378 results about "Oxazolidine" patented technology

An antibacterial 3,5-substituted oxazolidione derivative and its salt with strong activity to resist gram-position bacteria, their preparing process, their application in preparing antibacterial agents and the antibacterial medicine containing them as active components are disclosed.

The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (4R,5R)-3-acetyl-2,2-dimethyl-4-hydroxymethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine; and (4S,5R)-3-acetyl-2,2-dimethyl-4-fluoromethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine.

The invention relates to a ginger shampoo capable of protecting hairs and preventing losing hairs, wherein the ingredient of the shampoo comprises A group, B group and C group; A group: 38.24% of deionized water, 0.05% of EDTA (Ethylene Diamine Tetraacetic Acid) 4 sodium, 0.2% of hydroxypropyl three methyl ammonium chloride hydroxypropyl guar gum, 0.2% of hydroxypropyl guar gum, 53% of sodium lauryl ether sulfate, 2% of coconut oil amide diethanol amine and 1% of glycerol distearate; B group: 0.15% of anhydrous citric acid, 231.34% of simethicone, 0.2% of (propanediol and water) chamomile extraction, 0.3% of poly methoxy-double oxazolidine, 0.40% of essence and 5% of ginger juice; and C group: 0.73% of potassium chloride and 2.19% of deionized water. The shampoo comprising the ginger has the effects for cleaning scalp, removing scurf, preventing and cure alopecia, etc; and the shampoo can promote blood circulation of the head and strengthen hair roots.

The invention relates to a method for preparing an oxazolidinone compound and an intermediate thereof. Specifically, two fragments are coupled to prepare the oxazolidinone compound by virtue of Suzuki reaction. The method is simple in process, short in reaction time and high in yield and is suitable for industrial production. Furthermore, the method for preparing the intermediate of the oxazolidinone compound has the advantages of simplicity in operation, high yield and low cost.

The present invention relates to formulations of asphaltenes' inhibitor-dispersant additives based on oxazolidine derived from polyalkyl or polyalkenyl N-hydroxyalkyl succinimides. Said formulations can contain inert organic solvents, preferably including: toluene, mixtures of xylene, o-xylene, p-xylene, kerosene, turbo-fuel; or inert hydrocarbon solvents having boiling points within the range of gasoline and diesel; or inert hydrocarbon or organic solvents having a boiling point within a range from 75 to 300° C. The ratio in weight of inert organic solvents to additive that prevents and controls the precipitation and deposition of asphaltenes ranges from 1:9 to 9:1, preferably from 1:3 to 3:1.

The invention discloses a preparation method of an intermediate 3-[(2R,5S)-5-(4-fluorophenyl)-2-[(S)-(4-fluorophenylamino)(4-R-oxophenyl)methyl]-5-hydroxyvaleryl]-(4S)-phenyl-2-oxazolidinone (represented by general formula I) for synthesizing ezetimibe. The method is characterized in that the intermediate is prepared by using (4S)-3-[(5S)-5-(4-fluorophenyl)-5-hydroxyvaleryl]-4-phenyl-1,3-oxazolidin-2-one and 4-R-oxophenylmethylene-4-fluoroaniline as initial raw materials. The method has the advantages of no need of an expensive reagent, simple operation, high product yield, high product purity and the like, and is suitable for industrialized production.

The invention discloses a method for preparing hapten, antigen and antibody of 5-methylmorpholine-3-amino-2-oxazolidone derivatives. The hapten obtained by designing and preparing the 5-methylmorpholine-3-amino-2-oxazolidone derivatives is similar to counterparts of the 5-methylmorpholine-3-amino-2-oxazolidone derivatives in molecular structure, spatial chemistry and electron distribution. The linking arm in the hapten structure is not easy to induce and generate 'arm antibody', and the organism is easier to identify as a saturate carbon chain of a certain length is used; the antigen which is prepared by hapten cross coupling carrier protein ensures the organism to produce the antibody of high tilter and good specificity in accordance with the 5-methylmorpholine-3-amino-2-oxazolidone derivatives; and the antibody is used for detecting the residue of 5-methylmorpholine-3-amino-2-oxazolidone in animal source food with quick response and stable result.

The invention discloses a blood sample collecting device. The collecting device comprises a collecting tube, wherein an orifice of the collecting tube is provided with a sealing rubber plug, the outside of the rubber plug is provided with a protective cap, the collecting tube is filled with additives, the additives are composed of a blood anticoagulation, a hemocyte nucleic acid stabilizing agent, a blood plasma nucleic acid stabilizing agent, and a pH buffer solution; the blood anticoagulation is one or more of oxalate, heparinate and citrate, the pH buffer solution is one of glycine-sodium hydroxide-hydrochloric acid buffer solution; the hemocyte nucleic acid stabilizing agent is one or more of allantoin, 5,5-dimethyl hydantoin and oxazolidine; the blood plasma nucleic acid stabilizing agent is N-acetic acid azomethine, N-(3-acetic acid-amylamine)azomethine. The blood sample collecting device simultaneously contains the hemocyte nucleic acid stabilizing agent and the blood plasma nucleic acid stabilizing agent, and does not contain free aldehyde material, so that the blood sample can be stored in long term at normal temperature, and the free nucleic acid level of the blood sample can be stabilized, and the completeness of the free nucleic acid can be maintained.

