Application of cyclohexanol derivatives as antimicrobial active compounds
SUBSTANCE: application of at least one cyclohexanol derivative of the formula (Ia)
as an antimicrobial active compound is proposed, application of the same compounds as an anti-acne, antiperspirant, antiperspirant or deodorant active compound, a drug with antimicrobial action comprising at least one cyclohexanol derivative of formula (Ia) and/or (Ib), with exception of 2-hydroxycyclohexane-1-carboxylic acid, individual cyclohexanol derivatives of formula (Ia) and/or (Ib).
EFFECT: bacteriostatic action of compounds against Staphylococcus epidermidis, suppression of growth and reproduction of other gram-positive and gram-negative bacteria, yeast, fungi or viruses.
15 cl, 16 ex
SUBSTANCE: purification of pravastatin is carried out from stereoisomer 6-epipravastatin. The culture liquid is centrifuged with a content of 6-epipravastatin 7% by weight of pravastatin for separation of mycelium. The native solution is prepared having pH 6.6. Purification of the native solution is carried out by filtration through a layer of basic alumina with pH 10, having activity corresponding to 8% of moisture. Alumina is taken in an amount of 25:1 relative to the amount of pravastatin in the native solution. Pravastatin is extracted by the organic solvent. Final purification of pravastatin is carried out through obtaining of intermediate ammonium salt using 25% aqueous ammonia solution and subsequent conversion to its sodium salt.
EFFECT: invention enables to carry out purification of pravastatin according to the pharmaceutical requirements to quality.
2 cl, 2 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: present invention relates to methods of synthesis and to intermediate products of compounds of formula (XVII) and salts thereof.
EFFECT: preparing the hepatitis C virus protease inhibitor.
32 cl, 13 ex
SUBSTANCE: invention relates to a stereoselective method of producing norbornadiene-based stressed skeleton carbocyclic compounds. The method is characterised by that it involves codimerisation of norbornadiene with acrylic esters. The catalyst used is a bis(allyl)nickel-based single-component system.
EFFECT: use of the present method increases stereoselectivity of the codimerisation reaction and increases product output.
1 cl, 5 ex, 1 tbl
SUBSTANCE: present invention relates to methods for synthesis of bicyclo[3.1.0]hexane derivatives, used as mGIuR agonists having formulae ,
, where R1 and R2 represent hydrogen, X is a halogen, R3 is -O-Ra , Ra is C1-10alkyl, and R4 is (1) hydrogen or (2) Si-(R9)(R10)(R11), where each of R9, R10 and R11 is C1-10alkyl, as well as intermediate compounds obtained when realising the said methods.
EFFECT: design of an efficient method for synthesis of bicyclo[3,1,0]hexane derivatives.
26 cl, 17 ex, 1 tbl
SUBSTANCE: invention is related to the field of organic chemistry, in particular, to method for production of methyl ethers of 2-thiophen carbonic acid intended for use in synthesis of optical whiteners, dyes for cotton, wool, artificial fibers, medical preparations, and also as additive to oils or hydraulic liquids. Substance of the method consists in thiophen interaction with methanol in presence of carbon tetrachloride under action of catalysts - oxo-bis-(2,4-pentanodionato)vanadium VO(acac)2 or tris (2,4-pentanodionato)iron Fe(acac)3, or molybdenum hexacarbonyl Mo(CO)6 at the temperature of 130-170°C for 3-6 hours at the following mole ratio - catalyst:thiophen:CCl4:methanol equal to 1:100:200-300:200-300.
EFFECT: suggested method makes it possible to produce target product with yield of 63-85%, using simplified technology.
1 tbl, 14 ex
< / BR>where R is the ester residue, split in neutral or acid medium and which WITH1-18the alkyl possibly substituted with halogen or benzyl radical, possibly substituted on the tops of the aromatic ring by one or more halogen atoms, or a radical of formula (a) -(g),
< / BR>where R2Is h or methyl;
R4- CN, N.;
R5- fluorine, chlorine, bromine or hydrogen;
R6, R7, R8, R9is hydrogen or methyl;
S/1 symbolizes tetrahedrite
SUBSTANCE: invention relates to organic chemistry and specifically to an improved method of producing 16(S)-dihydrosteviol of formula (I), which can be used in synthesis of novel ent-kaurane diterpenoid derivatives. (I). The method involves mixing glucoside (stevioside) of a Stevia rebaudiana plant or a mixture of glucosides of said plant (sweetener) with 100-fold excess hydroxylamine in dimethyl formamide, adding 70-fold excess ethyl acetate at room temperature and then heating the reaction mixture to 100°C for 3 hours, concentrating said reaction mixture, dissolving the residue in water acidified to pH 1-3, boiling the aqueous solution for 2 hours, extracting the product with diethyl ether, drying, distilling the solvent and recystallising the end product from ethyl acetate.
