22 results about "Stereocenter" patented technology

Described is a compound for substituting amino acids of proteins or peptides, wherein the compound has the formula (1)wherein the stereocenter C1* represents CH that either results in the D- or L-form of the compound of formula (1); A− is a negatively charged ion compensating the positive charge; X1 is H or an amine protecting group; X2 is OH, an ester residue or an amide residue or an activated carboxylic acid derivate to be used for the formation of an amide bond; Y1, Y2 and Y3 are independently from each other a C1-C6 alkyl, and Z1 and Z2 are independently from each other a nucleobase, a C1 to C16 alkyl group, an aromatic residue or a heteroaromatic residue, wherein the aromatic residue or the heteroaromatic residue contains one 5, 6, or 7-membered ring or two condensed 5, 6, or 7-membered rings sharing two carbon atoms, wherein the aromatic residue or the heteroaromatic residue can be substituted by a linear or branched C1 to C16 alkyl group and / or a further aromatic group. Furthermore, a method for preparing this compound and proteins and peptides containing this compound are disclosed.

The present invention relates to the technical field of circularly polarized luminescent material preparation, and in particular to a spirochiral tetradentate platinum(II) complex-based circularly polarized luminescent material based on pyridine-carbazole-phenylcarbene and a derivative structure thereof, and an application thereof. The provided complex molecule autonomously induces, by means of a remote stereocenter-containing fragment in chirally substituted pyridine, an entire tetradentate ligand to coordinate with a metal ion in a less sterically hindered manner, so as to form an optically pure spirochiral metal complex-based circularly polarized luminescent material. Such spirochiral metal complex-based circularly polarized luminescent material does not require chiral resolution, has high molecular thermodynamic stability, and has important applications in circularly polarized light-emitting components.

The invention discloses a three-dimensional covalent organic framework material based on an adamantane three-dimensional center, a preparation method of the three-dimensional covalent organic framework material and application of the three-dimensional covalent organic framework material in hydrogen storage, and belongs to the technical field of hydrogen storage materials and preparation of the hydrogen storage materials. The hydrogen storage performance of the COF hydrogen storage material is further improved. According to the invention, TFPA and diamino monomers containing different numbers of benzene rings are taken as raw materials, covalent organic framework materials with different chain link lengths and a three-dimensional space network structure are constructed, the material has a dia topological structure, the three-dimensional structure enables pore channels to be complex, and the material has obvious advantages in gas adsorption. Test results show that when adamantane is taken as the three-dimensional center of the three-dimensional covalent organic framework material, the interpenetration degree is increased along with the increase of the length of the chain link, and different interpenetration structures have different hydrogen adsorption effects. When an organic chain link is short, a non-interspersed structure is more likely to be formed, at the moment, a higher specific surface area and more exposed active sites are achieved, and hydrogen storage is more facilitated.

The invention relates to the field of chemical synthesis, and discloses a method for constructing a full-alkyl quaternary carbon stereocenter through stereospecific conversion of chiral tertiary alcohol. The method successfully solves the industrial problem that the peralkyl quaternary carbon center is difficult to construct with high stereoselectivity due to huge steric hindrance and lack of electron difference, the process shows excellent stereospecificity and chemical selectivity, the ee value of the product is as high as 98%, the dr value is superior to 20: 1, and meanwhile, the excellent yield of 90% or above is kept; besides, according to the scheme, the substrate is wide in universality and can be compatible with various chemical small molecule substrates of different structures, the used reagents such as triethyl aluminum and KHMDS are cheap and easy to obtain, operation is easy and convenient, and a simple and efficient stereospecific conversion strategy with industrial application potential is provided for synthesis of complex drug intermediates.

The application provides a chiral spiro compound and a preparation method and application thereof, and belongs to the technical field of organic synthesis. The chiral spiro compound is obtained by mixing spiro olefin, alkyl iodide, cobalt salt, a chiral ligand, an organic solvent, a reducing agent and an alkaline substance to perform a hydrogen alkylization reaction. A cobalt-catalyzed stereodivergent asymmetric synthesis method is disclosed, high-efficiency preparation of a spiro compound containing 1,3-non-adjacent stereogenic centers is realized by ligand regulation, and the product has excellent biological activity. The method has wide substrate compatibility and high selectivity, and provides a new way for drug development.

