Method of producing d(+) glucosamine hydrochloride

FIELD: chemistry.

SUBSTANCE: method involves preliminary acetylation of chitin with acetic anhydride, washing and drying the acetylated chitin in order to reduce degree of deacetylation thereof and, as a result, increase output of the desired product - D(+)-glucosamine hydrochloride when obtaining said product through hydrolysis of acetylated chitin with concentrated hydrochloric acid while heating, followed by evaporation, crystallisation, separation, washing and drying the desired product.

EFFECT: high output of the desired product while maintaining its high quality; method is more environmentally friendly since pre-treatment of chitin reduces the amount of processing wastes.

1 cl, 2 ex

 

The invention is intended for use in medicine, veterinary medicine, cosmetics and relates to a method of obtaining amino sugars that are used as chemical reagents and drugs.

A method of obtaining D(+)-glucosamine hydrochloride, which consists in the hydrolysis of chitin in concentrated hydrochloric acid with stirring and heating in a boiling water bath for 2.5 hours, the Ratio of the mass of chitin and weight of hydrochloric acid with a specific gravity 11,18 g/cm3is 1:5,9. After hydrolysis to the solution was added water (at a ratio of chitin : water 1:5) and active carbon (with a ratio of 1:0,1). The mixture discolor under stirring at 60C for 1 h and filtered. If necessary, the discoloration of the hydrolyzate repeat. The purified hydrolysate evaporated in vacuum at 50C up to 2-4% of the original solution 10-15 ml.

Crystals of D(+)-glucosamine hydrochloride is washed with ethyl alcohol and then dried. The product yield is 60-70% (Synthesis of organic products. Collection 4 / Per. from English. - M.: Publishing house of foreign literature, 1953. - 660 S. P.140-141). (Purchase E.R., Braun SE D-Glucosamine hydrochloride // Organic Syntheses. - 1946. - Vol.26. - P.36-37).

Also known is a method of obtaining D(+)-glucosamine hydrochloride by dissolving chitin in excess of concentrated hydrochloric acid and subsequent evaporation of the solution to the images is of the slurry. The resulting suspension is diluted with water at a ratio of chitin and water 1:2.5 and the solution discolor active charcoal for 4-5 minutes, the Coal is separated by filtration, the filtrate is evaporated in a vacuum until the beginning of crystallization, is cooled, and the precipitated crystals are separated by filtration.

Next, the crystals are washed with cold water, alcohol, and dried. Additional purification of D(+)-glucosamine hydrochloride is carried out by recrystallization from hot 80%ethanol.

The product yield is 70-74% (S. Markov Method for polusavan on glucosaminidase // pharmacy (Bhlh). - 1964. - T, No. 2. - P.30-32).

Closest to the present invention is the method according to the invention (Cossacks A.L., Samokish I.I., Kompancev VA, Lobova H., Novikov V.Y., Orlova T.A. Pyatigorsk pharmaceutical Institute; NGO "Sevrybtekhcentr", Murmansk. The method of producing glucosamine hydrochloride with antiarthrotic activity: Patent RU 2038095. - MCI6AC 35/60. - Appl. 05.09.1991; No. 5037787/14; Publ. 27.06.1995. - Bull. No. 18), in which to obtain the target product of the hydrolysis of chitin conduct of concentrated hydrochloric acid (1:10) for 2 h at the temperature of the water bath at 75C, followed by dilution of the hydrolysate with water and a combination of hydrolysis and purification of its activated carbon at 60C, the evaporation of the hydrolyzate in vacuum at a temperature not exceeding 60C to a residual of what Yama liquid 15% of the original quantity of hydrochloric acid and isolation of the target product by crystallization from an aqueous acidic solution under stirring.

Sediment D(+)-glucosamine hydrochloride is separated and washed with 96%alcohol to white, dried at a temperature not exceeding 60C.

The yield of the target product is 69% when the content of the basic substance D(+)-glucosamine hydrochloride and 99.4-99.6% of the chloride ion and at least 99% by the method of Elson-Morgan.

Known also improved the way, precluding the use of active charcoal (Novikov V.Y. Ivanov A.L. Company "Atlant-SIM-Victor". The way to obtain hydrochloride of D(+)-glucosamine: RF Patent 2042685, MKI6SN 5/06, SW 37/08. - Appl. 02.11.92; No. 92003453/04; Publ. 27.08.95. - Bull. No. 24).