EFFECT: method ensures high output and does not require use of a catalyst.
1 cl, 2 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to improve method for production of trans-alkyl-substituted cyclohexanecarboxylic acids of general formula 1 , wherein R is C1-C10-alkyl and trans-4-(C1-C10-alkyl)cyclohexyl radical, by hydration of respective 4-alkyl-substituted benzoic acids. In aqueous-alkali solution at elevated temperature and elevated hydrogen pressure of 0.5-15 MPa in presence of catalyst followed by isomerization at 200-400°C and isolation of reaction products by mixture acidifying. As catalyst ruthenium-nickel catalyst on carbon carrier is used, wherein catalyst contains 5 mass % of metal calculated as total catalyst mass and Ni/Ru mass ratio is (0.01-1.5):(8.5-9.99). Process is carried out at 20-150°C for 0.25-1 h, and isomerization is carried out in inert gas atmosphere in several steps after mixture filtration to separate catalyst. Compounds of present invention represent value products in production of liquid crystal materials and biologically active materials.
EFFECT: accelerated process with reduced cost and increased effectiveness.
1 tbl, 9 ex
SUBSTANCE: invention relates to improved method of obtaining terephthalic acid, including a) interaction of 2,5-furanedicarboxylic acid, 2,5-furane dicarboxilate or their mixture with ethylene in presence of solvent with formation of bicyclic ether at temperature in the interval from 100°C to 250°C and pressure in the interval from approximately 10 lb/sq.inch (about 68.95 kPa) to 2000 lb/sq.inch (about 13.79 MPa) and b) dehydration of bicyclic ether.
EFFECT: method ensures effective obtaining terephthalic acid with reduced amount of admixtures, coloured admixtures and carbon oxides, which are formed in industry in case of liquid-phase oxidation of methyl-substituted benzoles, or without said admixtures at all.
16 cl, 1 tbl, 2 ex
SUBSTANCE: invention relates to method of reverse splitting of Michael adducts, contained in fluid F with weight part ≥ 10 wt %, counted per liquid F weight, which were formed in the process of obtaining acrylic acid or its esters, in installation of reverse splitting, which includes, at least, one pump P, separation column C, which from bottom to top consists of bottom part, separating part, which is adjacent to bottom part and contains internal devices with separating effect, and head part, which follows it, in which pressure in gaseous phase decreases from bottom to top, as well as indirect heat exchanger with circulation of heat carrier UW, which has, at least, one secondary volume and, at least, one primary volume, separated from said, at least, one secondary volume by means of real separating wall D, in which fluid F with supply temperature TZ is continuously introduced into separation column C in point of supply I, which is located in said separation column C above the lowest internal device with separating effect; expenditure flow
EFFECT: improvement of method.
14 cl, 9 dwg
SUBSTANCE: invention relates to use of a loop reactor, having gas and liquid recirculation systems which are connected through the combining nozzle of a reactor ejector, in which gas and liquid circulate in a parallel stream, and the combining nozzle is formed such that, mixing power of at least 50 W/l of the liquid phase can be imparted into the liquid phase, and in which the gas recirculation system has a device for continuous removal of gaseous HCl, formed during the process, from the recirculating gas and returning unreacted hydrogen gas into the mixing nozzle of the ejector of the loop reactor, for selective catalytic hydrogenation of the liquid dichloroacetic acid to monochloroacetic acid.
EFFECT: invention relates to a continuous or periodic method of producing monochloroacetic acid containing less than 0,1 wt % dichloroacetic acid from a liquid mixture of chloroacetic acid, containing monochloroacetic acid and dichloroacetic acid, in which the mixture is mixed with a suspended hydrogenation catalyst and mixed with hydrogen gas, wherein the formed mixture reacts in said loop reactor.
