The method of synthesis of 5-hydroxy-6-methyluracil

 

(57) Abstract:

The invention relates to organic chemistry, specifically to a method for producing 5-hydroxy-6-methyluracil, showing immunotropic activity permitted for medical use and industrial production, and can also be used in the treatment of immune disorders of various origins. Describes how to obtain 5-hydroxy-6-methyluracil, consisting in the oxidation with ammonium persulfate in an alkaline medium at 85-95C. the reaction mixture obtained by the saponification-enaminoketones ether, the allocation (or allocations) crystallization of the intermediate product - 5 - methyluracil-5-ammoniumsulfate and hydrolysis of the latter with sulfuric acid. The technical effect is to increase the yield and purity of the target product. 2 C.p. f-crystals.

The present invention relates to organic chemistry, in particular, to a method for producing 5-hydroxy-6-methyluracil formula

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manifesting pronounced immunotropic activity, and can be used in medicine and veterinary medicine. Created new original immunomodulator 5-hydroxy-6-methyluracil ("oximetry") enhances the immune response and effective in the treatment of infections, prepare the healing of wounds, trophic ulcers and burns, and reduces the harmful effects of radiation, protects from alcohol poisoning, nitrate, organophosphorus substances (dichlorvos, chlorophos, karbofos), normalizes the number of white blood cells, enhancing humoral and cellular immune system, has anti-stress, cardiotonic and anti-toxic effect.

5-Hydroxy-6-methyluracil is focused on the production of a product with new consumer qualities: treatment of immune disorders of various origins (infection, neoplastic disease, radiation injury, poisoning with various poisons, including dioxins). This property increases the value of the drug, especially in the regions with developed petrochemical industry.

5-Hydroxy-6-metalware by the Ministry of health and medical industry of the Russian Federation 302 from 29.07.96 registered in the Russian Federation and approved for medical use and industrial production (registration certificate 96/2).

A method of obtaining 5-hydroxy-6-methyluracil (H. R. Henze, Kahlenberg E. N., J. Am. Chem. Soc., 1958, v. 80, 7, R. 1664-1666) in 7 stages with a total yield of 9% by the interaction of monochloracetic acid (I) c storiesa the acid chloride (III) transform into secondary butylacetoacetate (IV) with excess secondary butyl alcohol, samarangense which methylate sodium gives secondary - butyl , - dialogselect (V), the treatment of the latter with thiourea gives 5-secondary butoxy-6-secondary butoxymethyl-2-thiouracil (VI), which is transformed under the action of monochloracetic acid in 5-secondary butoxy-6-secondary-butoxymethyl (VII), the treatment of which iodine-hydrogen acid gives the desired product (VIII).

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The total yield of 9% (0.8 x 0.6 x 0,56 x 0.79 x 0,84 x 0.51).

The disadvantage of this method is a multi-stage, low yield of the target product.

A method of obtaining 5-hydroxy-6-methyluracil by oxidation of 6-methyluracil with potassium permanganate in acetic acid at a temperature of 20-40oWith the release of 15-25% when the molar ratio 6th : KMPO4: CH3COOH = 1,5 : 1 : 1 ( Behrung R., Grunewald R., Justus Liebigs Annalen der chemie, 1902, I. 323, s.186-204).

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The disadvantage of this method is the low yield of the target product.

A method for the oxidation of 6-methyluracil with ammonium persulfate in an alkaline medium (the reaction of Elbs) followed by hydrolysis with hydrochloric acid at 100o(D. Hurst, T., Austr. J. Chem, 1983, 36, p.1285-1289).

The disadvantage of this method is that it leads to the production of 5-hydroxy-6-methyluracil with vyhodila by potassium persulfate (Gashev C. B., Bald L. C., Smirnov, L. D., latina B. N., CHC, 1989, 5, S. 636-640).

The authors identified the intermediate product is sulfate the ether of 6-methyl-5-hydroxyacyl with the release of 24%, the hydrolysis of which 10% N2SO4gives 5-hydroxy-6-methyluracil (VIII) with a yield of 78% (technical product).

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The disadvantage of this method is the low yield of the target product.

