16 results about "Phthalide" patented technology

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.

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 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 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 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 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 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 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;

This invention discloses a class of 3-substituted phthalide compounds (I) and their pharmaceutically acceptable salts, their preparation methods, pharmaceutical compositions, and their use in the preparation of drugs for the treatment and / or prevention of neurological diseases, including but not limited to vascular dementia, Alzheimer's disease, frontotemporal dementia, Prion's disease, Lewy body dementia, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, ischemic stroke, hemorrhagic stroke, and neurological damage caused by traumatic brain injury;

The invention discloses a 3-(piperidine alkyl sulfide or seleno) phthalide compound (I), pharmaceutically acceptable salts thereof, a preparation method thereof, a pharmaceutical composition and application thereof 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;

This invention discloses a class of piperidine alkyl dihydroxyphthalide compounds (I) and their pharmaceutically acceptable salts, their preparation methods, pharmaceutical compositions, and their use in the preparation of medicaments for treating and / or preventing diseases by means of anti-oxidative stress, inhibition of amyloid aggregation, metal ion complexation, or anti-neuroinflammatory effects, including but not limited to vascular dementia, Alzheimer's disease, frontotemporal dementia, Prion's disease, Lewy body dementia, Parkinson's disease, Huntington's disease, HIV-related dementia, multiple sclerosis, amyotrophic lateral sclerosis, neuropathic pain, ischemic stroke, hemorrhagic stroke, and neurological damage caused by traumatic brain injury;

This invention provides an environmentally friendly method for preparing the active pharmaceutical ingredient butylphthalide. Using butylphthalide as a raw material and water as a solvent, the active pharmaceutical ingredient butylphthalide is prepared in a simple, environmentally friendly one-pot process via hydrolysis with sodium hydroxide solution, acidification with sulfuric acid solution, and reductive lactone formation catalyzed by an iridium catalyst. After simple extraction, drying, and concentration, a product with a purity greater than 99% according to 1H NMR spectroscopy and a yield greater than 90% is obtained. The synthetic method provided by this invention features concise reaction conditions and steps, simple operation, is environmentally friendly, has high synthesis efficiency, and facilitates separation and purification. It has promising industrial applications and plays a positive role in organic synthesis, pharmaceutical production, and fine chemicals.