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64 results about "Tropine" patented technology

Tropine is a derivative of tropane containing a hydroxyl group at the third carbon. It is also called 3-tropanol.

Method for preparing tiotropium bromide

The invention relates to the application of microwave and ultrasonic technologies in synthesizing tiotropium bromide anhydride, in particular to a method for preparing the refined product of a finished product, namely, tiotropium bromide anhydride through crystallization and recrystallization processes by using a crude product of tiotropium bromide prepared through bromization reaction after hydrolytic reaction of scopolamine hydrobromide under microwave function, substitution and coupling reaction of bromothiophene, magnesium, and oxalic acid dimethyl ester under the microwave function, and condensation reaction of scopine and thiophen methyl glycollate under the microwave function. Using the invention to prepare tiotropium bromide anhydride, not only the reaction time is short, the side reaction is less, and the yield rate is high in the room temperature condition, but also the product quality is stable, controllable, safe and effective.
Owner:HONGYI SCI & TECH CO LTD NANCHANG

Synthesis method of ipratropium bromide

The invention provides a synthesis method of ipratropium bromide. The method comprises the steps of (1) carrying out acetyl protection reaction on tropic acid as a raw material to obtain a compound 1; (2) carrying out chloroformylation reaction on the compound 1 to obtain a compound 2; (3) dissolving isopropyl tropine and organic acid into dichloromethane, adding obtained solution to the compound 2 and carrying out acylation reaction to obtain a compound 3; (4) carrying out alcoholysis reaction on the compound 3 to obtain a compound 4; and (5) carrying out bromine methylation reaction on the compound 4 to obtain the ipratropium bromide. The synthesis method of the ipratropium bromide is simple and raw materials are easily available, the operation is simple and stable, various steps are mild in reaction conditions, reaction products of various steps are easy to purify, the purity of the obtained ipratropium bromide product reaches over 97% and the synthesis method is suitable for industrial production of ipratropium bromide.
Owner:WUHAN LEADPHARM TECH CO LTD

New application of benzo [C] phenanthridine and protopine in producing overriding resistant bacterium medicament

The invention relates to a new application of benzo [C] phenanthridine as formula I and original tropine alkaloid for preparing anti-drug-resistant bacterial drug, wherein R1-R10, R12-R15 are hydrogen and hydroxyl groups, cycloalkyl or alkyl groups with 1-12 carbon atoms, alkox or acyloxy groups, benzyloxy, chlorine or other halide atoms, amido, methylol, aldehydo, aldehydo, acetonyl, carboxy group, mesyloxy, 4-methyl-benzene sulfonyl oxygen group, aryl sulfonyl oxygen group, biphenyl phosphine acyloxy and -OCONH2, R11 is hydrogen, methyl or oxygen atom, R5 and R6 (or R15 of the formula I), R14 and R15 are formed with double bonds, R12 or R13 and nearby N atoms are formed with double bonds, N atom can be tertiary or quaternary N type, the substituents of nearby carbons of R1-R10 can have dioxolane structure. The inventive alkaloid can effectively restrain and kill drug-resistant bacterials as MRSA and ESBLs.
Owner:成都军区昆明总医院

Method for synthesizing SAPO-35 molecular sieve by using bi-template

The invention discloses a method for synthesizing an SAPO-35 molecular sieve by a two-mode agent, which is characterized in that the method comprises the steps of mixing aluminum source, phosphorus source, silicon source and an organic template to glue at the temperature of room temperature to 100 DEG C and preparing into the reaction mixture with the molar ratio components of a1R1+a2R2: Al2O3: bP2O5: cSiO2: dH2O, wherein R1 and R2 are the organic templates, the value of a1 is 0.5-1.8, the value of a2 is 0.1-1.0, the value of b is 0.5-1.5, the value of c is 0.05-2.5, and the value of d is 10-150; the reaction mixture undergoes hydrothermal crystallization for 0.5-500 hours at the temperature of 150-250 DEG C and the crystallization product is recovered. The R1 is hexamethylene imine, and the R2 is any of cyclohexane, piperidine, tropine, diethylamine and triethylamine. The method provided by the invention can synthesize the high-crystallinity SAPO-35 molecular sieve in a relatively wide silica content range. The SAPO-35 molecular sieve synthesized by the method of the invention is applicable to the hydrocarbon conversion technology. Applied to the olefin preparation reaction by methanol dehydration, the molecular sieve has very low alkane selectivity and high product yield of ethylene and propylene.
Owner:CHINA PETROLEUM & CHEM CORP +1