The invention discloses a preparation method for tedizolid as shown in a formula IV. According to the method, tedizolid is prepared through chemical combination of a compound as shown in a formula I and a compound as shown in a formula II via a coupling reaction; and tedizolid phosphate with medical purposes can be prepared by subjecting the obtained tedizolid to esterification by phosphate. The preparation method has the advantages of milder reaction conditions, a few produced impurities and simple post-treatment. According to the invention, the reaction mechanism of Suzuki-Miyaura coupling is employed to connect boric acid as shown in the formula I and derivatives thereof with the compound as shown in the formula II, so reaction selectivity is high, a few impurities are produced, and a synthetic ratio is more than 90%; and oxazolidinone borate is used to react with tetrazole, so conditions are milder, and the generation rate of impurities is lower.

The invention relates to a medicine producing field, specifically, to an improved producing method of antibacterial medicine nifuratel. The method makes use of thiourea as initial material to produce nifuratel. The improvement is that it is no longer to use methyl mercaptan or methomyl in the known method while producing the intermediate 2-(methylthiomethyl)hydropropane. Furthermore, the invention is no longer to use metal natrium in the known method when the 3-methylthio-2-hydroxy-propylhydrazine and diethyl carbonate are heated to produce N-amido-5-methylthiomethyl-2-oxazolidone in the existance of alkali. All of the improvements largely improve the preparation of the nifuratel, especially for the production condition in a large scale, reduce the environment pollution and benefit to ensure the production safety.

The invention provides a production method of a polyoxazolidone laminated board, comprising the following steps: reacting diisocyanate with epoxide resin by taking imidazole compounds as catalyst for producing polyoxazolidon resin during the gradual rise of temperature; and then producing the polyoxazolidone laminated board by using the polyoxazolidon resin. The polyoxazolidone laminated board the end of which is sealed with isocyanate has better mechanical strength, favorable heat resistance and high glass transition temperature above 155 DEG C; and when in use at 180 DEG C or 200 DEG C, the mechanical property and electrical propertye of the polyoxazolidone laminated board are over 70 percent.

The invention relates to a synthetic method of cabazitaxel, which comprises the following steps: taking a compound 10-deacetylbaccatin III as a starting raw material and reacting with a protective agent to carry out selective protection on 7 and 10 hydroxyls; then carrying out selective protection on 13 hydroxyls of the compound, removing 7 and 10 protection radicals and carrying out methylation reaction; removing 13 protection radicals and carrying out condensation reaction with an oxazolidine carboxylic acid side chain; and removing and protecting a condensation product to obtain the cabazitaxel. The synthetic method has the beneficial effects that the proper protection radicals and a removal and protection method are selected, the oxazolidine carboxylic acid side chain is finally connected, and the synthetic method has the characteristics of low production cost, high yield, mild reaction conditions and simplicity in operation and is particularly suitable for industrial production.

A process for the preparation of taxanes comprising

wherein R is a tert. butoxycarbonyl or benzoyl group; PMP is p-methoxyphenyl group; G₁ is acetyl group; G₂ is haloacetyl group comprising

• • a) protecting the C-7 hydroxyl group of 10-deacetylbaccatin III with haloacetyl chlorides and then acetylating the C-10 hydroxyl group with acetyl chloride to obtain a protected 10-deacetylbaccatin III (1);
  • b) subjecting the protected 10-deacetylbaccatin III (1) to coupling with an oxazolidine-5-caboxylic acid of formula 2

wherein R is tert. butoxycarbonyl or benzoyl; PMP is p-methoxyphenyl group in the presence of a condensation agent and an activating agent to obtain C-13 esters of formula 3;

c) treating the coupled products 3 with weak acidic medium to open the oxazolidine ring to obtain intermediates of formula 4;

wherein R is a tert. butoxycarbonyl or benzoyl group; G₁ is acetyl group; G₂ is haloacetyl group

d) subjecting the intermediates of compound 4 to selective deprotection of haloacyl group in the presence of acetyl group under mild alkaline condition at −20 to +40° C. for 6-24 h in the presence of ammonia or aliphatic amine or aromatic amines or their combination to obtain paclitaxel or docetaxel.