15 cl, 1 dwg, 4 ex
SUBSTANCE: invention relates to an improved method for synthesis of alkyl(meth)acrylates which are used in synthesis of polymers and copolymers with other polymerisable compounds, involving a step for re-esterification of alkyl ester of α-hydroxycarboxylic acid with (meth)acrylic acid, accompanied by formation of alkyl(meth)acrylates and α-hydroxycarboxylic acid, and a step for dehydration of α-hydroxycarboxylic acid, accompanied by formation of (meth)acrylic acid.
EFFECT: method enables to obtain a product with high selectivity.
22 cl, 2 tbl, 2 dwg, 38 ex
FIELD: organic chemistry.
SUBSTANCE: invention relates to new method for production of m- or p-substituted α-arylalkanecarboxylic acids of general formula I
from respective α-hydroxylated derivatives using inexpensive reagents and without converting of any reducible groups such as ester or ketone ones in side chains. In formula R is hydrogen, C1-C6-alkyl; R1 is hydrogen, linear or branched C1-C6-alkyl, phenyl, p-nitrophenyl, alkali or earth-alkali cation or cation of pharmaceutically acceptable ammonia salt: A is C1-C4-alkyl, aryl, optionally substituted with one or more alkyl, hydroxy, etc., aryloxy, arylcarbonyl; A is in m- or p-sites; P - linear or branched C1-C6-flkyl, phenyl, nitrophenyl. Claimed method includes the next steps: a) converting of compounds of formula II to compound of formula III either by reaction of II with compound of formula in presence of organic or inorganic base or by reaction of II with thiophene of formula and followed by reaction of obtained product with HNRaRb, wherein Ra andRb are as defined above; b) thermal rearrangement of III to form IIIb ; c) catalytic dehydration of IIIb to form IIIc ; and d) optional hydrolysis of IIIc to obtain target compound of formula I. Also are disclosed new compounds of formulae III and IIIb.
EFFECT: new α-arylalkanecarboxylic acids and intermediates thereof.
6 cl, 5 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: invention relates to pharmaceutical industry, namely represents composition, which contains mixture of particles of hydrophobic silicon dioxide aerogel, which have specific area of surface per weight unit (Sw) in range from 500 to 1500 m2/g and size, expressed in form of volume mean diameter (D[0.5]), in range from 1 to 1500 mcm, and at least one first linear silicone oil, which has viscosity higher than 50 mm2/s, and at least second and third linear silicone oils, and each of them has viscosity lower than or equal 50 mm2/s.
EFFECT: mixture of particles of silicon dioxide aerogel and linear oils provides possibility of obtaining compositions, which provide comfort and smoothness of skin after application and have dullness and "soft focus"-adding properties.
23 cl, 8 ex
FIELD: medicine, pharmaceutics.
SUBSTANCE: group of inventions refers to an antiseptic pharmaceutical composition applicable for oral hygiene and treatment of microbial oral diseases, to a method for producing and using it. The composition contains from 0.05 to 0.3 wt % of hydrogen peroxide or its equivalent amount in the form of carbamide peroxide, from 0.001 to 0.03 wt % of eugenol, from 0.001 to 0.01 wt % of camphor, from 0.001 to 0.5 wt % of a salt of zinc or other heavy metals, such as silver, mercury, copper or a mixture thereof; from 1 to 1.2 wt % of sodium fluoride; from 2% to 7 wt % of xylitol, from 0.002 to 0.05 wt % of cetylpyridinium chloride and excipients in an amount sufficient to reduce the composition to 100%. The composition possesses a wide spectrum of action. What is also presented is a method for producing the composition and using it for producing a therapeutic agent effective for odour elimination, suppression and relief of an oral inflammation, dental tartar inhibition; for treating oral diseases; for rinsing and treating orthodontic damages; for preventing oral diseases during orthodontic treatment after oral operations and in the patients using fixed and temporary dentures; for relieving, treating or preventing oral diseases in different categories of patients, such as the patients receiving radiation therapy or chemotherapy, hospital patients and terminally ill patients, patients suffering from eating disorders, endocrine, haematological, cardiovascular and psychosomatic disorders, and besides physically or mentally deprived patients, patients with genetic or inherited changes.
EFFECT: preparing the antiseptic pharmaceutical composition.
22 cl, 3 ex