19 results about "Tetralones" patented technology

The invention belongs to the field of organic synthesis, and discloses tetrahydronaphthalene-1-ketone as well as a preparation method and application thereof.The tetrahydronaphthalene-1-ketone is obtained by mixing tetrahydronaphthalene, carbon nitride and persulfate in an organic solvent (acetonitrile or dichloromethane) and reacting under the illumination condition of 395-457 nm. The preparation method disclosed by the invention is relatively high in yield, conforms to a green production concept, is environment-friendly, low in cost, simple to operate and high in selectivity, and is expected to be used for industrial production.

The invention relates to the technical field of medicine synthesis, and particularly discloses an aminoguanidine tetralone derivative and a structural general formula of the aminoguanidine tetralone derivative. The invention also discloses a preparation method and application of the derivative. The aminoguanidine tetralone derivative has a good inhibiting and killing effect on staphylococcus aureus and can be used for preventing and treating diseases caused by staphylococcus aureus infection.

The invention provides a method for performing defluorination cyclization reaction on perfluoroalkyl tetralone and benzylamine under the promotion condition of potassium phosphate, and a series of polyfluoroalkyl pyridine compounds are synthesized. According to the reaction, six C (sp3)-F bonds of three carbon sites on a perfluoroalkyl chain are selectively activated, accurate synthesis of the fluoroalkyl-containing substituted pyridine compound is achieved, and the method has the advantages of being mild in condition, good in functional group tolerance, simple in aftertreatment, green in step, low in pollution, high in economic benefit and the like.

The present invention discloses a rapid synthesis method for axially chiral aromatic amine compounds using metal-free catalysis. 1-substituted tetrahydro-2-naphthalenone and a cheap and readily available chiral amine are used as raw materials. Axial chiral aromatic amines are prepared by reaction under the action of a catalyst, and a wide range of substrates can be selected. Compared with traditional synthesis methods, the method of the present invention uses metal-free catalysis, has the advantages of simple conditions, convenient operation, relatively high yield, low environmental pollution, and ease of industrial production. The synthesis method of the present invention can simultaneously obtain two axially chiral aromatic amine compounds, and the yield range is 20%-70%.

The invention discloses an efficient synthesis method of a polyketone compound penicilfuranone A. The structural formula of the compound is # imgabs0. According to the invention, a tetralone skeleton with a tertiary alcohol structure is rapidly constructed through a Set-Aldol tandem cyclization reaction catalyzed by N-heterocyclic carbene (NHC), and efficient preparation of a natural product penicilfuranone A is realized. The synthesis method provided by the invention is novel, efficient and economical, reagents used in the whole synthesis process can be commercially purchased at low price, and the reaction strategy is also suitable for synthesis of intermediates or derivatives, so that a foundation is laid for structural modification, structure-function relationship research, new drug development and large-scale preparation of the intermediates or derivatives.

The application provides a method for defluorocyclization reaction of perfluoroalkyl tetrahydronaphthalenone and amidine compound and cobalt-1,3-dicarbonyl complex under the promotion condition of cesium carbonate, and a series of fluorine alkyl substituted furan quinazoline compounds are synthesized. The strategy is free from the dependence on multi-step pre-functionalization and transition metal catalysis in the traditional synthesis path. In the reaction process, six carbon-fluorine bonds at three perfluoroalkyl carbon sites of the polyfluoroalkyl ketone are continuously broken, five carbon-carbon / carbon-nitrogen / carbon-oxygen bonds and two heterocycles are constructed through one-pot method, the accurate synthesis of the fluorine alkyl substituted furan quinazoline compound is realized, and the method has the characteristics of mild condition, good functional group tolerance, simple post-treatment, green step, low pollution and high economic benefit; and the obtained compound shows certain inhibition activity on human malignant melanoma (A-375) cells.