As you can see, all the ways to obtain 5-hydroxy-6-methyluracil go from methyluracil. Methyluracil currently in the industry (Russia) is obtained by condensation of diketene with urea in the presence of acetic anhydride and pyridine with a yield of 75% (Khromov N. In., Borisov, Karlinsky R. S., GOH, 1956, T. 26, 4-6, S. 1728).

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The disadvantage is that plastic surgery is available in insufficient quantity and cannot provide all the needs of the country.

Known synthesis methyluracil by condensation of acetoacetic ester and urea Synthesis of organic drugs, 1949, sat 2, S. 335).

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Thus the condensation of urea with acetoacetic ester (XVII) in the presence of concentrated hydrochloric acid in ethanol gives - enaminoketones ether (XVIII), alkaline hydrolysis which when the 100oC for 1 h leads to sodium salt - ur">

The disadvantage of this method is the length of the process, a multi-stage, low yield and purity.

Closest to the present invention is a method of obtaining 5-hydroxy-6-methyluracil by oxidation of 6-methyluracil with ammonium persulfate in an alkaline medium 40-70oWith the selection of the intermediate product 6-methyluracil-5-ammoniumsulfate and hydrolysis of the latter with sulfuric acid at 85-95o(Patent of the Russian Federation 2000278 authors Krivonogov B. N., and others).

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The disadvantage is that plastic surgery is produced in insufficient quantity and cannot provide all the needs of the country.

The aim of the invention is to find a method to obtain 5-hydroxy-6-methyluracil with great output, great purity, and reduce mnogostadiinost and time consuming process.

This goal is achieved by conducting the condensation of urea with acetoacetic ester receiving - enaminoketones ether (ECAS). The latter is subjected to saponification with sodium hydroxide solution to obtain an alkaline solution of the reaction mixture, which is cooled to 40-50oTo add solid sodium hydroxide at a molar ratio of 1:1-2 and then ammonium persulfate for ocierror-5-ammoniumsulfate, which is subjected to hydrolysis after separation or directly in the reaction mixture with sulfuric acid at 85-95oC.

Selection 6-methyluracil-5-ammoniumsulfate of the reaction mixture is performed by adding sulfuric acid to a pH of 6-7 and, if necessary, recrystallized from water with coal.

The proposed method differs from the known fact that carry out the condensation of urea and acetoacetic ester with getting-enaminoketones ether, which amyraut sodium hydroxide solution to obtain an alkaline solution of the reaction mixture, cooling it to 40-50oC, followed by addition of solid sodium hydroxide at a molar ratio of the UKE : TV. NaOH = 1:1-2, then ammonium persulfate to oxidize, obtaining 6-methyluracil-5-ammoniumsulfate, which is hydrolized.

The target product is obtained with a yield of 50-58%. Preferably the molar ratio of the components of the UKE : NaOH : TV. NaOH : PSA : H2SO4= 1:2:1-2:1-1,19: 1-1,5 respectively. The reaction takes place according to the following scheme.

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The invention is illustrated by the following examples.

Example 1. In a three-neck flask with a capacity of 1000 ml, equipped with a mechanical stirrer, reflux condenser, loads of 86.1 g (0.5 mol) - ur is) is poured a solution of NaOH (40 g/1 mol 600 ml of water), the reaction mixture is heated on a boiling water bath to dissolve the crystals, stirred for additional 30 min, and then the resulting solution was divided into 2 parts (325 ml).

1A. To the alkaline solution (235 ml), cooled to 40-50oWith, sprinkled with 20 g (0.5 mol) of NaOH and sprinkled parts of solid ammonium persulfate (0.33 mol or 75.2 g). After complete addition of ammonium persulfate, the reaction mixture is stirred an additional 30 min and then acidified with sulfuric acid to neutral reaction (12 ml) at 60oWith and leave overnight. The next day, the precipitated crystals are filtered through Sutovsky funnel, washed with acetone (2 x 20 ml), dried on air and get to 35.7 g (60%) of 6-methyluracil-5-ammoniumsulfate.