Chitin from crustacean shell dissolved in concentrated hydrochloric acid 30-37%, heated in a boiling water bath for 45-120 min with a ratio of mass of chitin and weight of hydrochloric acid(1:2)-(1:4).

Within 5-10 min after the start of heating chitin is soluble in boiling hydrochloric acid, then the solution stand until complete hydrolysis of chitin, the reaction mixture is cooled to room temperature (10-20C) and left at this temperature for crystallization of D(+)-glucosamine hydrochloride in 8-48 hours

The precipitation dirty product is separated by decantation, filtration or centrifugation at room temperature. The precipitate is washed with an organic solvent (e.g. ethyl or isopropyl alcohol, acetone and others) when zootoxin and mass of chitin and solvent(1:5)-(1:3), the washed precipitate is dissolved with stirring in water with a temperature of 50-80C. the mass ratio of chitin and water(1:2)-(1:3).

The solution is filtered (centrifuged), evaporated in vacuo to 5-10% of the original volume at a temperature in the solution is not more than 60C.

Crystals of D(+)-glucosamine hydrochloride is separated and washed with an organic solvent portions 2-4 times. Washing is carried out until the pH of the leaching solution is not less than 2-3 on universal indicator paper.

The washed crystals of D(+)-glucosamine hydrochloride is dried in air at room temperature for 4-24 h, and then in a drying device at a temperature not exceeding 60C.

This method eliminates the use of activated carbon to carry out technological process without filtering hot hydrochloric acid solutions without expensive surgery evaporation of concentrated hydrochloric acid. Describes how close to the stated.

No loss of target product on active coal allows to increase the yield of D(+)-glucosamine hydrochloride to 70-76%.

All of the above methods of obtaining D(+)-glucosamine hydrochloride include the hydrolysis of chitin hydrochloric acid when heated, evaporation, crystallization, separation, washing and drying of the target product, the yield of the finished product does not exceed 60-76%, which is insufficient, as this is the results can be improved.

As raw materials typically used chitin, obtained according to the technology, including the deproteinization hot alkaline solution (usually 4% NaOH) and at room temperature a solution of mineral acid (usually 3.5 to 7% Hcl).

Analysis of samples of chitin obtained in this way, and known data on the same analysis described in the scientific literature show that chitin has a degree of deacetylation of about 15%.

This is because in the process of obtaining the product and during alkaline treatment, and when acid is the hydrolysis of amide bonds, causing the deacetylation.

It is also known that glycosidic bonds at the second carbon atom deacetylating unit link partially deacetylating chitin or chitosan) is subjected to acid degradation and depolymerization at a rate several times smaller than the same connection, the acetylated link that is explained by the fact that the amino group in position 2, the positively charged under the conditions of acid-catalyzed hydrolysis, reduces the electron density on the glycosidic centre, destabilizing carbocaine, shifting the equilibrium towards the initial state.

On the other hand, acetylation of the amino group at the second carbon atom accelerates the hydrolysis of glycosides by increasing the electron density and animaroo of things shall who I am. This stabilizes carbocation that increases the probability of dissociation and, therefore, the increase in the rate of cleavage of the glycosidic bonds (Komano T. Studies on the chemical structure of mucopolysaccharides // Thesis or Dissertation. - Kyoto University, 1962. - 112 p. Varum K.M., Ottoy M.H. Smidsrod O. Acid hydrolysis of chitosans // Carbohydrate Polymers. - 2001. - Vol.46, No.1. - P.89-98).

We found that the rate of degradation decreases sharply with increase in the initial degree of deacetylation of chitin (Novikov VY Acid hydrolysis of chitin and chitosan // Journal of applied chemistry. - 2004. - Vol.77, No.3. - P.490-493). This leads to an increase in the yield of by-products and the reduction of the yield of monomer D(+)-glucosamine.

The mechanism involves two ways to increase the yield of the target product: inhibition of deacetylation reaction in an acidic medium or decrease the initial degree of deacetylation of chitin.

The first way is almost impossible in acidic environment in which the amide bond is easily broken down in the presence of protons (acid catalysis).

