37 results about "Phthalide" patented technology

The invention discloses a paired electrochemical synthesis method of anisaldehyde and phthalide, which comprises the following steps of: adopting p-methyl anisole and phthalate as raw materials, oxidizing p-methyl anisole at an anode to generate anisaldehyde through electrolytic reaction in the same electrolytic bath, and reducing phthalate at a cathode to generate phthalide, an electrolyte system adopted in the electrolytic reaction comprises an electrolyte, water, N, N-dimethylformamide and methanol. In the same electrochemical synthesis system, p-methyl anisole and phthalate are used as raw materials, the mixed solvent which is low in price and easy to obtain is used, anisaldehyde is generated on an anode and phthalide is generated on a cathode through an electrolytic reaction, high-added-value products exist in the anode and the cathode, an oxidizing agent and a noble metal catalyst are not needed, and the method is simple and convenient to operate. Basically no three wastes are generated, and no hydrogen and oxygen are generated in the reaction process, so that the method is safer.

The invention belongs to the technical field of prevention and treatment of peanut southern blight, and particularly relates to a bactericidal composition for preventing and treating peanut southern blight. The invention relates to a sterilization composition. The effective component of the sterilization composition is formed by compounding butylphthalide and pyraclostrobin or tebuconazole according to the mass ratio of (1-150): (150-1). After the butylphthalide and the pyraclostrobin or the tebuconazole are compounded according to a certain mass ratio, the activity of the compounded formula is not simply superposed, but shows a very good synergistic effect. Compared with single pyraclostrobin or tebuconazole, the composition has the advantages that the prevention and treatment effect on the peanut southern blight can be improved, and on the basis, the dosage of medicaments can be reduced, and the environmental pollution can be reduced.

The invention discloses phthalide compounds as well as a preparation method and application thereof. The phthalide compounds comprise a compound 1 and a compound 2 as well as a preparation method and application thereof. The two compounds are separated and purified from the ethyl acetate extract of the traditional Chinese medicine ligusticum wallichii for the first time. An in-vitro biological activity test shows that the two compounds have obvious inhibitory activity on xanthine oxidase, which indicates that the two compounds can be used as novel potential candidate drugs for treating hyperuricemia and gout. The embodiment of the invention provides a preparation method, structural identification and pharmacological action of the two phthalide compounds, and provides a new strategy for treatment of hyperuricemia and gout diseases.

The application discloses a method for establishing a gynecological menstruation-regulating tablet fingerprint spectrum by using a high-performance liquid chromatography technology and application, by using the method, a good fingerprint spectrum is obtained, and the chromatographic peak is comprehensive, 12 fingerprint peaks are confirmed, wherein, corresponding attribution peaks of angelica sinensis, fried atractylodes macrocephala koidz, vinegar corydalis and chuanxiong are all in the gynecological menstruation-regulating tablet, and the angelica sinensis, fried atractylodes macrocephala koidz and vinegar corydalis all have exclusive peaks. By comparing with the reference substance, and combining with ultraviolet absorption spectrum characteristics, characteristic peaks of five chemical components, i.e., chlorogenic acid, ferulic acid, chuanxiongolide I, ligusticum lactone and butenyl phthalide are identified. The application further discloses a reference fingerprint spectrum of the gynecological menstruation-regulating tablet obtained by using the method, the gynecological menstruation-regulating tablet fingerprint spectrum detection method and the obtained reference fingerprint spectrum can objectively evaluate the overall quality of the gynecological menstruation-regulating tablet, and provide a research basis for quality control of the gynecological menstruation-regulating tablet.

Phthalide lactones, as an important class of benzopentolactone skeleton, are widely distributed in natural products, medicinal plants and bioactive molecules, and have significant pharmacological activities and synthetic application potential. This kind of structure not only shows various biological activities such as antibacterial, anti-inflammatory, antitumor, antioxidant, but also is an indispensable core structural unit in many drug molecules and lead compounds. At the same time, cyano is a very valuable functional group in the field of organic synthesis and medicinal chemistry, with strong electron-withdrawing properties, strong structural stability and other advantages, which can effectively improve the electronic distribution, lipid solubility and drug performance of the molecule. In view of the important significance of phthalide lactones and cyano in organic synthesis and drug research and development, the present invention develops a synthetic method for efficiently constructing cyano-containing alkyl chain substituted phthalide lactone compounds. It has important value in medicinal chemistry and organic synthesis.