The application discloses a method for efficiently synthesizing a full-carbon quaternary carbon stereogenic center compound by using nickel-catalyzed asymmetric amination. The method comprises the following steps: under the catalysis of a nickel catalyst, an alpha,alpha-dimethylamide compound is reacted with an O-benzoyl hydroxylamine compound in an organic solvent in the presence of an inorganic base, an additive, a molecular sieve and binaphthyl in a 60 DEG C environment for 24 hours or 36 hours, and then the amination product is separated by thin layer silica gel plate chromatography purification; the method has the advantages of mild reaction condition, cheap and easily obtained catalyst, simple process and convenient operation; the amine group can be directly introduced into the alpha,alpha-dimethylamide substrate, and the amination product containing the full-carbon quaternary carbon stereogenic center can be obtained with high stereoselectivity.

The present application belongs to the technical field of tumor targeted therapy, and particularly relates to a small-molecule compound targeting EGFR and application thereof. The present application provides a small-molecule compound targeting EGFR or a pharmaceutically acceptable salt thereof. The spiro alkaloid compound provided by the present application contains an arylated four-membered stereocenter heterocyclic framework, including a helical heterocycle, a distributed heterocycle, a fused heterocycle and a bridged heterocycle, which can be applied to preparation of an EGFR-targeted inhibitory drug.

The application belongs to the technical field of organic synthesis, and particularly relates to an alpha-stereocenter 1,4-dicarbonyl compound and a preparation method thereof, a derivative of the alpha-stereocenter 1,4-dicarbonyl compound and a preparation method thereof. The application provides that the alpha-stereocenter 1,4-dicarbonyl compound can be prepared by taking a gamma-hydroxy enone compound as a reaction raw material and taking a Lewis acid and a base as co-catalysts under normal pressure. The preparation method provided by the application is simple in operation, wide in application range, low in cost of raw materials, high in atom economy, and meets the demand of green chemistry development. The alpha-stereocenter 1,4-dicarbonyl compound prepared by the preparation method provided by the application has high yield and purity, and has good economic benefits and application prospect.

The application discloses a synthesis method of a multi-halogenated alkaloid Caulamidines and Isocaulamidines, and the synthesis method comprises the following steps: taking a thujanol derivative as raw material, and performing a series of synthesis and separation operations, and then performing an asymmetric Meerwein- Eschenmoser-Claisen rearrangement to build C10 and C23 continuous key stereogenic centers, and finally realizing a 6-exo-dig / 6-exo-tet amine / cyan group tandem cyclization reaction, so that the multi-halogenated alkaloid Caulamidines and Isocaulamidines are obtained. The synthesis method can be amplified, and can be used to solve the 'drug source bottleneck' problem of natural samples and homologues thereof in future drug research.

The invention relates to silicon-containing three-dimensional center silacyclohexenone skeleton borane as well as a preparation method and application thereof, the silicon-containing three-dimensional center silacyclohexenone skeleton borane has a structural formula as shown in a formula (I), and substituent groups R1 and R2 are respectively aryl or alkyl. According to the synthesis method of the compound, metal copper is used as a catalyst, and under the combined action of a chiral phosphine ligand and alkali, silacyclohexenone and a diborane compound are subjected to a hydroboration reaction to synthesize the compound. The synthesis method provided by the invention is simple to operate, mild in reaction condition, high in substrate universality, high in product yield and high in enantioselectivity. The synthesized compound is an important silicon-containing stereo center heterocyclic compound and can be widely applied to various fields of organic synthesis, medicine, material chemistry and fine chemical engineering.

