34 results about "Indolecarboxaldehyde" patented technology

The invention relates to a new class of indole derivatives and a preparation method thereof. The method comprises the steps of: taking indole-3-carboxaldehyde derivatives and isobutyryl hydrazine as raw materials, and partially or wholly introducing groups with anticancer activities such as -OCH3, -C=N-NH-C=O, and the like to proper positions of the indole derives through chemical reaction to obtain a series of indole compounds containing multiple functional groups. The technology is with simple operation, requires mild reaction conditions and has a high yield. Furthermore, the compounds have good biological activities, can be used for tumour therapy and have a wide application prospect in a pharmaceutical field.

The invention discloses an α-pinene-based cell nucleus fluorescent probe, a preparation method and application thereof. The invention utilizes the natural renewable resource α-pinene derivative myrtleenal as a raw material to condense with 4-methylthiosemicarbazide to generate α-pinene-based thiosemicarbazone; α-pinene-based thiosemicarbazone Cyclize with chloroacetic acid to obtain α-pinenyl thiazolidinone; α-pinenyl thiazolidinone is condensed with 3-indole formaldehyde to obtain α-pinene-based nuclear fluorescent probe, which can The cell nucleus is specifically imaged in situ and emits green fluorescence under 390nm ultraviolet light irradiation. As a new type of cell nucleus fluorescent probe, it has a good application prospect.

The invention discloses the application of indole-3-formaldehyde and its derivatives in preventing and treating plant diseases caused by plant pathogenic fungi. The invention provides the application of indole-3-carboxaldehyde or its derivatives or pharmaceutically acceptable salts in the prevention and treatment of plant diseases caused by phytopathogenic fungi, or in the preparation of pesticides for the prevention and control of plant diseases caused by phytopathogenic fungi Or application in biocontrol agents. The present invention proves that indole-3-formaldehyde and derivatives thereof have good inhibitory activity to phytopathogenic fungi through the measurement of bacteriostatic activity, and it has a good inhibitory effect on the growth and sexual coordination of phytopathogenic fungi, which can inhibit The formation of dikaryotic mycelia prevents phytopathogenic fungi from normally infecting plants, thereby effectively inhibiting the occurrence of plant fungal diseases, providing a reference for green prevention and control of plant diseases caused by phytopathogenic fungi, and has broad application prospects.

The invention discloses a 4-position chloroindole compound and a preparation method thereof. Various N-protected indole-3-formaldehydes and N-chlorosuccinimide (NCS) were used as reaction substrates to prepare 4-position chloroindole compounds. The reaction yield can reach moderate to excellent, the reaction chemoselectivity and regioselectivity are excellent, the reaction conditions are mild, and the substrate has a wide range of application; it is easy to operate, low in cost, less in side reactions, high in product purity, and easy to separate Purification and can be applied to large-scale preparation, so the resulting product has a very good application prospect in the field of biomedicine.

The invention discloses a synthetic method for indole-3-carboxaldehyde compounds. The synthetic method comprises the following steps: (1) using anhydrous dimethylformamide as a solvent, and slowly adding phosphorus oxychloride, and agitating for 30 minutes at 0 to 5 DEG C so as to obtain a Vilsmeier agent; (2) using the anhydrous dimethylformamide as the solvent, adding 2-methylaniline compounds shown in the formula (I), dropping the Vilsmeier agent prepared in step (1) at 0 to 5 DEG C, agitating for 1 to 2 hours at room temperature after dropping, and heating for reflux to react for 5 to 8 hours; and (3) cooling after the reaction, adding a saturated sodium carbonate solution to adjust to alkalinity, filtering the precipitated solid, an drying to obtain a product, and finally recrystallizing the product to obtain the indole-3-carboxaldehyde compounds as shown in the formula (II). The method disclosed by the invention is simple to operate, and low in cost of production, and is not only suitable for small-scale preparation in a laboratory, but also suitable for large-scale industrial production.

The invention discloses a fluorescent probe compound based on a purine parent, and also discloses a preparation method of the fluorescent probe compound and its application in detecting palladium ions and copper ions. In the present invention, a purine ring and 3-indole formaldehyde are used as fluorescent groups, and hydrazine hydrate is used as a linking group to synthesize a fluorescent probe compound based on a purine parent body, and the resulting fluorescent probe compound has high selectivity to copper palladium ions , high detection sensitivity, so it has the advantages of stable structure, good selectivity, high sensitivity and low toxicity; the preparation method of the invention has simple steps, easy-to-obtain raw materials, and the obtained product is solid powder, which is easy to store.

The present invention relates to the high enantioselectivity synthesis of indole skeleton-containing spiro compound (R)-1-aryl-1'H-spiro[dihydroindole-3,3'-spiro[dihydroindole-3,3'- The invention discloses a preparation method of oxazolo[3,4-α]indole]-1',2 diketone derivative and its good biological activity application. The general structural formula is as follows: where R 1 is a substituent for indole‑2‑carbaldehyde, R 2 is a substituent of indole-2,3-dione, R 3 are different protecting groups for indole‑2,3‑dione, methyl, benzyl, triphenylmethyl. Indole skeleton chiral spiro compound (R)-1-aryl-1'H-spiro[ Indoline-3,3'-oxazolo[3,4-α]indole]-1',2 dione derivatives, the derivatives of which have good universality and excellent yield up to 98%, Enantioselectivity up to 99% and good biological activity.