The invention relates to a preparation method of 7-methoxynaphthalene acetonitrile. The preparation method comprises the following steps: reacting 7-methoxy-1-tetralone with copper bromide under the action of a catalyst to generate 7-methoxy-2-bromo-1,2,3,4-tetralone; reacting 7-methoxy-2-bromo-1,2,3,4-tetralone under the catalysis of a heteropoly acid to obtain 7-methoxy-1,4-dihydronaphthalone; and directly condensing 7-methoxy-1,4-dihydronaphthalone with cyanoacetic acid in the presence of benzylamine and heptanoic acid to obtain 7-methoxynaphthalene acetonitrile. The preparation method of the catalyst comprises the following steps: mixing carrier particles and a metal salt solution, adjusting the pH to alkaline, washing, drying, immersing in a sulfuric acid solution, filtering, and then roasting to obtain the catalyst. The carrier particles are aluminum oxide or silicon dioxide, and the metal salt solution is a salt solution of Zr, Ti or Sn. The method reduces the difficulty of purification, improves the yield and purity, and reduces the cost.

The invention discloses 1, 1-bis (4-hydroxybenzene)-tetrahydronaphthalene as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. The invention provides a preparation method of 1, 1-bis (4-hydroxybenzene)-tetrahydronaphthalene, and the preparation method comprises the following steps: carrying out a melting reaction on 1-tetralone and phenol in the presence of an inert gas atmosphere and a catalyst, and carrying out separation and purification to obtain the 1, 1-bis (4-hydroxybenzene)-tetrahydronaphthalene. According to the preparation process provided by the invention, the homogeneous phase characteristic of a melting reaction system is utilized, reactants are in full contact and are subjected to directional condensation, the product can be purified only through simple separation and purification, the synthesis and purification difficulty of the product is greatly reduced, the synthesis yield can reach 85% or above, and the purity reaches 88% or above. The large-scale preparation of the 1, 1-bis (4-hydroxybenzene)-tetrahydronaphthalene is successfully realized for the first time, the molecular design space of a polyaryletherketone high-performance material is widened, and the method has a wide application prospect in integrated circuit boards.

This invention discloses a novel chiral sulfinamide monophosphine ligand based on an oxanthracene skeleton, its preparation method, and its application. The preparation method includes the following steps: (1) oxanthracene is subjected to a substitution reaction with RBr in the presence of sodium hydride and a solvent to obtain intermediate 1; (2) intermediate 1 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a halogen to obtain intermediate 2; (3) intermediate 2 is subjected to halogen-metal exchange with isopropylmagnesium chloride in the presence of a solvent, followed by the addition of diphenylphosphine chloride to undergo a substitution reaction to obtain intermediate 3; (4) intermediate 3 is subjected to lithium halide exchange with butyllithium in the presence of a solvent, followed by the addition of a compound to react in the presence of a Lewis acid to obtain the chiral sulfinamide monophosphine ligand. The chiral sulfinamide monophosphine ligand prepared by this invention can be used to prepare chiral α-alkyl-α-benzyltetrahydronaphthone compounds with high yield and ee value.

The invention relates to the technical field of organic synthesis, in particular to a method for asymmetrically synthesizing strigolactone derivatives GR24 through an enzyme-chemical method. The preparation method comprises the following steps: mixing alpha-tetralone with anhydrous tetrahydrofuran, and adding a lithium diisopropylamide solution for mixing reaction; 2-methyl bromoacetate and 1, 3-dimethyl-2-imidazolidinone are added for a reaction, and S3 is obtained; mixing the S3, NAD < + >, isopropanol and a buffer solution, and reacting by using a novel enzyme catalyst to obtain S4; mixing and reacting the HCO2Et solution in S4 with potassium tert-butoxide to obtain a crude product; the DMF solution of the crude product, potassium carbonate and the DMF solution of 5-bromo-3-methylfuran-2 (5H)-ketone are subjected to a reaction, and GR24 is obtained. The creativity of the method is mainly reflected in the application of the novel enzyme catalyst, and by using the novel enzyme catalyst, the reaction efficiency and selectivity are improved, the cost is reduced, the environmental pollution is reduced, and the application prospect is wide.

