47 results about "Tabersonine" patented technology

The invention relates to the plant extraction field, and aims to provide an efficient and environmentally-friendly technology for extracting tabersonine from Voacanga chalotiana Pierre ex Stapf. The technology comprises the following steps: 1, taking Voacanga chalotiana Pierre ex Stapf, sun-drying, peeling shells, and crushing; 2, micronizing treatment: adding submicron powder obtained in step 1 into ethyl acetate having a volume 1.5-3 times the mass of the submicron powder, and carrying out ultrasonic treatment at normal temperature for 0.5-1h, and centrifuging; 3, carrying out reflux extraction of the filter residue obtained in step 2 for 0.5-2h twice by utilizing ethyl acetate having a volume 2-5 times the mass of the filter residue; 4, mixing the obtained reflux extract liquid with the obtained centrifugate obtained after the ultrasonic treatment, and concentrating until no droplets drop; 5, adding an aqueous solution containing 6-10% of TritonX-114 having a volume 0.5-3 times the volume of the concentrate obtained in step 4, carrying out heat insulation stirring at 35-50DEG C for 0.5-1h, and centrifuging; and 6, adding a proper amount of water to the solid obtained in step 5, stirring for 10-20min, allowing the obtained solution to stand for separating out the upper layer yellow oil, and extracting 1-3 times by using the above same method, wherein the yellow oil is liquid tabersonine. The technology has the advantages of ingenious combination, high total extraction efficiency and less pollution emission.

The invention discloses a preparation method of high-purity vinpocetine. The preparation method comprises the following steps: S1, preparing vincamine, wherein tabersonine is dissolved, a hydrogenation reaction is performed under the catalysis of palladium and carbon to obtain vincadifformine, the vincadifformine is oxidized to obtain a vincadifformine nitric oxide, and an intermediate vincamine is obtained from the vincadifformine nitric oxide reaction liquid under the catalysis of an acid; S2, dewatering the vincamine by using toluene as a solvent and adding a dewatering agent to obtain apovincamine; and S3, on the basis of the step S2, carrying out a transesterification reaction by taking ethanol as a solvent, using dichloromethane as a cosolvent and using sodium ethoxide / sodium methoxide as a catalyst to obtain a vinpocetine crude product, and re-crystallizing with ethanol to obtain vinpocetine. The process provided by the invention has the advantages of simple production operation, avoidance of high-toxicity reagents, less impurity of the obtained product, high production efficiency, simple and convent operation and environmental friendliness, wherein the purity of the productis more than 99.9%, the quality of the product is higher than the quality of the product obtained by the original research factory, and the medicinal requirements are met.

The invention relates to a synthetic process for chemical medicines, in particular to a process for preparing vincamine by a semisynthetic method. At present, the process for preparing the vincamine is divided into a total synthetic method and the semisynthetic method, wherein the semisynthetic method has the problems of unstable and inflammable hydrogenation catalyst, large using amount, high hydrogenation pressure, insecurity in the preparation of monoperoxide maleic acid and the like. The process comprises the following steps of: preparing tabersonine vincadifformine hydrochloride, preparing the monoperoxide maleic acid, performing oxidizing reaction, performing reduction reaction and transposition reaction, precipitating ammonia and purifying products, wherein the low-cost and stable Pd / C hydrogenation catalyst is selected to reduce the pressure of the hydrogenation reaction; tabersonine sulfate is replaced by the tabersonine hydrochloride; the monoperoxide maleic acid is preparedby using low-concentration hydrogen peroxide; the reaction temperature is below 0 DEG C, and security coefficients are improved; the temperature of the oxidizing reaction is reduced, and the generation of isomers is reduced; purification and solvent recrystallization are performed by column chromatography; and the quality of the products reaches the pharmaceutical-grade standard.

The invention relates to a preparation method of plant extract, in particular to a preparation method of willow leaf tabersonine, which can resolve the problems of prior art such as complex process, long production period and low product yield. The preparation method comprises 1, material pretreatment: breaking and drying seeds, 2, heating, refluxing, extracting and acidifying, 3, purifying on column, 4, alkalizing, extracting, washing hexane layer via water and removing solvent to obtain the product. The preparation method has the advantages of simple chemical process, low environment pollution, high safety, short production period, support for large-scale industrial production, simple process, high controllability and high product yield, wherein unit kilogram of Africa potato can produce at least 98% willow leaf tabersonine whose yield is higher than 1.6%.

The invention discloses a method for extracting tabersonine from Voacanga Africana seeds. The method comprises the following steps: (1) crushing: crushing the dried Voacanga Africana seeds, screening the crushed seed by a 20-40 mesh screen to obtain powder, grinding the powder by liquid nitrogen to obtain superfine powder; (2) enzymolysis: adding the superfine powder obtained in the step (1) into a cellulase liquid with the enzyme concentration of 0.5-0.7 g / L, allowing the mixture to perform enzymolysis reaction for 2-3 hours at 40-45 DEG C, so as to obtain enzymatic hydrolysate; (3) carrying out supercritical extraction; (4) carrying out alcohol extraction; (5) carrying out separating and purifying. According to the extraction method, toxic solvents such as benzene and chloroform are not used, and no large amount of waste water is generated, and the environment is not polluted, meanwhile, the extraction method is simple to operate, short in time consumption, high in yield and purity, the yield is up to 3.9%, and the purity is 99.6%.

