254 results about "Cyclopropane" patented technology

The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-TH-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.

The present invention is directed to a water-soluble granule compositions comprising 1-amino-1-cyclopropanecarboxylic acid (“ACC”), a filler selected from the group consisting of lactose, dextrose, sucrose or a mixture thereof, one or more wetting agents selected from the group consisting of a non-ionic ethoxylated sorbitan, a polyoxyethylene glycol alkyl ether and an anionic dioctyl sulfosuccinate, one or more binders selected from the group consisting of polyvinylpyrrolidone and a lignosulfonate and one or more organosilicon surfactants selected from the group consisting of a polyalkyleneoxide modified heptamethyltrisiloxane and a polyether trisiloxane.

Environmentally friendly refrigerant blends utilizing refrigerants including 2,3,3,3-tetrafluoropropene (HFO-1234yf), 1,2-difluoroethylene, at least one hydrocarbon selected from the group consisting of propane, cyclopropane, propylene, isobutane, and n-butane, and optionally 1,1-difluoroethane (HFC-152a). The blends have low GWP, low toxicity, and low flammability with low temperature glide for use in a hybrid, mild hybrid, plug-in hybrid, or full electric vehicles for thermal management (transferring heat from one part of the vehicle to the other) of the passenger compartment providing air conditioning (A / C) or heating to the passenger cabin.

The invention belongs to the technical field of medicines, and discloses an application of a small molecule compound in preparation of a product for preventing and / or treating pulmonary arterial hypertension and complications thereof. The small molecule compound is 8-[[4-(cyclopropanecarbonyl) piperazine-1-yl] methyl]-1, 3-dimethyl-7-(3-methylbutyl) purine-2, 6-diketone, and the structural formula is as shown in a formula (I): # imgabs0. The small molecule compound and pharmaceutically acceptable salts thereof have a remarkable treatment effect on pulmonary arterial hypertension and complications thereof, and can be used for treating pulmonary arterial hypertension and complications thereof. The effects of preventing and / or treating the pulmonary arterial hypertension include the reduction of right heart hypertrophy, the reduction of right ventricular systolic pressure, right heart enlargement, right heart dysfunction, pulmonary vascular remodeling, pulmonary arterial intima thickness, increase of vascular myelization, pulmonary arterial smooth muscle cell proliferation and migration, the reduction of the right ventricular hypertrophy, the reduction of the right ventricular hypertrophy, the reduction of the right ventricular hypertrophy and the reduction of the right ventricular hypertrophy. The pulmonary arterial intima thickness and the vascular myelization level are improved, pulmonary vascular remodeling is reversed, and pulmonary artery smooth muscle cell proliferation and migration are inhibited.

The present invention relates to pharmaceutical compositions containing N-(1,3-dimethylpyrazol-4-yl)sulfonyl-6-[3-(3,3, 3-trifluoro-2,2-dimethyl-propoxy)pyrazol-1-yl]-2-[(4S)-2,2,4-trimethylpyrrolidin-1-yl]pyridine-3-carboxamide, a solid dispersion of (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-7V-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-en indol-5-yl)cyclopropanecarboxamide, and a solid dispersion of N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxo-quinoline-3-carboxamide, including formulations of the solid dispersions into powders, granules and mini-tablets, methods for manufacturing and processing the powders, granules and mini-tablets, and methods for treating cystic fibrosis employing the pharmaceutical compositions.

The invention relates to a novel spirocyclopropane tetronic acid derivative with insecticidal and acaricidal activity as well as preparation and application of the novel spirocyclopropane tetronic acid derivative. Specifically, the invention provides a compound as shown in a formula (I), and an optical isomer, a cis-trans isomer or a pharmaceutically acceptable salt thereof. The compound disclosed by the invention has obvious insecticidal and acaricidal activity, and can be used for developing novel crop insecticidal and acaricidal agents which are low in toxicity, efficient and environment-friendly. # imgabs0 #

There is provided peptidic compounds of Formula I, A or B(Rradn6-[linker]-RL-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-ψ-Xaa9-NH2). Xaa1 is D-Phe, Cpa, D-Cpa, Nal, D-Nal, 2-Nal, or D-2-Nal; Xaa2 is Asn, Gln, Hse, Cit or His. Xaa3 is Trp, Bta, Trp(Me), Trp(7-Me), Trp(6-Me), Trp(5-Me), Trp(4-Me), Trp(2-Me), Trp(7-F), Trp(6-F), Trp(5-F), Trp(4-F), Trp(5-OH), or αMe-Trp. Xaa4 is Ala or Ser. Xaa5 is Val, Cpg, or Tle. Xaa6 is Gly, NMe-Gly, or D-Ala. Xaa7 is His or NMe-His. Xaa8 is Leu or Phe. Xaa9-NH2 is a C-terminally amidated amino acid residue selected from Pro, 4-oxa-L-Pro, Me2Thz, or Thz. ψ represents a peptide bond or reduced peptide bond joining Xaa8 to Xaa9. Rradn6 is 1-5 radiolabeling groups. There is also provided the use of such compounds as imaging agents or therapeutic agents.

