a mixture of acetic acid (1.14 ml, 20 mmol) and hydrazine hydrate is added (18 mmol). Stirred for 10 minutes at 20°C. Extracted with diethyl ether and 5 ml × 5. The extract is dried over sodium sulfate and evaporated. The residue is recrystallized from ethanol. Output 0.284 g, 28%. T square 134-135°C (ethanol).1H NMR spectrum (CDCl3), d, ppm: 2.95 (ush. C., 3H, CH3), 7.77 (ush. C. 1H arene.).13The NMR spectrum (CDCl3), d, ppm: 10.78, 29.81, 161.71.

Example 3. Obtaining 3-methyl-4-nitroso-1-phenylpyrazole.

4,4-Diethoxybutane-2-he (1.32 g, 10 mmol) dissolved in 1 N. hydrochloric acid (10 ml) for 30 minutes, stirred at 20°C, cooled to 0°C. and dropwise within 30 minutes, add a solution of sodium nitrite (0.76 g, 11 mmol) in 4 ml of water. From the reaction mixture otdovat oxides of nitrogen in a water-jet vacuum pump, and then add the phenylhydrazine hydrochloride (4.5 mmol) in 8 ml of water. Stirred for 10 minutes at 20°C, the precipitated crystals green color filter. Yield 66%. T square 106-107°C (this is ol). 1H NMR spectrum (CDCl3), d, ppm: 2.70 (ush. s, 3H, CH3), 7.43-7.46 (m, N arene.), 7.53-7.55 (m, 2H arene.), 7.77-7.79 (m, 2H arene.), 8.54 (ush. S. N. arene.).13The NMR spectrum (CDCl3), d, ppm: 12.75, 119.82, 128.45, 129.79, 138.55, 162.44.

Example 4. Obtaining 3-methyl-4-nitroso-1-phenylpyrazole.

4,4-Diethoxybutane-2-he (1.32 g, 10 mmol) dissolved in 1 N. hydrochloric acid (10 ml), for 30 minutes, stirred at 20°C, cooled to 0°C. and dropwise within 30 minutes, add a solution of sodium nitrite (0.76 g, 11 mmol) in 4 ml of water. From the reaction mixture otdovat oxides of nitrogen in a water-jet vacuum pump, and then add the phenylhydrazine hydrochloride (9 mmol) in 8 ml of water. Stirred for 10 minutes at 20°C. Extracted with chloroform 5 ml × 3. The extract is dried over sodium sulfate and evaporated. The residue is recrystallized from ethanol. An output of 60%. T square 106-107°C (ethanol).1H NMR spectrum (CDCl3), d, ppm: 2.70 (ush. C., 3H, CH3), 7.43-7.46 (m, N arene.), 7.53-7.55 (m, 2H arene.), 7.77-7.79 (m, 2H arene.), 8.54 (ush. S. N. arene.).13The NMR spectrum (CDCl3), d, ppm: 12.75, 119.82, 128.45, 129.79, 138.55, 162.44.

The authors have obtained not previously described substances, which can be used as compounds with fungicidal activity, and as modifiers and stabilizers rubber compounds.

1. 3-Methyl-4-nitrosophenol General formula

where R is H, Ph.

2. The method of obtaining 3-methyl-4-nitroso is Rasulov, including cyclocondensation nitroso compounds and salts of hydrazine of the formula NH2Other, where R is H, Ph, as nitroso compounds use the product of nitrosation of an aqueous solution of sodium nitrite 4,4-diethoxybutane-2-she previously stored in an aqueous solution of hydrochloric acid, at a molar ratio of 4,4-diethoxybutane-2-it-to-hydrazine 1:0,5-1,8.



 

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1 cl, 5 ex, 5 tbl

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40 cl, 16 sch, 12 tbl, 65 ex

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25 cl, 6 tbl

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