The method of producing ergosterol
(57) Abstract:Usage: the invention relates to the field of biotechnology, and more specifically to methods of obtaining vitamins. The inventive method involves the production of ergosterol from yeast by processing a mixture containing 25-30% sodium hydroxide, 15-50% water and 25-50% of isopropyl alcohol extraction of ergosterin organic solvent selected from the group of substances comprising: isopropyl alcohol, distillation of isopropyl alcohol, a mixture of isopropyl alcohol and its distillate in a ratio of 1:1. table 2. The invention relates to the field of biotechnology, and more specifically to methods of obtaining vitamins, namely a process for the production of ergosterol.Vitamin D2get technology, including the cultivation of yeast Sacch. cerevisiae, the allocation of them ergosterol, photoisomerization of the latter under the action of UV-irradiation and selection of vitamin D2from photomay 
The biggest problem causes the stage of selection of ergosterol from yeast.Known methods of extraction of ergosterol, its extraction from yeast, processed COHN, dichloroethane or benzene, with subsequent distillation of the solvent [2,3]
The disadvantages of these methods, I is the technology of obtaining ergosterol, includes treatment of yeast with a water-alcohol solution of KOH in boiling, after which the mixture is filtered, the filtrate concentrated and crystallized, getting ergosterol raw, which is optionally crystallized from 65% ethyl alcohol 
Ergosterol has a melting point of not less than 158oC a purity of 88% and output depending on the composition of the yeast from 73 to 81%
The disadvantages of the prototype are the high consumption of ethyl alcohol, the need for its rectification, the duration of solvolysis (not less than 6 h), the need for filtering of neomillennial residues of yeast and low output.The purpose of the invention to develop more effective and manufacturable process.It was found that the efficiency of the process can be improved by conducting solvolysis mixture containing 25-50% isopropyl alcohol (IPA), 15-50% water and 25-35% sodium hydroxide, followed by extraction of ergosterol isopropyl alcohol in the ratio to the original yeast is not less than 0.6:1. A higher ratio is practically not lead to increased output, demand additional expenses for the selection of the target product.As solvent in the extraction step can be used as Tova what I solvolysis and extraction in the literature for obtaining vitamin D2not described, which confirms the compliance with the criterion of "world novelty."The study of the new conditions of solvolysis and extraction shows that the application of the new formula allows, in contrast to the use of ethyl alcohol, to create a two-phase system that eliminates stage filtration and loss of ergosterol, and, in contrast to the use of higher alcohols, such as butyl, managed in the process to avoid emulsification and foaming. Application for the extraction of the distillate IPS simplifies the process and increases the yield of ergosterol to 85-90%
The mentioned set of features not previously found, leads to unexpected results, in particular, to increase the yield of ergosterol to 90% which indicates compliance with a criterion of "inventive step".Example 1.A 5-liter flask with stirrer, thermometer and reflux condenser load of 2.25 kg of yeast, 450 ml of an aqueous NaOH solution containing 260 g of dry alkali and 250 g technical IPS. The mixture is boiled for 4 hours with stirring, cooled and add 1.5 kg technical IPS or its distillate, stirred for 30 min, defend and separating the upper layer of the extract, which is filtered from neznachytelnaya), which is boiled with 10-fold volume of isopropyl alcohol, filtered, the solvent is distilled off, the residue is dried in vacuum.The product contains 88-92% of ergosterol with tpl.159-160oC. Yield 90%
Example 2.In the conditions of example 1 were solvolysis various alkaline mixtures. The results obtained are given in table. 1.Example 3.In the conditions of example 1 were extracted and IPA distillation of isopropyl alcohol. The results obtained are given in table. 2.The application of new technology for production of ergosterol to produce vitamin D2"Farmakon" managed by reducing energy and labor costs, cost of reagents, increasing the output of ergosterol to get ready the economic effect of more than 4 million rubles (price 1992).Literature
1. A. I. Vorobyov. Microbiological synthesis of vitamins. M MSU, 1982, S. 139-150.2. HFG. 1971, No. 9, S. 41.3. Berezovsky C. M. Chemistry of vitamins. M Food industry, 1973, S. 130. The method of producing ergosterol from yeast by treating them with an alkaline reagent, extraction of ergosterol organic solvent and selection of the target product, characterized in that as the alkaline reagent, a mixture, startelem, selected from the group of substances including isopropyl alcohol, distillation of isopropyl alcohol, obtained at the stage of evaporation, the mixture of isopropyl alcohol and its distillate in a ratio of 1 to 1.
