53 results about "Spiro compound" patented technology

This invention discloses a chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups, with the following structural formula: The preparation includes the following steps: 1. Sequentially adding a metal catalyst, a chiral ligand, a base, indigo-derived trifluoromethylimine ylide, and 3-methylene β-lactam, followed by the addition of an organic solvent to obtain a mixture. The mixture is stirred at a reaction temperature of 0℃ to 50℃. 2. After the reaction is complete, the chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups is obtained through post-processing. The chiral [oxyindole-pyrrolidine-β-lactam] bispirocyclic compound containing trifluoromethyl groups prepared in this application lays a material foundation for in-depth drug activity research based on new drug development.

The invention discloses a nitrogen-containing spiro compound crystal form and a preparation method and application thereof. The invention provides a crystal form I of a nitrogen-containing spiro compound as shown in a formula A. The crystal form I of the nitrogen-containing spiro compound is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 2 theta angle has diffraction peaks at 5.67 + / -0.20 degrees, 11.37 + / -0.20 degrees, 16.69 + / -0.20 degrees, 17.32 + / -0.20 degrees and 19.73 + / -0.20 degrees. The invention provides a crystal form II of a nitrogen-containing spiro compound as shown in a formula A. The crystal form II is radiated by Cu-K alpha, and an X-ray powder diffraction pattern expressed by a 20 angle has diffraction peaks at the positions of 11.32 + / -0.20 degrees, 11.70 + / -0.20 degrees, 11.93 + / -0.20 degrees, 18.03 + / -0.20 degrees, 18.81 + / -0.20 degrees and 19.17 + / -0.20 degrees. The crystal form of the nitrogen-containing spiro compound has good stability and complement factor D inhibitory activity, has a good inhibitory effect on rabbit red blood cell hemolysis, and has high in-vivo exposure and high oral bioavailability.

The invention relates to a compound synthesis technology, in particular to a preparation method of 4-boron-L-phenylalanine. The reaction route of the preparation method is shown in the specification. According to the reaction route of the preparation method of the 4-boron-L-phenylalanine provided by the invention, the L-BPA is prepared by utilizing the boron spiro compound provided by the invention, so that the problems that the existing direct synthesis reaction route is relatively long, the reaction condition is harsh, a chiral catalyst is difficult to obtain and the like can be avoided. L-BPA with higher chemical yield is obtained through a shorter reaction route under mild reaction conditions.

Provided are a crystal form and an amorphous substance of an indoline spiro compound represented by formula (1), and a preparation method therefor and the use thereof. The X-ray powder diffraction pattern of the crystal form comprises characteristic peaks at 5.43±0.20°, 12.28±0.20° and 17.91±0.20° 2θ, as determined by using Cu-Kα radiation; and the XRPD spectrum of the amorphous substance has no obvious diffraction peak. The provided crystal form and the amorphous substance have high purity and good stability, and are beneficial to drug formation.

This invention discloses crystals of nitrogen-containing spiro compounds, methods for producing the same, and uses thereof. This invention provides a type I crystal of a nitrogen-containing spiro compound represented by formula A, in which the powder X-ray diffraction pattern displayed at a 2θ angle using Cu-Kα rays has diffraction peaks at positions 5.67±0.20°, 11.37±0.20°, 16.69±0.20°, 17.32±0.20°, and 19.73±0.20°. This invention also provides a type II crystal of a nitrogen-containing spiro compound represented by formula A, in which the powder X-ray diffraction pattern displayed at a 2θ angle using Cu-Kα rays has diffraction peaks at positions 11.32±0.20°, 11.70±0.20°, 11.93±0.20°, 18.03±0.20°, 18.81±0.20°, and 19.17±0.20°. The nitrogen-containing spiro compound crystals of the present invention exhibit good stability and complement factor D inhibitory activity, good inhibitory effect against rabbit erythrocyte hemolysis, high in vivo exposure levels, and high oral bioavailability. JPEG2026513298000037.jpg5469

The application discloses a chromone spiro compound, a preparation method and application thereof, and the chromone spiro compound is shown as formula I. The compound has selective CDK4 / 6 inhibitory activity, can relieve and / or treat myelosuppression caused by chemotherapy, improve weight loss caused by chemotherapy and improve survival rate, and has good drug safety. The compound has simple preparation method, is convenient for large-scale production, and has great application prospect.