The second path is successfully used by us to improve the method of obtaining the target product - D(+)-glucosamine hydrochloride.

The proposed method provides the pre-acetylation of chitin acetic anhydride, washing and drying acetylated chitin in order to reduce the degree of deacetylation and, as R is the result, increase the yield of the target product - D(+)-glucosamine hydrochloride at getting it through hydrolysis of acetylated chitin with concentrated hydrochloric acid by heating with subsequent evaporation, crystallization, separation, washing and drying of the target product.

The proposed method 1 h (100 g) of chitin for acetylation fill 10 hours (1 l) 20% solution of acetic anhydride in ethanol, thoroughly stirred for 2-3 h and left at 4C for 24 hours with occasional stirring. Upon completion of the reaction in solution add 20 hours (2 l) of water and bring the solution to pH 7 using 1N. NaOH, filtered and washed several times with acetylated chitin distilled water. The obtained acetylated chitin pre-dried at a temperature not exceeding 60C. After the acetylation deacetylation of chitin is reduced and ranges from 1 to 3%.

The degree of acetylation was determined by the method of infrared spectrophotometry (Chebotok H.E., Novikov V.Y., I. Konovalov. The influence of crystallinity of chitin and chitosan on the kinetics of the alkaline deacetylation // Journal of applied chemistry. - 2007. - C, No. 10. - S-1729).

Subsequent obtaining the target product - D(+)-glucosamine hydrochloride from acetylated chitin can be made of the above described known methods, including acid hydro is from when heated (analogues of the proposed method). Thus, for example:

- according to the invention (U.S. Pat. No. 2038095), including the hydrolysis of chitin with concentrated hydrochloric acid under heating, adding activated charcoal, filtration, evaporation, washing and drying, the yield of the target product increased from 69% when the content of the basic substance D(+)-glucosamine hydrochloride and 99.4-99.6 percent to 81% at the same purity of the product;

- according to the invention (U.S. Pat. No. 2042685), including hydrolysis with hydrochloric acid under heating, cooling and crystallization, filtration, washing with ethanol, dissolution and filtration, evaporation, washing, drying, the yield of the target product increased from 70 to 76% to 87%, mass fraction of it in the product was 99.5 to 99.9%.

Studies have shown that pre-acetylation of chitin acetic anhydride in obtaining D(+)-glucosamine hydrochloride by known methods, including the hydrolysis of chitin with concentrated hydrochloric acid when heated, allows to increase the yield of the target product from 60-76% to 81-87% by reducing the degree of deacetylation of chitin subjected to hydrolysis. Thus, the technical result of the invention is a significant improvement in the yield of the target product, while maintaining its high quality.

Examples of the method.

Example 1.

In a round bottom flask with a capacity of 4 liters with a mixing device C is poured in 1 l of a 20% solution of acetic anhydride in ethyl alcohol, was cooled to 4C. and added with stirring 100 g of chitin. The mixture was continuously stirred for 3 h and then left at 4C and periodic stirring for 24 hours

After the reaction the mixture under stirring was added 2 l of distilled water and neutralized 1 N. solution of sodium hydroxide to a pH of 7.

The residue acetylated chitin separated by filtration under vacuum on a Buchner funnel through 1-2 layers of filter paper, washed 2-3 times with distilled water until the pH of the leachate is not below 6.5.

The precipitate was dried in air at 20-25C, and then in a drying Cabinet at a temperature not exceeding 60C.

Dried acetylated chitin loaded into a round bottom flask with a capacity of 2 liters was filled with 1000 g (at 847.5 ml) of concentrated hydrochloric acid (d=1,18 kg/m3) at room temperature (U.S. Pat. 2038095).

The flask with a reflux condenser and a stirrer was placed in a water bath with a temperature of 75C. After complete dissolution of chitin spent the hydrolysis at a temperature of 75C and stirring for 120 minutes

After hydrolysis in the flask with the reaction mixture was added 500 ml of distilled water (1:5 chitin:water) at a temperature of 80C, 50 g of active charcoal (1:0.5 chitin:coal) and the mixture was stirred at 60C for 2 h for the purification of the hydrolysate.

The hot solution profile is listed through 4 layers of filter paper on a Buchner funnel under vacuum. After filtering the coal was washed on the filter with hot (70C) distilled water 500 ml (1:5 chitin-water). The wash water was combined with the filtrate, which should be colorless or have a faint greenish-yellow color.