The invention discloses a 1, 2, 4-triazoline derivative containing trifluoromethyl and a preparation method of the 1, 2, 4-triazoline derivative, and belongs to the technical field of organic synthesis. Under the action of alkali, difluoromethyl bromohydrazone is used as a 1, 3-dipole and 3, 3, 3-trifluoro-2-(N-aryl) iminopropionic acid ethyl ester is used as a dipole, synthesis of difluoromethyl substituted 1, 2, 4-triazoline is smoothly realized through [3 + 2] cycloaddition reaction between difluoromethyl bromohydrazone and 3, 3, 3-trifluoro-2-(N-aryl) iminopropionic acid ethyl ester, meanwhile, trifluoromethyl is introduced into a 1, 2, 4-triazoline molecule, and a 3, 3, 4-triazoline derivative is provided. The invention relates to a synthetic method of 1, 2, 4-triazoline substituted by 1, 5-difluoroalkyl. In addition, through [3 + 2] cycloaddition reaction of halogenated hydrazone containing no fluoroalkyl and ethyl 3, 3, 3-trifluoro-2-(N-aryl) iminopropionate, a new method is provided for synthesis of the 1, 2, 4-triazoline compound substituted by trifluoromethyl and having a three-dimensional center.

The present disclosure is directed to an analytical method for determining the concentration of a chiral alcohol in a sample and one or both of (i) the absolute configuration of the chiral alcohol in the sample, and (ii) the enantiomeric and / or the diastereomeric composition of the chiral alcohol in the sample. The present disclosure is also directed to an aryl or heteroaryl sulfonamide probe having the structure according to formula (I): Formula (I), where Ar, R1, R2, and n are as described herein, as well as to a kit for carrying out the analytical method described herein.

The present invention relates to stereoisomeric phosphatidyl oligoglycerols having a predetermined configuration in at least three stereocenters, in particular to phosphatidyl oligoglycerols as a single stereoisomer. The present invention also relates to a stereospecific method for providing a stereospecific phosphatidyl oligoglycerol having a predetermined configuration in at least three stereocenters, in particular for providing a phosphatidyl oligoglycerol as a single stereoisomer, and to a liposome comprising the novel stereoisomeric phosphatidyl oligoglycerol, in particular, liposomes comprising novel stereoisomeric phosphatidyl oligoglycerols as a single stereoisomer.

The application discloses a kind of based on attention mechanism correction Kuroshio front stereo center line reconstruction method, including the following steps: (1) based on Soble algorithm obtains three-dimensional Kuroshio front area;(2) extract Kuroshio initial stereo center line;(3) using the characteristics of flow field and sea surface height anomaly field to remove outliers;(4) using attention mechanism to adjust correction field weight.The application first uses Soble algorithm to obtain the initial stereo center line of Kuroshio front, then uses the characteristics of flow field and sea surface height anomaly field to correct the stereo center line, and introduces attention mechanism to adjust the correction field weight, realizes the stereo reconstruction of Kuroshio front center line, and effectively describes the vertical swing characteristics of Kuroshio axis, provides an effective tool for the description of Kuroshio front three-dimensional characteristics.

The application belongs to the technical field of organic synthesis, and particularly relates to an amino nitrile compound with a remote chiral center and a preparation method and application thereof. The nickel-hydrogen catalytic asymmetric hydrogenation reaction provided by the application is realized through non-covalent pi-pi interaction between a cyano group in an olefin substrate and a chiral bisoxazoline ligand. The method not only realizes efficient and high-selectivity conversion of various olefin substrates and amine electrophilic reagents, but also is compatible with secondary alkyl amine electrophilic reagents, amide electrophilic reagents and benzisoxazole electrophilic reagents, thereby providing a reliable way for synthesizing chiral amino nitrile compounds (formula I) with a remote (beta-, gamma- and delta-) stereogenic center and various structures.

Methods, compositions, and kits are provided for synthesizing bioactive chromane, the method including: constructing a tertiary ether stereocenter enantioselectively by catalyzed alkynylation of a substituted chromenone to obtain a chromanone; reducing alkyne and ketone in the chromanone to obtain a chroman; and converting ester to methyl group thereby obtaining chromane.