an intermediate product in the synthesis of natural phytohormone of epibrassinolide with high growth promoting activity (1-3)
which is an intermediate substance to obtain (22R, 23R)-3- acetoxy-22,23-isopropylidenedioxy-24-metalholic-5 - ene of formula II;
Compound II is a well-known synthetic precursor hormone brassinolide) III, which is found in very low concentrations in some plants and is the most active of the new class of natural hormones - steroids, and therefore can be used in agriculture as a growth promoter, plant /1/
cholesterol (Chs)< / BR>testosterone (TS)which can be used as source reagents for solid-phase synthesis of steroid derivatives of oligonucleotides and their analogues
FIELD: organic chemistry, steroids, medicine, pharmacy.
SUBSTANCE: invention relates to 3-methylene-steroid derivative of the general formula (1):
wherein R1 means hydrogen atom (H), or in common with R3 it forms β-epoxide; or R1 is absent in the presence of 5-10-double bond; R2 means (C1-C5)-alkyl; R3 means βH, βCH3 or in common with R1 it forms β-epoxide; either R3 is absent in the presence of 5-10-double bond; R4 means hydrogen atom, lower alkyl; Y represents [H, H], [OH, H], [OH, (C2-C5)-alkenyl], [OH, (C2-C5)-alkynyl] or (C1-C6)-alkylidene, or =NOR5 wherein R5 means hydrogen atom (H), lower alkyl; dotted lines represent optional double bond. Compound can relate also to its prodrug used for treatment of arthritis and/or autoimmune diseases.
EFFECT: valuable medicinal properties of compounds, improved method for treatment.
38 cl, 1 tbl, 18 ex
FIELD: organic chemistry, medicine, pharmacy.
SUBSTANCE: invention represents new derivatives of 17,20-dihydrofusidic acid of the formula (Ia)
wherein Q1 and Q2 are similar or different and mean -CO-, -CHOH-, -CHRO- wherein R means (C1-C4)-alkyl; Q3 means -CH2-; Y means hydrogen atom (H); A means -O- or -S-; R1 means (C1-C4)-alkyl, (C2-C4)-olefin, (C1-C6)-acyl, (C3-C7)-cycloalkylcarbonyl, benzoyl. These derivatives are used in pharmaceutical compositions for treatment of infectious diseases, in particular, in composition for topical applying for treatment of infectious diseases of skin and eyes.
EFFECT: valuable medicinal properties of compounds.
22 cl, 7 tbl, 41 ex
FIELD: organic chemistry, chemistry of steroids.
SUBSTANCE: invention relates to a new method for synthesis of 6β-formyl-B-norcholestane-3β,5β-diol of the formula (I): by constricting six-membered B-ring of cholesterol. Method involves photooxidation of cholesterol with air oxygen at irradiation by visible light in the presence of porphyrine photosensibilizing agent immobilized on low-molecular fraction of copolymer of tetrafluoroethylene and perfluoro-3,6-dioxo-5-methyl-6-sulfonylfluoride octene-1 in the mass ratio porphyrine photosensibilizing agent : cholesterol = 1:(12-15). As porphyrine photosensibilizing agent 5,10,15,20-tetraphenylporphyrine can be used. Method shows technological simplicity, it doesn't require rigid conditions and provides the high yield of the end product.