The invention discloses an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure and a preparation method and application thereof. The chemical structural formula of the ferroptosis inhibitor is shown as a formula 1 or a formula 2. The ferroptosis inhibitor can inhibit ferroptosis caused by a ferroptosis inducer and can reduce the level of active oxygen in cells. Nerve injury caused by cerebral ischemia reperfusion can be relieved, and symptoms of neurological diseases such as Alzheimer's disease and Parkinson's disease can be relieved; compared with a ferroptosis inhibitor Ferrostatin-1, the aryl alkyl amine compound disclosed by the invention has better metabolic stability and is suitable for in-vivo drug effect evaluation. Therefore, the novel aryl alkyl amine compound provided by the invention has a very good application value in treatment of neurological diseases related to ferroptosis.

The present application belongs to the field of pharmaceutical chemistry, and relates to the prevention and treatment of peanut stemphylium leaf blight and peanut root rot, in particular to amino acid-oriented phthalide analogues and a preparation method and application thereof. The phthalide analogues have a structural general formula as shown in formula A or formula B: and formula B, wherein R and R' are selected from natural amino acids or unnatural amino acids, and the unnatural amino acids are substitution products of 4-NO2, 4-F or 4-Cl of amino acids. The results of bioactivity determination show that all the compounds have Sclerotium rolfsii mycelium growth inhibition activity, wherein the 5-substituted phthalide of phenylalanine and the 5-substituted phthalide of arginine in formula A have obvious bacteriostatic activity, and meanwhile, the results of pot experiments show that the 5-substituted phthalide of phenylalanine has good control effect. Therefore, the amino acid-oriented phthalide analogues have good development and application prospects.

Disclosed are an aromatic alkylamine ferroptosis inhibitor based on a butylphthalide structure, a preparation method therefor, and an application thereof. The chemical structural formula of the ferroptosis inhibitor is as shown in formula (1) or formula (2). The ferroptosis inhibitor is capable of inhibiting ferroptosis caused by a ferroptosis inducer, and reduces the level of intracellular reactive oxygen species. The ferroptosis inhibitor reduces neurological damage caused by cerebral ischemia-reperfusion, and alleviates symptoms of neurological disorders such as Alzheimer's disease and Parkinson's disease. Compared to the ferroptosis inhibitor Ferrostatin-1, the arylalkylamine compound exhibits better metabolic stability and is suitable for in-vivo efficacy evaluation. Therefore, the novel arylalkylamine compound provided by the present invention demonstrates great application value in the treatment of ferroptosis-related neurological disorders.

The present application relates to a kind of tetrahydropyrrolizino [2, 3-c] quinoline alkaloid compound and derivative with novel structure and preparation method and purposes thereof.The new compound bungeanoline G provided in the present application is extracted and separated from Papaveraceae Corydalis bungeana Turcz.The present application also proposes a method for artificially synthesizing bungeanoline G, and a series of derivatives of bungeanoline G are prepared.Biological activity experiments show that the compounds have acetylcholinesterase and butyrylcholinesterase inhibitory activity, and can be applied in the preparation of drugs for treating or improving various neurodegenerative diseases such as Alzheimer's disease, vascular dementia, myasthenia gravis and the like.

The invention belongs to the technical field of pesticides, and relates to a phenol derivative containing a phthalide structure as well as a preparation method and application thereof. According to the invention, phthalide and phenol are organically combined and modified to synthesize the phenol derivative containing the phthalide structure. According to the invention, carboxybenzaldehyde, phthalide, phenol compounds and the like are respectively used as raw materials, the phenol derivative containing the phthalide structure is prepared through condensation, nucleophilic substitution and other reactions, the reaction conditions are mild, the used acidic reagent, alkaline reagent and Lewis acid are easy to obtain, and the product is simple and convenient to purify. The phenol derivative containing the phthalide structure has a good prevention and treatment effect on various plant viruses such as tobacco mosaic viruses, pepper viruses and wheat viruses, solves the problems that existing plant virus resisting agents are deficient in variety and insufficient in activity, and is expected to be developed into a novel plant virus resisting agent which is efficient, safe, economical and environmentally friendly.