Method for preparing 2-hydroxyl-2,2-diphenyl acetic acid-3alpha-(8-azabicyclo[3,2,1]-3-octyl ester

The invention discloses a method for preparing 2-hydroxyl-2,2-diphenyl acetic acid-3alpha-(8-azabicyclo[3,2,1]-3-octyl ester which is a key intermediate of trospium chloride of an anticholinergic agent. The method comprises the following steps that: firstly, 2-hydroxyl-2,2-diphenyl acetic acid serving as a raw material is mixed with carbonyl imidazole for activation of acyl radicals; secondly, theresulting product reacts with tropine alcohol to form 2-hydroxyl-2,2-diphenyl acetic acid tropine ester; and finally, the resulting product of the previous step undergoes N formylation and acidulation reaction to obtain the 2-hydroxyl-2,2-diphenyl acetic acid-3alpha-(8-azabicyclo[3,2,1]-3-octyl ester. The method has the advantages of mild reaction conditions, little pollution and easy realizationof industrialized production.
Owner:北京迈劲医药科技有限公司

Method for testing tropine alcohol of residual intermediate product in synthesizing Troipisetron

A method for detecting residual intermediate of tropaic alcohol in tropisetron synthesis includes preparing test solution and control solution , dropping them separately on the same silica gel G thin layer plate , using acetone ¿C ammonia water as developing agent to carry out thin layer chromatography determination, developing chromatographic cylinder, using developer of bismuth potassium iodide solution with assistance of sodium nitride solution to develop color and checking colour developed result.
Owner:QINGDAO PURUISEN MEDICINE SCI & TECH CO LTD

Analytical method for measuring raw medicine content of thiohydroxylamine tropine by non-aqueous titrimetry

The invention discloses an analysis method for determining the hydroxamamide tropine raw drug content through a non-aqueous titration method and relates to the hydroxamamide tropine raw drug quality control technology field. The method for determining the content of hydroxamamide tropine is provided, the process of which is as follows: glacial acetic acid-acetic oxide is used as a solvent for the quantitative dissolution of the hydroxamamide tropine. Then, perrchloric acid titrating solution is sued as titrant, and a potentiometric titration method is adopted for the titration. The method has the advantages of small sample amount, simple operation, good precision, and the like, and can be applied to the routine analysis and the quality control of hydroxamamide tropine raw drugs.
Owner:JIANGSU INST OF NUCLEAR MEDICINE

Detection method for alpha-tropine as impurity in hydrochloric acid tropisetron

The invention relates to a detection method for alpha-tropine as impurity in hydrochloric acid tropisetron, which is characterized by adopting the gas chromatography for detection, and particularly includes the following steps: (1) preparing sample hydrochloric acid tropisetron solution with concentration of 10mg / m1 to 30mg / ml; (2) preparing reference sample alpha-tropine solution with the concentration of 0.02mg / m1 to 0.06mg / m1; (3) performing headspace sample injection and chromatogram acquisition; and (4) calculating the result through the appearance method based on the peak area. The invention has the characteristics that the detection method is convenient, quantitative and sensitive, and can be widely applied to the control and improvement of the medicine quality.
Owner:SHANDONG QIDU PHARMA

Improvement of nortropine synthesizing process

The invention discloses an improvement method of a nortropine synthesizing process. In the method, tropine and ethyl chloroformate are adopted as raw materials to synthesize nortropine. By adjusting the experimental operating steps, the method achieves the effects of moderate reaction condition, safe, simple as well as convenient operation, good product quality, and low cost.
Owner:YANGTZE RIVER PHARM GRP CO LTD +1