1B. The second part of the op.1 (325 ml) solution is poured in a three-neck flask with a capacity of 1000 ml, equipped with a mechanical stirrer, reflux condenser, sprinkled with 20 g (0.5 mol) of NaOH, heated to 40-50oC and at this temperature, sprinkled parts of solid ammonium persulfate (0.33 mol or 75.2 g) within 30 minutes After the complete addition of ammonium persulfate, the reaction mixture is stirred an additional 1 h 20 min and then acidified with sulfuric acid until neutral pH 6-7 (14 ml) for 30 VOUT acetone (2 x 20 ml), air-dried and receive 43,27 g (73%) of light yellow crystals of 6-methyluracil-5-ammoniumsulfate. Purity is proved by TLC (thin layer chromatography).

Example 2. Getting 5-hydroxy-6-methyluracil. In a three-neck flask is charged with 28.4 g (0,0118 mol) of 6-methyluracil-5-ammoniumsulfate (op.1A), dissolve it in 135 ml of water, heated to 85-95oC and at this temperature, added dropwise 14 ml conc. H2SO4. At the end of the addition of acid significantly drop crystals. The reaction mixture is left overnight. The next day, the precipitated crystals filtered off, washed with water until neutral (3 x 20 ml), acetone (2 x 15 ml) and receive 11.5g (68,2% taken 6-methyluracil-5-ammoniumsulfate or 41% on taken - enaminoketones ether) 5-hydroxy-6-methyluracil in the form of light yellow crystals with so pl. 340-345o(Crystals in a diamond shape).

Found, %: C 42; N 4,1; N 19,9. The content of 5-hydroxy-6-methyluracil 98,9% (titration method). Purity proved by TLC (absence of methyluracil). Calculated for C5H6N2O3, %: 42; N 4,2; N 19,7. IR spectrum ( cm-1: 1130 (=HE); 1260 (CO-NH); 1380 (sCH3); 1660, 3100 (); 1680 (-NH-CO-NH-); 3260 (HE). NMR1N ( M. D., D20): 1,99 (C., 3H, C6-CH3) regarly flask with a capacity of 500 ml, equipped with a mechanical stirrer, reflux condenser, load of 21.5 g (0.125 mol) - enaminoketones ether, obtained by the method of J. Donlevy and M B, poured a solution of NaOH (20 g (0.5 mol NaOH) in 150 ml of water), the reaction mixture is heated on a boiling water bath to dissolve the crystals, stirred for additional 30 min, cooled to 63-68oWith, and then sprinkled 8 g (0.2 mol) of NaOH and sprinkled parts of solid ammonium persulfate (0,158 mol, or 36 g). After complete addition of ammonium persulfate, the reaction mixture is stirred for an additional 120 min, and then heated to 85-95oC and at this temperature, added dropwise 34 ml conc. H2SO4. At the end of the addition of acid significantly drop crystals. The reaction mixture is left overnight. The next day, the precipitated crystals filtered off, washed with water until neutral (3 x 20 ml), acetone (2 x 15 ml) and obtain 10.3 g (58% taken - enaminoketones ether) 5-hydroxy-6-methyluracil in the form of yellow crystals with so pl. 340o.

Example 4. Synthesis of 5-hydroxy-6-methyluracil without isolating the intermediate product - 6-methyluracil-5-ammoniumsulfate.

In a three-neck flask with a capacity of 500 ml, equipped with a mechanical stirrer, reverse x is elewaut solution of NaOH (20 g (0.5 mol NaOH) in 150 ml of water), the reaction mixture is heated on a boiling water bath to dissolve the crystals, stirred for additional 30 min, cooled, and then sprinkled 5 g (0.125 mol) of NaOH and sprinkled parts of solid ammonium persulfate (0,158 mol, or 36 g). After complete addition of ammonium persulfate, the reaction mixture was stirred for additional 90 min, and then add a little activated charcoal, boiled for 15 min, the activated carbon is filtered off on shutovskoy funnel, and the mother liquor is heated to 85-95oC and at this temperature, added dropwise 20 ml conc. H2SO4. At the end of the addition of acid significantly drop crystals. The reaction mixture is left overnight. The next day, the precipitated crystals filtered off, washed with water until neutral (3 x 20 ml), acetone (2 x 15 ml) and gain of 7.1 g (40% taken - enaminoketones ether) 5-hydroxy-6-methyluracil in the form of light yellow crystals with so pl. 342-345oC.