The invention relates to the technical field of organic synthesis, in particular to a method for synthesizing cyclopentane compounds through [3 + 2] cycloaddition reaction of aryl cyclopropane and olefin under the synergistic catalysis of bromide ions / visible light. The method comprises the following steps: in a nitrogen atmosphere, sequentially adding aryl cyclopropane, a benzyl malononitrile derivative, pyridine tribromide and a photocatalyst into a reaction solvent to obtain a mixture, stirring the mixture at the temperature of 40 DEG C under the irradiation of a 12W blue light LED lamp until the reaction is complete, and performing concentration and column chromatography purification to obtain the cyclopentane compound. The method has the advantages of mild reaction conditions, simple operation, simple and easily available raw materials and low cost.

Mixtures configured to etch a thin film of an integrated circuit material are disclosed. The mixtures may include a first compound comprising one or more of: A, B, and C; and a second compound comprising one or more of: oxygen, argon, helium, nitrogen, octafluorocyclobutane (C4F8), hexafluorobutadiene (C4F6), carbonyl fluoride (COF2), difluoromethane (CH2F2), trifluoromethane (CHF3), carbon tetrafluoride (CF4), methyl fluoride (CH3F), octafluorocyclopentene (C5F8), 2,3,3,3-tetrafluoropro-l-ene (C3H2F4), 2,3,3,3-tetrafluoropro-l-ene (C3H2F4), hexafluoropropene (C3F6), hexafluorocyclopropane (C3F6), or 1,1,3,3,3-pentafhioropropene (C3HF5).

The present disclosure relates generally to crystalline forms of (1S,2S)-N-(2-(4,6- bis(methoxy-d 3)pyrimidin-5-yl)-1-methyl-1H-pyrrolo[2, 3-c]pyridin-5-yl)-2- fluorocyclopropane-1-carboxamide (Compound 1), compositions thereof, and methods of using any of the foregoing.

The application relates to the technical field of organic compound synthesis, and particularly provides a preparation method of a cyclopropane compound. gem The dichloro compound is used as raw material, a piezoelectric material, a metal reducing agent and an additive are added under a nitrogen atmosphere, a mechanical grinding method is used for reaction, and the reaction solution is subjected to post-treatment to obtain the cyclopropane compound. The method is simple in operation and mild in conditions, the raw material and reagent are cheap and easy to obtain and environment-friendly, a large amount of solvent or a high-cost catalyst does not need to be used, and the conversion can be successfully realized. In addition, the preparation method has good yield and functional group tolerance, is suitable for scale-up production, has a good industrial application prospect, and can be widely used in the fields of medical raw materials, intermediates and fine chemical synthesis.

Disclosed in the present invention are a method for synthesizing deucravacitinib and intermediates thereof. An intermediate 2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)aniline is prepared by subjecting 2,3-dichloronitrobenzene to an etherification reaction and a cyanation reaction to prepare 2-methoxy-3-nitrobenzonitrile; then reacting 2-methoxy-3-nitrobenzonitrile with ammonium chloride under the action of an alkali to generate 3-(2-methoxy-3-nitrophenyl)-1-methyl-1H-1,2,4-triazole; and finally, carrying out a catalytic reduction reaction to obtain the target product. Another intermediate N-(5-bromo-6-cyanopyrazin-3-yl)cyclopropanecarboxamide is prepared by subjecting 3-amino-6-chloropyridazine to a bromination reaction to prepare 3-amino-4-bromo-6-chloropyridazine, then reacting 3-amino-4-bromo-6-chloropyridazine with sodium nitrite under low-temperature condition and in the presence of an acid to generate a diazonium salt, and then adding a cyanate reagent to generate 4-bromo-6-chloro-3-cyanopyridazine; and finally carrying out a substitution reaction to obtain a target product (I). Deucravacitinib is obtained by subjecting these intermediates to a Buchwald-Hartwig coupling reaction, carrying out nitrile hydrolysis, and carrying out condensation.