The invention discloses a process for preparing tabersonine, aiming at solving the problems of tedious process, higher cost, lower yield and the use of solvents serious harmful to human bodies in the prior art. The process comprises the steps of: crushing raw materials, extracting with acid water, alkalizing and extracting the extracting solution, mixing an organic extraction layer, concentrating, recycling until no solvent exists, placing in a refrigerator, standing overnight, precipitating crystals, centrifuging, and drying the crystals. In method disclosed by the invention, the properties of alkaloid are utilized for acidizing tabersonine into salt with a water extraction process, thus, the production steps are simplified, and the production cost is reduced; the method has the advantages of simple process and easiness for operation, the yield is largely improved by about 3%, and the products are light yellow powder and have higher quality; and in addition, because less solvent is used, the pollution to the environment and the harm to human bodies are lowered.

The invention discloses a method for extracting tabersonine from voacanga africana. The method comprises the following steps: S1, crushing a raw material; S2, soaking, namely soaking crushed voacangaafricana fruit seeds into a 2-4% sulfuric acid solution; S3, performing percolation, namely putting the soaked voacanga africana fruit seeds into a percolation tube, continuously adding the sulfuric acid solution from an upper part, and collecting a percolation liquid; S4, filtering, namely filtering the obtained percolation till the filtrate is clear and transparent; S5, performing column chromatography, namely adsorbing the filtrate with a macroporous resin, washing the resin with water when the content of an effluent is greater than or equal to 0.2mg / ml, and collecting a desorption liquid,wherein a 65-75% ethanol solution is adopted as a desorption solvent; S6, performing concentration centrifugation, namely concentrating the desorption liquid, adjusting a pH value, leaving to stand, and performing centrifugation, so as to obtain a product. The method disclosed by the invention is simple and convenient to operate, environmentally-friendly and high in extraction recycling rate.

The invention relates to the plant extraction field, and aims to provide an efficient and environmentally-friendly technology for extracting tabersonine from Voacanga chalotiana Pierre ex Stapf. The technology comprises the following steps: 1, taking Voacanga chalotiana Pierre ex Stapf, sun-drying, peeling shells, and crushing; 2, micronizing treatment: adding submicron powder obtained in step 1 into ethyl acetate having a volume 1.5-3 times the mass of the submicron powder, and carrying out ultrasonic treatment at normal temperature for 0.5-1h, and centrifuging; 3, carrying out reflux extraction of the filter residue obtained in step 2 for 0.5-2h twice by utilizing ethyl acetate having a volume 2-5 times the mass of the filter residue; 4, mixing the obtained reflux extract liquid with the obtained centrifugate obtained after the ultrasonic treatment, and concentrating until no droplets drop; 5, adding an aqueous solution containing 6-10% of TritonX-114 having a volume 0.5-3 times the volume of the concentrate obtained in step 4, carrying out heat insulation stirring at 35-50DEG C for 0.5-1h, and centrifuging; and 6, adding a proper amount of water to the solid obtained in step 5, stirring for 10-20min, allowing the obtained solution to stand for separating out the upper layer yellow oil, and extracting 1-3 times by using the above same method, wherein the yellow oil is liquid tabersonine. The technology has the advantages of ingenious combination, high total extraction efficiency and less pollution emission.

A preparation method of a vinpocetine analogue comprises the following steps: using UHP (urea hydrogen peroxide) for selective oxidation of a tabersonine analogue, then performing reduction, rearrangement, crystallization, and the like; or using the UHP for selective oxidation of a tabersonine reduction analogue (vinca-fuming analogue), then performing rearrangement, crystallization, and the like to obtain the vinpocetine analogue. Compared with the prior art, the preparation method has the advantages of high yield, direct quantification, simple operation, mild reaction conditions, suitability for industrial production, the yield reaching over 87%, more than 99% of HPLC (high performance liquid chromatography), a white product, good quality and low preparation cost.

Methods that may be used for the manufacture of a class of chemical compounds known as terpenoid indole alkaloids, including tabersonine and catharanthine are provided. Compositions useful for the synthesis of terpenoid indole alkaloids, including tabersonine and catharanthine are also provided. The provided compounds are useful in the manufacture of chemotherapeutic agents.

The invention discloses a production process using a semi-synthetic method to prepare vincamine. The production process comprises the following steps: using a tabersonine salt as a reaction starting raw material, performing hydrogeneration catalytic reduction, enzyme method hydroxylation and rearranged crystallization to obtain vincamine. The process is simple and short in process route; the obtained vincamine is high in yield and good in purity; the whole production process is low in cost and suitable for industrial production; the enzyme method hydroxylation is performed by oxygenase, so that the process is clean, safe and environment-friendly.