The application discloses four kinds of tetra-cyclic compounds of four amino acids which selectively inhibit arachidonic acid (AA), and discloses a preparation method of the tetra-cyclic compounds and application of the tetra-cyclic compounds in treating arterial thrombosis diseases. Experiments prove that the arachidonic acid selective inhibitor has good anti-arterial thrombosis effect. Thus, the application provides an effective technical means for resisting arterial thrombosis.

The invention relates to novel tetralone derivatives as GPER pathway modulators, and to their use in particular for nociception control.

The application provides a novel preparation method of tetrahydronaphthone compounds, and comprises the following steps: 1,6-alkynyl compounds are reacted with water under the synergistic catalysis of a transition metal and an amine nucleophile to generate tetrahydronaphthone compounds. The above synthesis method is simple and fast in preparation process, the catalyst is low in price, and the substrate has wide applicability, and therefore, the method is expected to be used for industrial production.

The present invention relates to novel tetralone derivatives as modulators of the GPER pathway, and their application in particular to the control of nociception. Abstract figure: Figure 13

The present application is related to a process for preparing 1-tetralone compounds such as compounds of Formula I by reacting a,|3-unsaturated cyclic ketones that comprise two available hydrogens on the y carbon to the carbonyl with acrolein derivatives with heating in the presence of a suitable organic acid, a suitable organic amine base and suitable inert solvent. For example, the 1-tetralone compound is a tetralone derivative of abscisic acid (ABA).

The present invention discloses a metal-free synthesis method for aromatic amine compounds. Cyclohexenone or tetrahydro-2-naphthone compounds and various amines are used as raw materials. In the presence of a catalyst, a wide range of substrates can be selected. Compared with traditional synthesis methods, the method has the advantages of simple conditions and convenient operation because no metal catalyst is used. The yield is also relatively high (up to 90%), the pollution to the environment is small, and the method is easy to industrialize.

The present invention provides fluoroalkoxyalkylenedihydroimidazo[5,1-d]tetradinone compounds and related compounds, pharmaceutical compositions, and their use in the treatment of cancer.

The present application belongs to the technical field of biotechnology and enzyme engineering, and particularly relates to a lysine amine dehydrogenase mutant and application thereof in synthesis of chiral amine compounds. Specifically, the present application takes lysine amine dehydrogenase LE-AmDH-v1 (i.e. LysEDH F173A) from Geobacillus stearothermophilus (Vasilis Tseliou et al, 2019) as a female parent, and through semi-rational modification and site-directed mutation, a lysine amine dehydrogenase mutant with improved catalytic performance, significantly improved soluble expression and improved temperature stability is screened, and the lysine amine dehydrogenase mutant is used as a catalyst, so that cheap and easily available alpha-tetralone can be used as a substrate to synthesize chiral R-1-tetralylamine with high stereoselectivity and high conversion rate, and therefore the present application has good practical application value.

The present application relates to the field of chemical synthesis, and specifically discloses a method for synthesizing 3-bromo-1-phenylnaphthalene. The method comprises the following steps: preparing a bromobenzene Grignard reagent using bromobenzene as a raw material; 1-tetralone reacts with a bromobenzene Grignard reagent to generate a mixture of 1-phenyl-1-hydroxytetralin and 1-phenyl-3,4-dihydronaphthalene; a mixture of 1-phenyl-1-hydroxytetralin and 1-phenyl-3,4-dihydronaphthalene undergoes a bromination reaction with N-bromosuccinimide in the presence of an initiator to generate 3-bromo-1-phenylnaphthalene. The method for synthesizing 3-bromo-1-phenylnaphthalene of the present application has the advantages of low cost, short route, simple operation, high product yield and purity.