The application discloses a synthesis method of alpha-substituted arylacetamide compounds. The method is based on a light-driven iron-catalyzed decarboxylative arylalkylation reaction system of ligand-metal charge transfer (LMCT) mechanism, can efficiently couple readily available N-arylacrylamide with commercial and various carboxylic acids, and can prepare a series of alpha-substituted arylacetamide compounds containing acyclic quaternary carbon stereogenic centers with high chemical selectivity. The system is suitable for various carboxylic acid substrates, including primary, secondary and tertiary alkyl carboxylic acids and complex biological active carboxylic acid molecules.

The application discloses a kind of chiral nitrogen a spiro compound and its preparation method and application, specifically related to a kind of chiral nitrogen a spiro compound and its synthesis method, wherein the preparation method includes with metal chiral cobalt (III) complex anion as catalyst, with amine, aromatic aldehyde, alkyne acid and isocyanide as starting material asymmetric Ugi four-component reaction, obtain chiral alpha-amido propargyl amide;The species is deformed under the action of metal (such as Au (I), Ag (I), Sc (III) and the like), and controllable intramolecular Michael addition reaction, finally obtain chiral nitrogen a spiro derivative and nitrogen a spiro fused ring compound with multiple stereogenic centers, the optical purity of obtained compound can be up to 98%ee.The chiral nitrogen a spiro compound and nitrogen a spiro fused ring compound prepared by the application have potential use as a kind of bioactive molecular skeleton, and preliminary antibacterial biological activity test results show that it has certain antibacterial activity to plant pathogenic fungi.

The invention belongs to the technical field of catalyst preparation, and discloses a method for constructing a chiral ferrocene phosphine ligand. According to the invention, a ferrocene phosphine-containing substrate and an imidoium cation salt are used as reaction substrates, and the chiral supramolecular catalyst is accurately regulated and controlled under mild conditions, so that synergistic induction of a phosphine substitution site and an ethylamine group chiral center is realized, and double stereo centers are effectively constructed. The obtained target product has excellent enantioselectivity (ee value is greater than or equal to 96%), is clear and stable in structure, and is suitable for subsequent derivative development of chiral ligands or catalysts. Moreover, the reaction system is mild and safe, the process flow is simple, the catalyst can be recycled, the yield of the target product reaches 90% or above, and the method is green and environment-friendly, has good industrial amplification potential and green synthesis advantages, and provides a brand-new chiral construction strategy for synthesis of the chiral ferrocene phosphine ligand.

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad-spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

The application discloses a preparation method and application of chiral 1,4-dihydroquinoline. The method adopts a chiral Ir-SpiroPAP catalyst to perform asymmetric catalytic hydrogenation on 4-substituted-quinoline-3-carboxylate, and a series of chiral 1,4-dihydroquinoline with high enantioselectivity is obtained. The reaction has a wide substrate application range, the catalyst consumption can be as low as 0.05 mol%, and the obtained chiral 1,4-dihydroquinoline has an enantioselectivity as high as 99% ee. The optical active 1,4-dihydroquinoline with one stereogenic center is used as a key chiral raw material and applied to asymmetric synthesis of Melatonin MT2 receptor and ABCB1 inhibitor respectively.

The invention discloses a three-dimensional covalent organic framework material based on double three-dimensional centers, a preparation method of the three-dimensional covalent organic framework material and application of the three-dimensional covalent organic framework material in hydrogen storage, and belongs to the technical field of hydrogen storage materials and preparation of the hydrogen storage materials. The invention aims to further improve the gas adsorptivity of the existing COF hydrogen storage material. According to the invention, two tetrahedron construction base blocks are directly condensed to construct the three-dimensional covalent organic framework material with the non-interpenetrating dia topological structure, and the COF shows good crystallinity and high BET specific surface area. By utilizing a higher specific surface area brought by a non-interpenetrating structure and fully exposed high-energy adsorption sites as well as high-density three-dimensional central units and high-energy adsorption sites provided by imine bond nitrogen atoms in a framework, the hydrogen adsorption performance is excellent, and a contribution is made for improving the hydrogen adsorption capacity.