Novel method for preparing nor-tropine

The invention relates to a novel method for producing and preparing nor-tropine. The method comprises the following steps: taking N-alkoxycarbonyl nor-tropine as a raw material, adopting a small amount of potassium hydroxide (2-10 equivalent weights); rapidly hydrolyzing at the temperature of 100-160 DEG C and at high pressure of 1-10 atmospheric pressure and cooling to -5 to 10 DEG C after finishing reaction; filtering the collected and precipitated product; and carrying out recrystallization by ethyl acetate to obtain the product with purity being more than 99%. The products are all in extravert-type structure by GC detection. The method has the following advantages: 1. reducing the dosage of the potassium hydroxide to 10-25% of original dosage, thus saving the cost; 2. leaving out the cumbersome operation of chloroform and extraction, saving solvent, saving a large number of manpower and reducing pollution; 3. the actual pressure is about 5kg which is safe relatively when a high pressure autoclave is operated, thus eliminating explosion risk generated by the reaction of chloroform and potassium hydroxide; and 4. the color and luster and purity of the product is higher.
Owner:NINGBO TEAM PHARMA

Analysis method of mercapto amine tropine content

The invention relates to a content analysis method for sulfhydryl-amine tropine. It uses high efficiency liquid phase chromatogram-vaporizing light scattering detector to test sulfhydryl-amine tropine. The devices that are used for chromatographic analyzing are WATERS 600 high efficiency liquid phase chromatograph, WATERS 2420 vaporizing light scattering detector, and the chromatographic column of Hypersil C8 column, 5um, 4.6*250mm. The results shows that it has good separation of the main constituents peak and the impurity peak, the linear range is 12.5-50ug / mL, and the minimum detecting quality is 3.0ng (S / N>=3), and that has about 3.6% error compared to relative standard error. The invention could test content and impurity of sulfhydryl-amine tropine, and it is simple and convenient.
Owner:JIANGSU INST OF NUCLEAR MEDICINE

Preparation method of white thiophanate methyl

The invention discloses a preparation method of white thiophanate methyl, wherein diatomite is used as a decoloring agent, a color o-phenylenediamine industrial product is dissolved in an organic solvent, decolored by reflux and filtered to obtain a mixture of colorless o-phenylenediamine and the organic solvent, and the mixture is directly used in the synthesis of thiophanate methyl to obtain white tropine with whiteness of above 85 percent. The invention has less equipment investment, simple operation, low production cost, no three wastes and suitability for industrialized production.
Owner:HUNAN CHEM RES INST

Nimbin-tropine emulsion

Nimbin is extracted from nim kernel and has both pesticidal and bacteriostasis functions. Tropine is a kind of alkaloid extracted from solanaceae plant, such as henbane seed, belladonna and datura flower, and has powerful pesticidal function. Recompounding nimbin and tropine can obtain synergistic pesticidal effect. The nimbin-tropine emulsion of the present invention is recompounded with nimbin and tropine as main components and through adding proper amount of assistant. The pesticide has high efficiency, low toxicity, no pollution, safety to human body and farm animal and less resistance and may be used in preventing and treating various pests with resistance to other pesticides.
Owner:于建垒

Synthesis method of atropine and atropine sulfate

The invention provides a synthesis method of atropine and atropine sulfate, which comprises the following steps: carrying out acetylation reaction on tropine acid to form acetyl tropine acid, reactingthe acetyl tropine acid with a chlorination reagent to form acyl chloride, reacting the acyl chloride with tropine alcohol, removing acetyl to obtain atropine, and salifying atropine and sulfuric acid to obtain atropine sulfate. The whole synthesis process can be completed by adopting a one-pot reaction, additional steps for completing the process by isolating intermediates are avoided, the reaction conditions are mild, the steps are simple, the yield is high, the purity is high, and the method is suitable for large-scale industrial production.
Owner:合肥创新医药技术有限公司

