64 results about "Tropine" patented technology

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.