The invention provides a preparation method of diethyl N,N-bis(2- hydroxyethyl) aminomethylphosphonate, comprising the following steps: (1) carrying out depolymerization on paraformaldehyde; (2) carrying out ring formation on formaldehyde and diethanol amine to prepare 3-(2- hydroxyethyl)-1,3-oxazolidine; (3) reacting 3-(2- hydroxyethyl)-1,3-oxazolidine with diethyl phosphite in the presence of anhydrous Lewis acid catalysts; and (4) filtering and recovering the catalysts to obtain a yellow transparent liquid product. The overall yield of the whole process reaches more than 99 %, and the content of diethyl N,N-bis(2- hydroxyethyl) aminomethylphosphonate in the product is 94 %-96 %. The preparation method disclosed in the invention is simple and efficient, has the advantages of high product yield, high content of effective components in the product, reduction of temperature in dehydration process, shortening of time, and low energy consumption, reduces the water content of the final product to 0.1-0.2 %, and reduces the dosage of the catalysts by 20-50%. The preparation method is suitable for large-scale industrial production.

The leather tanning agent having no chrome or having little chrome is made up by using amine material containing carboxymethyl group and aliphatic aldehyde compound through the processes of N-carboxymethylation reaction and ring-closing reaction. In addition to oxazolidine naphthenicbase its molecular structure also contains several functional groups of aldehyde group, carboxyl group, hydroxyl group and quaternary amino-group. Said main tanning agent can be combined with vegetable tannin extract, also can be combined with chrome for tanning leather, and can raise wet and thermal stabilizing of the finished leather and reduce dose of chrome by 30-40%.

The invention belongs to the field of drug synthesis and provides a novel method for synthetizing nifuratel. The synthesis method of the nifuratel disclosed by the invention innovatively adopts a post-treatment method of 'ethanol with water' to obtain a midbody 3-methyl mercapto-2-hydroxy propyl hydrazine (A1); high-vacuum reduced pressure distillation of the midbody 3-methyl mercapto-2-hydroxy propyl hydrazine (A1) is avoided; the nifuratel is prepared by a 'one-pot' method; preparation of a midbody N-amino-5-methylthiomethyl-2-oxazolidinone (A2) and post-treatment operation of 5-nitro-furfural (B1) are simplified; the purity of the obtained nifuratel product is higher than 99.8%; and the yield is higher than 30%. The synthesis method of nifuratel disclosed by the invention is simple, convenient and easy to control; the post-treatment operation is simple and feasible; industrialized production is facilitated; the used material is available in China; the pollution on the environment is small; and the material is cheap and easily available.

The invention discloses novel oxazolidine, a preparation method, application, and mono-component polyurethane waterproof paint. The novel oxazolidine is named as 4-mehtyl-3-(2-phenylcarbinol)-1,3-oxazolidine. The novel oxazolidine is used as a latent curing agent of the mono-component polyurethane waterproof paint. During the production process of the waterproof paint, the novel oxazolidine is added into the raw materials, one naked hydroxy group of the novel oxazolidine will react with the polyurethane prepolymer formed by the raw materials, thus the novel oxazolidine is grafted to the polyurethane prepolymer, and the novel oxazolidine (latent curing agent) can be more evenly dispersed in the waterproof paint. If the waterproof paint is stored for a long time, the grafted novel oxazolidine will be dissolved out continuously, the stability of the waterproof paint is improved, the latent curing effect is improved, and avoided is the phenomenon that the latent curing agent is precipitated from the mono-component polyurethane waterproof paint or the latent curing agent aggregates in the waterproof paint. After the waterproof paint is used, the quality of the film formed by the waterproof paint is improved.

The invention relates to a coating, in particular to a spraying polyurea elastic coating. The spraying polyurea elastic coating is composed of a component A and a component B. The component A is prepared from, by mass, 55% to 65% of polyisocyanate and 35% to 45% of polyether polyol. The component B is prepared from, by mass, 45% to 55% of amine-terminated polyether, 34% to 45% of amine chain extenders, 5% to 10% of polyfunctionality oxazolidine, 0.5% to 1% of defoaming agents and 0.5% to 1% of dispersing agents. According to the spraying polyurea elastic coating, as the polyfunctionality oxazolidine is added into the dewatered amine-terminated polyether, hydroxyl terminated polyether and the amine chain extenders and can be firstly reacted with a small amount of moisture generated in the use process, the transport process and the use process to generate amino-and-hydroxyl-containing open-loop compounds, then the compounds are reacted with isocyanate groups of polyurea curing agents to be cured, carbon dioxide gas is not generated in the whole curing process, and the defect that a paint film is bubbly is well overcome.

The present invention is directed to processes for the preparation of N-(3R, 3aS, 6aR)-hexahydrofuro[2,3-b]furan-3-yl-oxycarbonyl-, (4S,5R)-4-[4-(2-methylthiazolo-4-methyloxy)-benzyl]-5-i-butyl-[(3,4-methylenedioxyphenyl)sulfonyl]-aminomethyl-2,2-dimethyl-oxazolidine.