Then the purified solution was evaporated under vacuum on a rotary evaporator IL-1M at a temperature in a solution of 40-50C at 85%. The suspension is cooled to a temperature not exceeding 4C, kept for 8 h to complete crystallization of the dissolved product.

The obtained crystals were washed with 96%ethanol portions 3-4 times to white. The total number of alcohol wash 300 ml (240 g).

The washed crystals are dried first in air at room temperature for 3 h, and then in a drying Cabinet at 60C for 2 hours

Got 81 g D(+)-glucosamine hydrochloride. The yield of the target product was 81%.

Example 2.

Acetylated chitin obtained from 100 g of chitin, as described in example 1.

Part of the dried acetylated chitin (40 g) was loaded into a round bottom flask with a capacity of 500 ml, poured 120 g (101,7 ml) of concentrated hydrochloric acid (d=1,18 kg/m3) at room temperature (U.S. Pat. 2042685).

The flask with a reflux condenser and a stirrer was placed in a boiling water bath. After 5-10 min of chitin is completely dissolved in boiling acid. When premesis the Institute in the flask was added the rest of acetylated chitin (about 60 g). After complete dissolution of chitin spent hydrolysis at the boiling temperature of the mixture 94-96C and stirring for 120 minutes

After hydrolysis of the flask with the reaction mixture was cooled to room temperature and left for crystallization at 18 o'clock

Sediment dirty glucosamine hydrochloride was separated from the solution by filtration under vacuum on a Buchner funnel through 5 layers of filter paper.

The precipitate was washed with portions (4 times) with ethyl alcohol. Wash used 200 ml (160 g) of alcohol.

The washed precipitate dirty product was dissolved in 200 cm3hot distilled water with a temperature of 50C. the Hot solution was filtered through 2 layers of filter paper on a Buchner funnel under vacuum.

Then clean the solution was evaporated under vacuum on a rotary evaporator IL-1M at a temperature in a solution of 40-50C at 95%. The suspension was cooled to room temperature.

The obtained crystals were washed with ethyl alcohol portions 4 times. The total number of alcohol wash 200 ml (160 g). The washed crystals are dried first in air at room temperature for 3 h, and then in a drying Cabinet at 60C for 2 hours

Got 87 g of D(+)-glucosamine hydrochloride. The output is 87%.

The obtained D - (+)-glucosamine hydrochloride is a white crystalline powder odourless, non-hygroscopic, mod is CNA humidity of 0.5% ash less than 0.1%. Decomposition temperature (blackening of the sample) 195-200C, pH of aqueous 20%solution at 20C 3.5 to 4.5%

Mass fraction of D(+)-glucosamine hydrochloride in the product obtained by the proposed method, 99.5 to 99.9%.

Determination of the mass fraction of the main substances in the product was performed by two methods: titration of hydrogen chloride associated with the molecule of D(+)-glucosamine, a solution of sodium hydroxide with registration of changes in pH or conductivity of the solution; determination of mass fraction of total nitrogen by the method of kildala. Both methods gave similar results.

Identification was performed by infrared spectroscopy method.

The identity and purity of the product was determined by high performance liquid chromatography.

As the standard used drug in THE 6-09-05-936-78, D(+)-glucosamine hydrochloride qualification pure.

The obtained results demonstrate that pre-treatment of chitin, by acetylation with acetic anhydride to reduce the initial degree of deacetylation of chitin in obtaining D(+)-glucosamine hydrochloride by known methods, including the hydrolysis of chitin with concentrated hydrochloric acid when heated, can significantly increase the yield of the target product from 60-76% to 81-87%. The quality of the product remains high.

Cu is IU, the proposed method is more eco-friendly, as the pretreatment of chitin reduces the amount of waste to 11-14%.

The method of obtaining D(+)-glucosamine hydrochloride by hydrolysis of chitin with concentrated hydrochloric acid when heated with selection of the target product, including evaporation, crystallization, separation, washing and drying of the target product, characterized in that before the hydrolysis of chitin with concentrated hydrochloric acid to conduct preliminary preparation of chitin by acetylation with acetic anhydride, washing and drying acetylated chitin.



 

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