Method for preparing 2-hydroxy-2,2-diphenylacetic acid-3alpha-(8-aza-bicyclo(3,2,1))-3-trioctyl

The invention discloses a method for preparing 2-hydroxy-2,2-diphenylacetic acid-3alpha-(8-aza-bicyclo(3,2,1))-3-trioctyl. The method comprises the following steps of: by taking dibenzoyl as a raw material, carrying out rearrangement on the raw material so as to obtain dihydroxy-phenylacetic acid; reacting dihydroxy-phenylacetic acid with dimethyl carbonate under the DBU catalysis and microwave actions so as to obtain methyl benzilate; reacting the methyl benzilate with tropine so as to obtain tropine benzilate; and carrying out N formylation and alcoholysis on the obtained tropine benzilate so as to obtain nor-tropine benzilate. Compared with the prior art, the total reaction time of the method disclosed by the invention is greatly reduced, the total yield is increased greatly, and the reaction condition is more simple, and therefore, the method is suitable for industrial production.
Owner:SICHUAN UNIVERSITY OF SCIENCE AND ENGINEERING

Compound bonding agent for baking-free magnesium vibration material

The invention discloses a compound bonding agent for a baking-free magnesium vibration material. The compound bonding agent is composed of the following components by mass percent: 86.35 wt% of anhydrous dextrose, 4.55 wt% of borax, 4.55 wt% of tropine and 4.55 wt% of industrial salt. The bonding agent is the non-toxic, tasteless and nuisanceless white crystalline particles or powder, has strong basicity, is easily dissolved in water, and is insoluble in alcohol and acid, the aqueous solution of the bonding agent is alkaline, and the bonding agent belongs to inorganic salt products. No elements polluting molten steel exist, no toxic or harmful gas is produced during heating the bonding agent, occupational safety and health of workers cannot be influenced, and no pollution to the environment is caused.
Owner:浙江攀盛冶金材料有限公司

Alpha-tropine related substance and isomer inspecting method

The invention discloses a method for inspecting alpha-tropine related substance and isomer inspecting method by a thin-layer chromatography. By means of preparing a related substance and isomer reference substance solution, a sample loading amount is controlled; after a developer is spread, a color developing agent is sprayed; thus, tropine related substance and isomer can be controlled under 0.5%. The method has the advantages of simpleness in operation, convenience and quickness; dedicated inspecting instruments are avoided; an economical, practical and effective method is provided for quick detection on tropine.
Owner:SHANDONG QIDU PHARMA

Preparation method of tropisetron hydrochloride

The invention discloses a preparation method of tropisetron hydrochloride. The Preparation method of the tropisetron hydrochloride is characterized by comprising the following preparation steps: (A) performing substation reaction on 3-indolecarboxylic acid (I) serving as a starting material and thionyl chloride by adding a reaction solvent to prepare 3-indoleformyl chloride (II), and directly performing condensation reaction on the 3-indoleformyl chloride (II) and alpha-tropine (III) under the existence of an acid-binding agent triethylamine to produce tropisetron (IV); and (B) performing acid and alkali salt-forming reaction on the tropisetron (IV) and hydrochloric acid in ethanol to produce the tropisetron hydrochloride (V). Raw materials used in the process reactions are the conventional reagents, are easily available on the market and are low in cost; the conditions are simple and not harsh, the conventional equipment can meet production requirements and are easy to control, and industrialized production can be realized; and dichloromethane and tetrahydrofuran have low boiling point and are easily evaporated to dryness, so energy conservation and safety are achieved.
Owner:KAMP PHARMA

3 alpha-high tropine aliphatic amine salt, crystal formation and preparation method