The invention provides a method for preparing indole-3-formaldehyde, comprising the following steps: (1) inoculating Vibrio New Caledonia CGJ02-2 into LB liquid medium for cultivation, and centrifuging to remove bacteria after the cultivation body, harvest the fermentation supernatant; (2) extract the fermentation supernatant with an organic solvent, concentrate the organic phase under reduced pressure to obtain a crude extract; (3) separate the indole-3-formaldehyde from the obtained crude extract . In the present invention, the indole-3-formaldehyde is produced by a microbial fermentation method, and a large amount of indole-3-formaldehyde can be obtained only by cultivating the microorganisms with a simple culture medium. The method of the invention is not only low in cost, but also environmentally friendly than chemical synthesis. The in vitro enzyme activity test of indole-3-formaldehyde shows that it has strong xanthine oxidase inhibitory activity, and has great development potential and application prospects in the treatment of hyperuricemia and gout.

The invention discloses a metabolomics-based chilled meat freshness marker and a screening and prediction model fitting method and application thereof. The markers include indole-3-formaldehyde, uridylic acid, phenylthiouric acid, gluconic acid, tyramine, serine-phenylalanine. The prediction model is: Y=3.964+1.97E ‑7 X 1 ‑4.22E ‑7 X 2 ‑3.37E ‑7 X 3 +8.80E ‑8 X 4 +1.26E ‑8 X 5 ‑5.57E ‑7 X 6 , This method uses Agilent 1290 UHPLC tandem Q Exactive Orbitrap high-resolution mass spectrometry, which has higher resolution, can detect more substances more accurately, and can more comprehensively elucidate the metabolism of chilled chicken during storage. product, the results obtained are more reliable.

The invention provides an indole ethylene-substituted quinoline derivative with a structure shown in a formula (I). A series of indole ethylene-substituted quinoline derivatives with the structure shown in the formula (I) can be obtained by introducing indole-2-formaldehyde to quinoline site as a parent and selecting special substituent groups. Proofed by experiment results, the indole ethylene-substituted quinoline derivative with the structure shown in the formula (I) has the advantages that when the indole ethylene-substituted quinoline derivative is used as a fluorescent probe, the action force with G-quadruplex is stronger, and the action with other secondary nucleic acids is weaker; specifically, when the fluorescent probe is mixed with different secondary nucleic acids, and the nucleic acid is the G-quadruplex, the specific action with probe molecules can produce the change of fluorescent spectrum; when the secondary structure of the nucleic acid adopts the other structure, the obvious signal change is not produced.

The invention discloses a near-infrared two-photon photosensitive dye SBOPI and its preparation method and application. The near-infrared two-photon photosensitive dye SBOPI comprises a push-pull electronic conjugated structure of thiophene-fluoroboron dipyrrole and indole and a lysosome target site. The preparation method of the near-infrared two-photon photosensitizing dye SBOPI is prepared by reacting iodothiophene-fluoroboridipyrrole SBOP and 1-(2-morpholinoethyl)-1H-indole-3-formaldehyde. The application of the near-infrared two-photon photosensitizing dye SBOPI is that under near-infrared light irradiation, the near-infrared two-photon photosensitizing dye SBOPI can efficiently release singlet oxygen, inhibit tumor cell migration, and promote tumor cell apoptosis. As a near-infrared two-photon photosensitizer and fluorescent dye with excellent performance, it has been widely used in near-infrared fluorescence imaging, fluorescence sensing, fluorescent labeling, and two-photon photodynamic therapy.

The invention relates to a method for separating and purifying methyl p-hydroxybenzoate and 3-indole formaldehyde from the stems and leaves of Trichosanthes chinensis. The stems and leaves of Trichosanthes chinensis are used as raw materials, and the following steps are carried out: (1) Crude extracts of stems and leaves of Trichosanthes chinensis (2) Extraction; (3) Separation and purification of reversed-phase C18 column; (4) Separation and purification of semi-preparative high-performance liquid chromatography: separation and purification by semi-preparative high-performance liquid chromatography, the mobile phase is methanol-water, Two high-purity components were obtained, which were identified as methyl p-hydroxybenzoate and 3-indole carboxaldehyde. The technological process is green and environmentally friendly, has no serious harm to the environment, and has low overall cost.

The invention discloses a 4-position iodoindole compound and a preparation method thereof. Various N-protected indole-3-formaldehydes and N-iodosuccinimide (NIS) were used as reaction substrates to prepare 4-position iodoindole compounds. The reaction yield can reach moderate to excellent, the reaction chemoselectivity and regioselectivity are excellent, the reaction conditions are mild, and the substrate has a wide range of application; it is easy to operate, low in cost, less in side reactions, high in product purity, and easy to separate Purification and can be applied to large-scale preparation, so the resulting product has a very good application prospect in the field of biomedicine.

The invention discloses a compound with antibacterial activity in mulberry plants, a preparation method and its application in the preparation of antibacterial drugs, belonging to the field of phytochemistry. The present invention uses mulberry as raw material, dried and pulverized, soaked and extracted with an organic solvent, and then the extracts are combined, filtered and concentrated to obtain a mulberry extract; then extracted with n-butanol and methylene chloride, the The dichloromethane extract is concentrated under reduced pressure to obtain the dichloromethane extract extract; the dichloromethane extract extract is dissolved, mixed and then subjected to silica gel column chromatography, and the eluent is concentrated and then normal phase silica gel chromatography column (200 ~300 mesh) separation and purification, and gel column chromatography separation and purification to obtain the pure product of the target indole-4-formaldehyde. The product of the present invention has stronger antibacterial effect, and the minimum inhibitory concentration MIC value of described indole-4-formaldehyde compound to methicillin-resistant Staphylococcus aureus is 128 μ g / mL, and its antibacterial effect is far better than clindamylate hydrochloride Mycin (MIC=1024 μg / mL).