The present disclosure relates to spirocyclic compounds targeting KRAS G12C, pharmaceutical compositions containing the compounds, and methods of using such compounds to treat disease, such as cancer.

The invention discloses a heterocyclic spiro compound and an organic light-emitting device, the heterocyclic spiro compound has a structural general formula as shown in formula (1): in the formula (1), ring A and ring B are independently selected from naphthalene rings or benzene rings; one of X and Y is S, and the other one is O or S; x1, X2 and X3 are respectively and independently selected from N or CR5, and at least one is N; and Ar1, Ar2 and Ar3 are independently selected from a substituted or unsubstituted C6-C30 aryl group, a substituted or unsubstituted C3-C16 cycloalkyl fused C6-C30 aryl group, and a substituted or unsubstituted C2-C30 heteroaryl group. The compound has the advantages of high optical and electrical stability, low driving voltage, high luminous efficiency, long device service life and the like, can be used as a hole blocking material and an electron transport layer material, and is used in OLED luminescent devices.

The present application relates to a nitrogen-containing spirocyclic compound, a pharmaceutical composition and a use thereof. The nitrogen-containing spirocyclic compound has the structural formula represented by formula (I). The compound of the present invention has TRPV3 inhibitory activity and can be used as a TRPV3 antagonist or inhibitor

This invention discloses a spiro compound and its applications, belonging to the field of display technology. The chemical structural formula of the compound is as follows: ; wherein, Ar1 to Ar4 are each independently one of a substituted or unsubstituted C6-C60 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; Ar5, Ar6, and R are each independently one of a substituted or unsubstituted C6-C60 aryl group or a substituted or unsubstituted C3-C30 heteroaryl group; at least one of Z1 to Z3 is N, and the rest are CH; L is one of the following groups: , , ; R1 to R 10 Each of these compounds is independently one of hydrogen, halogen, cyano, nitro, C1-C8 alkyl, C1-C12 alkoxy, substituted or unsubstituted C6-C30 aryl, or substituted or unsubstituted C3-C30 heteroaryl. This compound exhibits excellent electron transport properties, which is beneficial for improving the voltage, efficiency, and lifetime of devices.

This application discloses a synthetic method for azaspirocyclic compounds and their derivatives, comprising reacting an alkynylamine of Formula I, an activator, and an additive to obtain a compound of Formula II. The method described in this application employs a σ-rearrangement and spirocyclic strategy to construct an azaspirocyclic skeleton in one step, overcoming the limitations of traditional multi-step synthesis. Furthermore, this method is characterized by mild conditions, simple operation, and broad functional group compatibility, showing promising application prospects. This application also successfully developed a systematic and diverse derivatization pathway using the core spirocyclic skeleton as a key intermediate, overcoming subsequent modification bottlenecks and providing efficient tools for drug development, natural product simulation, and ligand design. It possesses both academic breakthrough and industrial application potential, promoting the green and precise development of synthetic methodology.

The application belongs to the field of electroluminescence, and particularly discloses a spiro compound, a preparation method thereof, a light-emitting layer, a light-emitting device and a display device, the spiro compound has a structural formula of formula (I) or formula (II): formula (I); formula (II); the structure of D is ; and the structure of A is. The spiro compound provided by the application can be used as a host material of a light-emitting layer, has excellent organic solvent solubility and good film-forming property, and an organic electroluminescent device prepared by using a solution processing technology has balanced carrier transport performance; the structure of the spiro compound can assist light-emitting materials to realize the advantage of relatively aggregated accumulation, and finally can effectively improve the maximum current efficiency of the device and reduce the efficiency roll-off.

