10 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 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 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.

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 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 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.