The invention relates to a method for selectively removing undifferentiated pluripotent stem cells, which comprises the following steps of: firstly inducing stem cell differentiation, and then applying an effective amount of phthalide compound to remove the undifferentiated stem cells.

The invention discloses a method for synthesizing a phthalide compound with high selectivity under a biological compatibility condition. According to the method, a thiol compound and a 2-formyl benzoate compound are taken as raw materials, coupling is efficiently and rapidly realized in a PBS buffer solution under the action of potassium carbonate, and a phthalide product is generated. The reaction has the advantages of high yield and high reaction speed, shows excellent chemical selectivity on cysteine sulfydryl, and can effectively distinguish other nucleophilic amino acids. The method disclosed by the invention is wide in substrate applicability, simple and convenient in steps, low in cost, mild and green in conditions and good in functional group compatibility, and provides an efficient, safe and practical new way for construction of a linker of an antibody-coupled drug (ADC) and modification of phthalide active molecules.

The application discloses a preparation method of o-carboxybenzaldehyde, which comprises the following steps: S1, reacting a phthalide with a potassium hydrogen peroxysulfate complex salt and an alkali in a polar protic solvent to prepare an intermediate; S2, hydrolyzing the intermediate obtained in the step S1 by using a strong protic acid aqueous solution to obtain a product o-carboxybenzaldehyde; and S3, adjusting the pH of the product obtained in the step S2 to 3-4 by using a sodium hydroxide aqueous solution, quenching excessive potassium hydrogen peroxysulfate complex salt by using a saturated sodium sulfite solution, cooling, recrystallizing, filtering and vacuum drying to obtain a final product o-carboxybenzaldehyde. The preparation method of the o-carboxybenzaldehyde can effectively reduce the synthesis cost, avoids the use of dangerous and toxic reagents, effectively reduces the generation of industrial three wastes, and is simple in process, convenient in operation, low in raw material cost, high in yield and beneficial to large-scale industrial production.

The invention provides a phthalide ring-opening derivative as shown in a formula (I-1) and a stereoisomer or pharmaceutically acceptable salt thereof and application thereof. Experimental results show that the compound disclosed by the invention has excellent pharmacokinetic properties, and the release of butylphthalide and dexcanthanol in vivo is superior to that of single drug butylphthalide and dexcanthanol and is also superior to that of a compound composition. The compound disclosed by the invention has an excellent brain protection effect and can greatly reduce the cerebral infarction area; the compound can be used for preventing and treating nerve injury, degenerative diseases and ischemic diseases. # imgabs0 #

The invention belongs to the technical field of medicines, and discloses phthalithiazole amine derivatives as well as a preparation method and application thereof. In particular discloses a phthalithiazole amine derivative, a preparation method thereof and application of the phthalithiazole amine derivative in the aspect of resisting epilepsy accompanied by cognitive impairment. The invention specifically relates to a phthalithiazole amine derivative as shown in a general formula (I). The invention also relates to a preparation method of the compounds, a pharmaceutical composition containing the compounds, and an application of the compounds in preparation of medicines for treating and / or preventing epilepsy accompanied by cognitive impairment.

The embodiment of the application discloses a natural small molecule inhibitor targeting NLRP3 inflammasome and application thereof, and belongs to the technical field of biological medicine. Chuanxiongdiolide R11 is a phthalide dimer compound with clear stereochemistry found in traditional Chinese medicine Chuanxiong, which can target NLRP3 inflammasome, prevent the activation and assembly of the inflammasome, thereby inhibiting caspase-1 activation, GSDMD cleavage, pyroptosis and the maturation and release of IL-1beta / IL-18. The compound can be used for preparing a drug for treating NLRP3 related inflammatory diseases such as systemic inflammation and peritonitis, and has a good clinical application prospect, and provides a new idea for developing and applying NLRP3 inhibitors in clinic.