The invention relates to a 3 alpha-high tropine aliphatic amine salt, crystal formation and preparation method, which is to resolve problems of poor stability for preparing midbody of Granisetron, inconvenience for storage and transportation and low purity of final products. The 3 alpha-high tropine aliphatic amine is dissolved in one or more organic solvents and 1-10 equivalent hydrochloric acid, sulphuric acid or phosphoric acid are added in for crystallization and filtration after mixing to cool. 1 to 20-fold water and 10 to 100-fold alcohols solvent are used for recrystallization for cooling, crystallization, filtration and vacuum drying for 12 hours.
Owner:SINOPHARM CHUANKANG PHARMACEUTICAL CO LTD

Synthesis method of homatropine hydrobromide

The invention discloses a synthesis method of a homatropine hydrobromide shown in a formula (V), comprising the following steps of: tropine shown in a formula (I) and a compound (III) obtained by esterification of O-formyl almond acyl chloride shown in a formula (II); acidic hydrolysis is carried out to the compound (III) to obtain a compound (IV); and the compound (IV) is salified by the hydrobromide to obtain a compound (V). The synthesis method has the beneficial effects of: avoiding the use of benzene as a toxic solvent, having mild reaction condition, simple operation, short production period, high reaction yield and low production cost, being applicable to industrial production and having larger implement value and social and economical benefits.
Owner:ZHEJIANG UNIV OF TECH

Synthesis method of atropine sulfate

ActiveCN113321648AHigh yieldQuality is stable and qualifiedOrganic chemistryChemical synthesisPtru catalyst
The invention belongs to the field of chemical synthesis, and particularly relates to a preparation method of atropine sulfate. The preparation method comprises the following steps: firstly preparing tropine ester, then preparing atropine, salifying to prepare atropine sulfate, and finally refining to obtain the product. In the preparation process of the tropine ester, the reaction temperature is strictly controlled to be 105-111 DEG C, and the crystallization temperature is controlled to be 0-5 DEG C, so that the yield of the tropine ester is improved. In the process of preparing atropine through reduction reaction, palladium-carbon is adopted as a catalyst, and the reaction temperature is strictly controlled to be 10-15 DEG C, so that the product quality is effectively improved. Sulfuric acid is diluted by preparing a sulfuric acid ethanol solution, and the dripping speed of the sulfuric acid ethanol solution is controlled, so that the stable quality of atropine sulfate is ensured.
Owner:常州康普药业有限公司

Method for testing tropine alcohol of residual intermediate product in synthesizing Troipisetron

A method for detecting residual intermediate of tropaic alcohol in tropisetron synthesis includes preparing test solution and control solution , dropping them separately on the same silica gel G thin layer plate , using acetone - ammonia water as developing agent to carry out thin layer chromatography determination, developing chromatographic cylinder, using developer of bismuth potassium iodide solution with assistance of sodium nitride solution to develop color and checking colour developed result.
Owner:QINGDAO PURUISEN MEDICINE SCI & TECH CO LTD

Application of arabidopsis thaliana UGT74F2 in catalyzing phenyllactic acid to synthesize phenyllactoyl glucose

The invention discloses an application of arabidopsis thaliana UGT74F2 in catalyzing phenyllactic acid to be subjected to glycosyl transfer reaction to synthesize phenyllactoyl glucose. Research finds that UGT74F2 from arabidopsis thaliana can catalyze phenyllactic acid to synthesize phenyllactoyl glucose, and the catalytic activity of the UGT74F2 is higher than that of AbUGT1 reported at present and used for tropine alkaloid synthesis. The UGT74F2 can be used for tropane alkaloid metabolic engineering to improve the alkaloid content, the application value of UGT74F2 is widened, and the UGT74F2 has very important significance on medicinal TA metabolic engineering and synthetic biology.
Owner:SOUTHWEST UNIV