This invention provides spirocyclic compounds as inhibitors of KRASG12D mutants, including compounds, pharmaceutically acceptable salts, isotopic variants, tautomers, or stereoisomers thereof. The invention also provides pharmaceutical compositions comprising said compounds and their use in the treatment of cancer.

The present invention relates to a spiro compound, a preparation method therefor and a use thereof. Specifically, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, tautomer, polymorph, solvate, N-oxide, isotopically labeled compound, metabolite or prodrug thereof, a pharmaceutical composition comprising same, a preparation method therefor, and a use thereof in the preparation of drugs for preventing or treating KRAS-mediated related diseases.

The application provides a kind of spiro compound and its application, the structure of the spiro compound is as shown in formula I or formula II, the spiro compound is used for the preparation of spiro compound, and the preparation method comprises the following steps: (1) compound I is subjected to alkylation reaction to obtain compound II;(2) compound II is reacted with benzylamine compound to obtain compound III;(3) compound III is reduced to obtain compound IV;(4) compound IV is mixed with debenzyl reagent to obtain compound V, and then chiral resolution obtains the target spiro compound.The preparation method provided by the application is simple in process operation, raw materials are cheap and easy to obtain, the yield is high, and the process avoids the use of hydrogen and metal catalyst in the debenzyl process through specific process design, greatly reduces the safety and environmental problems, and also reduces the production cost.

The present application provides a new compound having a binding activity with E3 ligase protein CRBN, and a use thereof in the preparation of a medicament for treating a cell abnormal proliferation disease.

The application provides a kind of containing spiro compound and its preparation method and application, belong to organic synthesis technical field.The structure formula of containing spiro compound described in the application is as shown in formula 1, formula 2 or formula 3: formula 1, formula 2, formula 3, in formula 1, formula 2 and formula 3, R2It is selected from hydrogen, deuterium, methyl, methoxy, hydroxyl or halogen, R3It is selected from hydrogen, methyl, halogen, cyano or trifluoromethyl, R4It is selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted benzyl, substituted or unsubstituted phenyl, cyclic alkyl containing double bond or deuterated methyl, R5It is selected from substituted or unsubstituted C1-C4 alkyl, substituted or unsubstituted naphthyl, unsubstituted phenyl or phenyl substituted by one or more of halogen, methyl, tert-butyl, methoxy, alkyl, n is the positive integer of 0-3.The application realizes excellent site selectivity, avoids C3 position side reaction, and has good chemical selectivity.

The application relates to the technical field of chemical synthesis, and provides an oxaspirocyclic compound and an intermediate, and a preparation method of the oxaspirocyclic compound and the intermediate. The preparation method of the oxaspirocyclic compound comprises the following steps: an olefin metathesis reaction of a compound VII occurs in the presence of a catalyst, so that the oxaspirocyclic compound shown in formula VIII is obtained. The preparation method is simple in operation, does not need to use dangerous reagents, is safe and controllable in a reaction process, and is high in yield.

The present disclosure provides a use of a catalyst for catalyzing a reaction of an epoxide compound and carbon dioxide, the catalyst includes a spirocyclic compound including at least one compound of formula (1):where X is selected from nitrogen, or phosphorus; Y is selected from halogens; A and B are independently selected from materials having formulae (a) to (d). Compared with catalysts with a non-spirocyclic structure or Lewis acid metal catalysts, the catalyst including the spirocyclic compound having the structural shown in formula 1 has the advantages of better catalytic effect, more stable performance and longer service life when catalyzing the reaction of the epoxy compounds and carbon dioxide. The present catalyst has both high efficiency and safety, and thus has broad application prospects.

The application relates to a preparation method of a spiro compound, and belongs to the field of pharmaceutical chemistry; the method comprises the following steps: under the condition of a catalyst, raw materials are subjected to a cycloaddition reaction, an amidation reaction and a cyclization reaction to obtain a target compound; the method provided by the application avoids using medicines as raw materials, and high-purity products can be obtained.