EFFECT: improved preparing method.
2 cl, 3 ex
FIELD: medicinal industry, sterols.
SUBSTANCE: invention relates, in particular, to the improved method for producing sterols - lanosterol and cholesterol from wooly fat that can be used in preparing medicinal and cosmetic preparations. Method is carried out by alkaline hydrolysis of raw, extraction of unsaponifiable substances, removal of solvent and successive isolation of lanosterol and cholesterol. Alkaline hydrolysis of raw is carried out with a mixture of ethanol, sodium hydroxide, pyrogallol and water at temperature 70°C for 4 h at stirring in the following ratio of components: raw : ethanol : sodium hydroxide : pyrogallol : water = 100.0:(300.0-350.0):(30.0-35.0):(0.01-0.05):(7.5-12.0), respectively, with the indicated mixture with addition of toluene in the following ratio: raw : ethanol : sodium hydroxide : pyrogallol : toluene : water = 100.0:(220.0-255.0):(30.0-38.0):(0.05-0.12):(100.0-137.0):(2.5-7.0), respectively, and lanosterol is isolated by precipitation from mixture of methylene chloride and ethanol in the ratio = 1:1. Before removal of solvent unsaponifiable substances are extracted at temperature 50°C for 2-3 h at stirring. Invention provides increasing yield of the end product, enhancing qualitative indices and reducing cost of production.
EFFECT: improved producing method.
2 cl, 3 ex
SUBSTANCE: polyaminosteroid branched derivatives of general formula I are described, where R1 is saturated or unsaturated C2-C10alkyl (conjugated or branched) or methyl, R2 is COOH or branched polyamine fragments, R3 is H, OR19, where R19 is H or C1-6acyl, R4 is H, R5 is H, CH3, R6 is H, CH3, R7=R8=R9=H, R10 is H, CH3, R11 is OH,-OSO3, - O-acyl, -(Z)n-(NR-Z)p-N(R)2, Z is linear hydrocarbon diradical, n=0, 1, p=1, R-H, C1-6alkyl, C1-6aminoalkyl, possibly substituted by C1-6alkyl, R12=R13=R15=H, R16 is H, OH, R17 is H, R18 is H, CH3, possible double bond. Compounds possess bactericidal activity and can be used for prevention of bacterial infections.
EFFECT: production of polyaminosteroid derivatives, possessing bactericidal activity which can be used for prevention of bacterial infections.
27 cl, 31 ex, 1 tbl, 2 dwg
SUBSTANCE: claimed invention describes paroxetine cholate or salt of cholic acid derivative and composition, which contains paroxetine and cholic acid or its derivative. Also described is pharmaceutical composition for treatment of depressive states, containing paroxetine salt or composition. Pharmaceutical composition can be part of peroral medication, swallowed without water, on form of disintegrating in mouth paroxetine tablet.
EFFECT: obtaining paroxetine cholate or salt of cholic acid derivative, which can be used in pharmacology.
19 cl, 38 ex, 12 tbl
SUBSTANCE: invention refers to synthesis of biologically active substances, in particular specifically, to improved method of producing 2,3-monoacetonide 20-hydroxyecdysone of formula found in very small amounts in some plants, e.g. Rhaponticum carthamoides. Method is implemented by interaction of 20- hydroxyecdysone (1.0 g, 2.08 mmole) and acetone with phosphomolybdic acid (PMA) added. As suspension is effected by mother compound in PMA acetone (0.3 g, 0.16 mmole), after 5 min homogenisation of reaction mixture is observed to be steamed by neutralisation with 0.1% sodium hydrocarbonate solution with following ethyl acetate and chromatography extraction of the end product, thus resulting in isolation of the end 2,3-monoacetonide 20- hydroxyecdysone of 32% yield.
EFFECT: method is highly selective and single-stage.
2 cl, 1 ex