Example 5. In a three-neck flask with a capacity of 500 ml, equipped with a mechanical stirrer, reflux condenser, loads of 51.6 g (0.3 mol) - enaminoketones ether, poured into NaOH solution (24 g (0.6 mol of NaOH in 300 ml of water), the reaction mixture is heated on a boiling water bath to dissolve the crystals, ne:

5A. To 100 ml of the solution obtained above, sprinkled parts of solid ammonium persulfate (0.1 mol or 22.8 g) at a temperature of 30-40oC. After complete addition of ammonium persulfate (30 min) the reaction mixture is stirred an additional 2 h, and then neutralized with sulfuric acid (4 ml), heated to 85-95oC and at this temperature was added 26 ml of concentrated sulfuric acid, stirred for 1 h, but the crystals do not fall, then 5-hydroxy-6-methyluracil failed.

5B. To 100 ml of the solution obtained above, sprinkled with a 4 g (0.1 mol) of NaOH and sprinkled parts of solid ammonium persulfate (0.1 mol or 22.8 g) at a temperature of 40oC. After complete addition of ammonium persulfate (30 min) the reaction mixture is stirred an additional 2 h, and then neutralized with sulfuric acid (4 ml), heated to 85-95oC and at this temperature was added 26 ml of concentrated sulfuric acid. At the end of the addition of sulphuric acid crystals fall 5-hydroxy-6-methyluracil. The reaction mixture is stirred for 1 h, cooled and allocate 5.9 g (41,6%) 5-hydroxy-6-methyluracil.

5V. To 100 ml of the solution obtained above, sprinkled 8 g (0.2 mol) of NaOH and sprinkled parts of solid ammonium persulfate (0.1 mol or 22.8 g) at a temperature of at 55o(The precipitate dissolves), stirred for additional 2 h, and then heated to 85-95oC and at this temperature, add 30 ml of concentrated sulfuric acid. At the end of the addition of sulphuric acid crystals fall 5-hydroxy-6-methyluracil. The reaction mixture is stirred for 1 h, cooled and release of 7.1 g (50%) 5-hydroxy-6-methyluracil.

According to the invention, carried out laboratory tests. First it is shown that the reaction mixture obtained after saponification - enaminoketones ether in alkaline medium, it is possible to oxidize the ammonium persulfate to obtain 5-hydroxy-6-methyluracil. It is established that this method is easily reproducible and can be used to develop laboratory regulations and building technologies production of 5-hydroxy-6-methyluracil on the enlarged installation and subsequent development of technological regulations.

Technical and environmental advantages of this method is the reduction of two stages, namely:

- reduction stage of the hydrolysis of sodium salt - enaminoketones acid (not spent hydrochloric acid);

- methyluracil is not allocated, and the reaction mixture obtained after saponification - enaminoketones ether is the additional amount of alkali for education disodium salt methyluracil (1 mol methyluracil in the oxidation of the ammonium persulfate were spent 4 mol of sodium hydroxide);

- due to this the cost of 5-hydroxy-6-methyluracil is almost 2 times cheaper than obtained from methyluracil.

1. The way to obtain 5-hydroxy-6-methyluracil formula

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using persulfate oxidation of ammonia in alkaline medium at 40 - 70oC, obtaining 6-methyluracil-5-ammonium sulfate, which is hydrolized with sulfuric acid at a temperature of 85 - 95oC, characterized in that conduct the condensation of urea and acetoacetic ester with getting - enaminoketones ether (ECAS), which amyraut sodium hydroxide solution, to obtain the alkaline solution of the reaction mixture, cooling it to 40 - 50oC, followed by addition of solid sodium hydroxide at a molar ratio ECAS : TV. NaOH = 1 : 1 - 2, and then the ammonium persulfate to oxidize, obtaining 6-methyluracil-5-ammoniumsulfate, which is hydrolized.

2. The method according to p. 1, characterized in that the 6-methyluracil-5-ammoniumsulfate separated from the reaction mixture by adding sulfuric acid to pH 6 - 7 and recrystallized.

3. The method according to p. 1, characterized in that the oxidation of lead within 30 minutes

 

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