The application belongs to the technical field of microbial fermentation, and particularly relates to a fermented lactobacillus mucioparius FJ701 and application of the fermented lactobacillus mucioparius FJ701 in preparation of high-biological-activity angelica fermentation product. The angelica fermentation product prepared by fermentation of the fermented lactobacillus mucioparius FJ701 has high content of dihydroferulic acid, butenyl phthalide, polyphenol and flavone, and in vitro simulation digestion experiments show that the bioavailability of dihydroferulic acid, butenyl phthalide and polyphenol is significantly improved.

This invention provides a method for the oxidation of o-xylene to phthalide, comprising reacting o-xylene with an oxidant in the presence of a catalyst, wherein the catalyst comprises at least two transition metal ions and carbon nanotubes. The method for the oxidation of o-xylene to phthalide provided by this invention utilizes a composite catalyst of at least two transition metal ions and carbon nanotubes, effectively improving the selectivity of phthalide.

The invention belongs to the technical field of Chinese mesona herb cultivation, and particularly relates to a green, ecological and disease-resistant Chinese mesona herb cultivation method which comprises the following steps: S1, soil preparation and ridging; s2, film covering and punching; s3, field planting and watering; s4, timely topdressing; s5, disease prevention and treatment: mainly preventing and comprehensively preventing and treating; when the Chinese mesona herb has a stem rot symptom in the growth process, spraying a bactericide of which the effective components are compounded by butenyl phthalide and berberine or osthole; and S6, timely harvesting. According to the method, in the cultivation process of the mesona chinensis, by spraying the bactericide with the effective components compounded by butylenephthalide and berberine or osthole, the prevention and treatment effect on the stem rot of the mesona chinensis can be improved, the dosage of pesticide and pesticide residues are reduced, and then support can be provided for green, ecological and disease-resistant cultivation of the mesona chinensis.

The invention relates to the technical field of traditional Chinese medicine, and provides a pharmaceutical composition capable of preventing and treating headache and application thereof.The pharmaceutical composition is composed of ligusticum wallichii phthalide lactone extract and angelica dahurica coumarin extract which serve as effective components and pharmaceutically acceptable auxiliary materials or carriers, the weight ratio of the ligusticum wallichii phthalide lactone extract in terms of ligustilide to the radix angelicae coumarin extract in terms of imperatorin is 10: (1-10). The composition can enhance the effects of ligustilide and imperatorin which are known at present, can also achieve remarkable synergistic interaction and complementary effects in the aspect of the comprehensive effect of preventing and treating headache, can also avoid the loss and waste of senkyunolide A, butylphthalide and other more possible beneficial effective components, and has a good application prospect. The traditional Chinese medicine resources are fully and well utilized, and the production cost and the medicine price are remarkably reduced.

The present invention relates to a 2-pentanoylbenzonitrile reductase mutant and its use in preparing optically pure n-butylphthalide. Specifically, it relates to a 2-pentanoylbenzonitrile reductase mutant with improved activity, stability, and enantioselectivity, a gene encoding the 2-pentanoylbenzonitrile reductase mutant, a recombinant expression vector containing the gene sequence, and a recombinant expression transformant, as well as the use of the 2-pentanoylbenzonitrile reductase mutant as a catalyst for catalyzing the asymmetric reduction of 2-pentanoylbenzonitrile compounds, particularly catalyzing the asymmetric reduction of 2-pentanoylbenzonitrile to prepare optically pure n-butylphthalide (n-butylphthalide). Compared with the prior art, the present invention has the advantages of high enzymatic reaction substrate concentration, mild reaction conditions, environmental friendliness, high yield, and high product optical purity, and has good application prospects.

The application discloses a preparation method of a chiral phthalic ester prodrug and relates to the technical field of organic chemical synthesis. In the application, isothiourea is used as a Lewis base catalyst, and acyl chloride is used as an acylating agent, so that an acylation dynamic kinetic resolution process of racemic 3-hydroxyisobenzofuran-1(3H)-one (hereinafter referred to as phthalide) is realized, thereby forming a chiral phthalic ester with good to excellent yield and enantioselectivity and natural products and drugs containing the structure.