The invention discloses an environment-friendly refrigeration composition for compression refrigeration, the ODP value of the environment-friendly refrigeration composition is 0, the GWP is less than 150, and the refrigeration composition comprises hexafluoropropylene serving as a first component and accounting for 30-50% of the total mass of the refrigeration composition; the trifluoroethylene is used as a second component and accounts for 30-50% of the total mass of the refrigeration composition; the third component is selected from at least one of cyclopropane, difluoromethane or trifluoroacetyl fluoride, and the mass of the third component accounts for 10-30% of the total mass of the refrigeration composition. The refrigeration composition can replace R410A to be used for a household air conditioner or a commercial air conditioner system, parts of the air conditioner system do not need to be replaced, the environmental performance is far better than that of the R410A, and the cycle performance is equivalent to or slightly better than that of the R410A.

To provide an etching method using hexafluoropropene.SOLUTION: Etching gas contains at least one kind of component selected from the group consisting of hexafluoropropene and hexafluorocyclopropane, and a dimer and / or a trimer derived from hexafluoropropene and hexafluorocyclopropane. With respect to the total amount of the etching gas, (1) 95 vol.% to 99.99999 vol.% of the hexafluoropropene is contained, and (2) 1 vol.ppm to 1,000 vol.ppm of at least one kind of component selected from the group consisting of hexafluoropropene and hexafluorocyclopropane, and a dimer and / or a trimer derived from hexafluoropropene and hexafluorocyclopropane is contained.SELECTED DRAWING: None

The application discloses a chiral fluorocyclopropane carboxylate and a preparation method thereof. Under the catalysis of divalent rhodium, ethyl aryl diazoacetate and fluorostyrene are reacted through an asymmetric cyclopropanation reaction to generate a chiral fluorocyclopropane compound. Different substitution types of substrates in the system are expanded, and good universality is shown. Various types of substituted substrates can smoothly participate in the reaction to synthesize 12 fluorocyclopropane ester substrates with a yield of 56-89%, 82-99% ee and a highest >20.0:1.0 dr. The application efficiently realizes the introduction of a fluorine atom to a cyclopropane skeleton, and efficiently constructs the fluorocyclopropane compound under mild conditions, thereby providing a new strategy which is simple, efficient and has strong universality for the synthesis of the important compound.

The invention relates to a synthesis method of polysubstituted pyrrolidone. The method is characterized in that # imgabs0 # R1 is alkyl-substituted phenyl, trifluoromethyl-substituted phenyl, cyano-substituted phenyl, methylthio-substituted phenyl, dimethylamino-substituted phenyl, alkenyl-substituted phenyl, alkynyl-substituted phenyl, naphthyl, benzothienyl, cyclohexyl, benzyl and indolyl, R2 is long-chain alkyl and phenyl, R3 and R4 are cyano and ester groups, and R3 and R4 can be the same or different. According to the method, azide and vinyl cyclopropane which are different in substitution are taken as raw materials, palladium and phosphine are taken as a catalytic system, the polysubstituted pyrrolidone compound is synthesized by taking carbon dioxide as a raw material, and the yield of a target product is as high as 90%. The palladium and the phosphine which are cheap and easy to obtain are used, and the catalyst cost is low. The nitrine substrate used in the method is easy to prepare, does not have explosiveness, is wide in application range, effectively realizes high-value utilization of carbon dioxide, and meets the requirements of green chemistry.

The present invention provides a salt of a dioxane quinoline compound, a crystal form thereof, preparation methods therefor and uses thereof. Specifically, the present invention relates to N-(3-fluoro-4-((5-(3-morpholinopropoxy)-2,3-dihydro-[1,4]dioxano[2,3-f]quinolin-10-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, a crystal form thereof and preparation methods therefor, and uses in the preparation of a drug as an inhibitor of tyrosine kinases (e.g. VEGFR-2 and c-MET, etc.).

The invention discloses a preparation method of a 3-aryl pyrazolidine compound, which comprises the following steps: in an inert gas atmosphere, sequentially adding aryl cyclopropane, an azodicarboxylic acid derivative, NaBr and a photocatalyst into acetonitrile to obtain a mixture, reacting for 12 hours at room temperature under the irradiation of 5W blue light with the wavelength of 456nm, and separating from the reaction liquid to obtain the 3-aryl pyrazolidine-1, 2, 3-triazole compound. The invention relates to a 1, 2-dicarboxylic acid derivative. The preparation of the 3-aryl pyrazolidine compound can be carried out at room temperature, the reaction condition is mild, the adopted raw materials are simple and easy to obtain, and the cost is low.