The invention relates to a compound synthesis technology, in particular to a boraspiro compound as well as a preparation method and application thereof. The structural formula of the borane spiro compound is shown in the specification. Wherein B is B10 or B11. When the boronspiro compound is used for preparing L-BPA, the problems that an existing direct synthesis reaction route is long, reaction conditions are harsh, and a chiral catalyst is difficult to obtain can be solved. L-BPA with higher chemical yield is obtained through a shorter reaction route under mild reaction conditions.

Provided herein are novel spiro compound derivatives, compositions containing the compounds, and preparation methods and uses thereof. The spiro compound derivatives are compounds represented by Formula (I), or tautomers, stereoisomers, prodrugs, crystal forms, isotopically labeled forms, pharmaceutically acceptable salts, hydrates or solvates thereof. The compounds and compositions of the present disclosure can be used to treat diseases or disorders mediated by USP1, in particular, cancer.

The application discloses a pyrrolidone 2-indoline imine spiro compound with a structure as shown in formula A and a preparation method and application thereof. The preparation method comprises the following steps: taking benzylidene indoline-2-imine as raw material, and reacting with 2-chloro-2-aryl acetyl hydroxylamine under the action of an organic or inorganic base to obtain the target object A. The pyrrolidone 2-indoline imine spiro compound disclosed by the application has certain antibacterial activity, is a novel substance with a novel structure, raw materials are easy to obtain, reaction conditions are mild, green and environment-friendly, and operation is simple.

This invention discloses a spiro(thioxanthracene-9,9'-oxoxanthracene)-2'-boronic acid pinacol ester and its synthetic method, belonging to the field of organic chemical synthesis. Its structural formula is as follows: This invention uses 2-bromothonone as a starting material, reacting it with benzenethiol to synthesize 2'-bromospiro(thioxanthracene-9,9'-oxoxanthracene), and then synthesizing the compound spiro(thioxanthracene-9,9'-oxoxanthracene)-2'-boronic acid pinacol ester via a Suzuki-Miyaura reaction. The synthetic method of this invention is simple to operate, has low production costs, and produces a product with a purity greater than 99.9%, meeting the needs of industrial production and application. It is suitable for industrial production and expands the application of spirocyclic compounds as intermediates in the design and synthesis of organic optoelectronic functional materials.

The invention relates to a spiro compound and application thereof in the field of medicine. Specifically, the invention discloses a compound as shown in a formula (I), an isotope labeled compound thereof, an optical isomer thereof, a tautomer thereof, or a pharmaceutically acceptable salt thereof, or a crystal form or a solvate form of the compound or the pharmaceutically acceptable salt thereof.

The present application relates to a nitrogen-containing spirocyclic compound, a pharmaceutical composition and a use thereof. The nitrogen-containing spirocyclic compound has the structural formula represented by formula (I). The compound of the present invention has TRPV3 inhibitory activity and can be used as a TRPV3 antagoni st or inhibitor

The invention discloses a chiral spiro compound and a preparation and use method thereof. In particular, provided are spiro compounds useful as chiral ligands and chiral organic catalysts, including chiral spiro diamines, chiral spiro aminonaphthol, chiral spiro bis (indole), chiral spiro diaryl diol, chiral spiro diaryl diamines, chiral spiro aminonaphthol, chiral spiro diaryl diindole, and chiral spiro phosphoropentane. Due to molecular shape and three-dimensional orientation, chiral diamine and chiral aminonaphthol molecules provide backbones for use as ligands and organocatalysts.

The invention relates to a spiro compound as well as a preparation method and application thereof. Specifically, the invention relates to a compound as shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, N-oxide, isotope labeled compound, metabolite or prodrug thereof, and a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt, the stereoisomer, the tautomer, the polymorphic substance, the solvate, the N-oxide, the isotope labeled compound, the metabolite or the prodrug thereof. The invention also relates to a preparation method of the compound and application of the compound in preparation of drugs for preventing or treating KRAS-mediated related diseases.

The present application provides a spiro compound having a binding activity with E3 ligase protein CRBN shown in formula I, and a use thereof in preparing a medicine for treating a cell abnormal proliferation disease.