The application discloses a method for preparing o-phthalaldehyde from o-xylene. V2O5-TiO2 doped with metal elements is used as a catalyst, o-xylene and an oxygen-containing gas are reacted to obtain a mixed oxidation product containing o-phthalic anhydride, o-phthalic acid and phthalide; the mixed oxidation product is reacted with a reducing agent in a solvent, and o-phthalalcohol is obtained after separation; and the o-phthalalcohol is reacted with an oxidizing agent, and o-phthalaldehyde is obtained after separation. The application avoids the use of corrosive substances such as bromine or chlorine and nitric acid, has low requirements on equipment, is small in environmental pollution, and is high in overall yield of o-phthalaldehyde.

The invention relates to the technical field of Chinese patent medicine analysis, in particular to a multi-component characterization method of Jichuan decoction and application of the multi-component characterization method. According to the multi-component characterization method provided by the invention, an off-line two-dimensional liquid chromatography tandem quadrupole-electrostatic field orbitrap high-resolution mass spectrometry technology is adopted, and efficient and accurate analysis of various chemical components of Jichuan decoction is realized through specific chromatographic conditions and mass spectrometry conditions. By means of the method, more than two hundred compounds can be identified from the Jichuan decoction, the compounds contain flavonoids, terpenoids, phenylethanoid glycosides, organic acids, coumarins, phenylpropanoids, iridoids, phthalides, steroids and other components, and reference can be provided for research of pharmacodynamic substances of the Jichuan decoction.

The application provides a catalyst system for preparing phthalide by oxidizing o-xylene, which comprises at least two kinds of transition metal ions and carbon nanotubes. The catalyst system provided by the application can effectively improve the selectivity of phthalide in the reaction of preparing phthalide by oxidizing o-xylene.

The application belongs to the field of traditional Chinese medicine preparation analysis, and specifically discloses a method for rapidly identifying main chemical components in Guipi mixture by using ultra-high performance liquid chromatography-quadrupole-electric field orbitrap high-resolution mass spectrometry (UHPLC-Q-Exactive MS) technology, which realizes the purpose of rapidly qualitatively identifying 115 components such as phenylalanine, phthalide, flavonoids, ketones and terpenes in Guipi mixture. The method has the advantages of simplicity, rapidness, high efficiency and sensitivity, and can provide evidence for establishing the interaction between the components and the curative effect of Guipi mixture, and provide basis for the research on the safety and effectiveness of clinical medication.

The invention discloses a 3-(piperidine alkyl dithioalkyl) phthalide compound (I), pharmaceutically acceptable salts thereof, a preparation method thereof, a pharmaceutical composition thereof and application of the 3-(piperidine alkyl dithioalkyl) phthalide compound in preparation of drugs for treating and / or preventing nervous system related diseases. Comprising but not limited to vascular dementia, Alzheimer's disease, frontotemporal dementia, Prion disease, dementia with Lewy bodies, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, cerebral arterial thrombosis, hemorrhagic stroke, nerve injury caused by cerebral trauma and other diseases;

The invention discloses application of butenyl phthalide in preparation of a medicine for treating ulcerative colitis, and belongs to the technical field of biological medicines. The invention discovers that butenyl phthalide has better improvement and treatment effects on ulcerative colitis for the first time. Butenyl phthalide exerts a treatment effect from tissue, cells and molecular levels in a multi-level manner through a synergistic effect of a plurality of mechanisms of enhancing intestinal barriers, promoting epithelial repair, inhibiting secretion of inflammatory factors and exerting an anti-oxidation effect, jointly relieves intestinal inflammation and oxidative damage, protects and repairs intestinal functions, and has a good treatment effect. The invention provides a new treatment strategy for ulcerative colitis, and has a good prospect.

The invention discloses a method for synthesizing chiral phthalide derivatives through dynamic kinetic resolution. A catalyst used in the method is a chiral diphosphine complex of palladium. According to the method, asymmetric allylation of the phthalide compound can be realized, and the high-optical-purity phthalide derivative containing continuous tertiary carbon and quaternary carbon three-dimensional centers can be obtained with excellent yield (the enantiomer excess can reach 99%, and the diastereomer proportion is up to gt; 20: 1). The method has the advantages of excellent chemical selectivity, enantioselectivity and diastereoselectivity, simple and easy operation, commercially available catalyst, mild reaction conditions, low energy consumption, environmental friendliness and high yield.