Method for preparing retapamulin

The invention discloses a method for preparing retapamulin. The method comprises the following steps that a compound of a formula 3 and a compound of a formula 4 are subjected to a nucleophilic substitution reaction to obtain a compound of a formula 5; the compound of the formula 5 is subjected to a hydrolysis reaction to obtain beta-tropine mercaptan shown in a formula 6; the beta-tropine mercaptan shown in the formula 6 is not separated and purified to be subjected to condensation with a compound of a formula 2 to obtain retapamulin 1; the reaction formula is shown in the specification, wherein M in the compound of the formula 4 is a metal ion of a potassium ion or a sodion or a calcium ion or an iron ion or an ammonium ion, n corresponds to the valence of the metal ion M and is 1 or 2 or 3, and R is alkyl groups C1-C3 or a phenyl group or a substituted phenyl group or a benzyl group or a substituted benzyl group. The method is easy and convenient to implement, a cheap reagent is adopted, the influences on the environment are greatly reduced, intermediate products are easy to purify, no column chromatography is needed, the defects of reported methods for preparing beta-tropine mercaptan and retapamulin are overcome, and the method has obvious positive and progressive effects and practical application value.
Owner:SHANGHAI INST OF PHARMA IND CO LTD +1

Atropine alkaloid hapten and artificial antigen as well as preparation methods and application thereof

The invention discloses an atropine alkaloid hapten and artificial antigen as well as preparation methods and application thereof The structural formula of the atropine alkaloid hapten is shown as a formula I. The atropine alkaloid hapten is prepared according to the following method: 1) taking pyridine as a solvent, and carrying out reaction on tropine and succinic anhydride; and 2) adding the succinic anhydride into the reaction liquid after the reaction in the step 1) again, and stirring to obtain the atropine alkaloid hapten. A carrier protein can be coupled to carboxyl carbon of the hapten by adopting an active ester method to obtain the atropine alkaloid artificial antigen. The invention also provides a monoclonal antibody of the atropine alkaloid, which is obtained by immunizing an experimental animal (female BALB / c mouse) through the atropine alkaloid artificial antigen and carrying out cell fusion, screening and in-vitro induction. The monoclonal antibody of the atropine alkaloid can be used for preparing an atropine alkaloid detection reagent or kit. Thehapten and artificial antigen have a good application prospect in veterinary drug residue detection.
Owner:CHINA AGRI UNIV

A method for preparing high-purity 1,8-cineole from camphor crude oil

The invention discloses a method for preparing high-purity 1,8-cineole from camphor crude oil. The method uses crude camphor oil as a raw material, and removes 1,8-cineole with a boiling point above 200°C through a simple vacuum distillation step. heavy fraction, and collect camphor leaf oil with an average content of 1,8-cineole of more than 80%, and then use tropin alcohol low eutectic solvent as a green medium from the oil containing 80% of 1,8-cineole Preparation of high-purity 1,8-cineole by liquid-liquid extraction from camphor leaf oil. The process of the present invention purifies 1,8-cineole from camphor leaf crude oil by using one-time rectification and one-time liquid-liquid extraction to prepare high-purity 1,8-cineole, compared with the existing one-step rectification and The two-step freezing and crystallization method has a simple process and is more energy-saving. In addition, the low eutectic solvent can be recycled and reused, and the process is green.
Owner:成都市明典世家生物科技有限公司

Three points three p450 enzyme and its application in the preparation of tropinone

The invention discloses a three-point three-point P450 enzyme, which can convert 4-(1-methyl-2-pyrrolidinyl)-3-oxobutanoic acid into tropine through joint catalysis of the P450 enzyme and cytochrome P450 reductase ketone. The method of the invention is environmentally friendly, has mild reaction conditions and has industrial development prospects.
Owner:CAS CENT FOR EXCELLENCE IN MOLECULAR PLANT SCI

Preparation method of choline receptor antagonist

The invention provides a preparation method of a choline receptor antagonist. The choline receptor antagonist is ipratropium bromide. According to the method provided by the invention, alpha-formyl phenylacetic acid is taken as an initial raw material and reacts with isopropyl tropine alcohol to generate a compound II, the compound II is subjected to a reduction reaction to generate a compound III, and the compound III reacts with bromomethane to generate ipratropium bromide. Compared with the prior art, the method is easy to operate, high in safety, low in cost, high in yield and product purity and more suitable for industrial production.
Owner:SHANGHAI FANGYU HEALTH PHARMA TECH CO LTD
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