Disclosed are 1,5,6-polysubstituted-2-oxo-3-oxabicyclo[3.1.0]hexane and a preparation method thereof. The reaction process comprises the following steps: using α-substituted allyl acetate as a raw material under the action of an inexpensive metal catalyst, the acetic acid acrylate structure contains a cyclopropane-γ-lactone structure, and the substituent types are diverse, making it easy to perform subsequent derivatization modification. The target product is prepared efficiently and with high non-corresponding selectivity through a one-pot process. The method has the advantages of simple and readily available raw materials, mild reaction conditions, simple operation, wide substrate universality, easy large-scale production, no safety hazards, and low cost, and can provide support for relevant drug activity testing.

A working medium for a heat cycle includes trifluoroethylene, a low boiling point compound having a lower boiling point than the boiling point of the trifluoroethylene, and high boiling point compounds having higher boiling points than the boiling point of the trifluoroethylene. In the working medium, the low boiling point compound is at least one selected from the group consisting of carbon dioxide, R116, and R41, and the high boiling point compounds are at least two selected from the group consisting of HFC-32, HFO-1234yf, HFO-1234ze (E), HFO-1243zf, PFC-14, HFC-134, HFC-143a, HFC-227ea, cyclopropane, isobutene, isobutane, dimethyl ether, and ammonia. An application of the working medium is provided.

The present invention provides a new crystalline form of Cabozantinib free base, Formula (I), which is chemically known as N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4- fluorophenyl)cyclopropane-1,1-dicarboxamide and preparation of its novel crystalline polymorph Form E, Formula (II).

Disclosed are crystalline salt Forms C and D of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)amino)-N-(methyl-d3)pyridazine-3-carboxamide. Form C is a MSA salt and Form D is a sulfate salt of Compound (I). Characterization data for the Forms are disclosed.

The present invention relates to fungicidal compositions comprising at least one compound selected from the group consisting (I-1) N-[1,3-dimethyl-1-(phenylmethyl)butyl]-8-fluoro-3- quinolinecarboxamide, (I-2) N-[(1R)-1-benzyl-1,3-dimethyl-butyl]-8-fluoro-quinoline-3- carboxamide, (I-3) N-[(1S)-1-benzyl-1,3-dimethyl-butyl]-8-fluoro-quinoline-3-carboxamide, as active component 2) at least one compound, or an N-oxide, or an agriculturally useful salt thereof, selected from the group consisting of (II-1) 2-fluoro-4-[5-(trifluoromethyl)-1,2,4- oxadiazol-3-yl]benzanilide, (II-2) metarylpicoxamid,(II-3) N-methoxy-N-[[4-[5-(trifluoromethyl)- 1,2,4-oxadiazol-3-yl]phenyl]methyl]cyclopropanecarboxamide, (II-4) N,2-dimethoxy-N-[[4-[5- (trifluoromethyl)-1,2,4-oxadiazol-3-yl]phenyl]methyl]propenamide,(II-5) methyl (Z)-3-methoxy-2- (2-methyl-5-phenyl-phenoxy)prop-2-enoate, wherein the weight ratio of compound I to compound II is from 10:1 to 1:10. The invention also relates to an agrochemical composition comprising the composition and a solvent of solid carrier. Further, the invention relates to a non- therapeutic use of the inventive compositions controlling phytopathogenic harmful fungi.

The present specification reports a polypeptide-linker-nucleic acid conjugate, wherein the linker comprises a 3-aminopropanamide unit, a 2,6-diaminohexanoic acid amide unit, and a 1,4,5,5a,6,6a,7,8-octahydrocyclopropa[5,6]cycloocta[1,2-d]-1,2,3-triazole unit, the polypeptide comprises a C-terminal lysine residue, the nucleic acid comprises an oxygen atom at the 5' or 3' end linked to a phosphorus atom in oxidation state V, and the 3-amino group of the 3-aminopropanamide unit and the carboxy functional group of the lysine residue of the polypeptide are linked by / form an amide bond, and the 3-aminopropanamide unit is linked to the carboxy functional group of the lysine residue of the polypeptide. The carboxyl functional group at position 1 and the alpha amino group of the 2,6-diaminohexanoic acid amide unit are linked by / form an amide bond, the 6-amino group of the 2,6-diaminohexanoic acid amide unit is the nitrogen of the 1,2,3-triazole element of the 1,4,5,5a,6,6a,7,8-octahydrocyclopropa[5,6]cycloocta[1,2-d]-1,2,3-triazole unit, and the oxygen linked to the phosphorus atom of the nucleic acid is covalently linked to the cyclopropane element of the 1,4,5,5a,6,6a,7,8-octahydrocyclopropa[5,6]cycloocta[1,2-d]-1,2,3-triazole unit.

The invention discloses a synthesis method of a novel fluorine-containing allyl tertiary nitro alkane compound, which comprises the following steps: by taking a gem-difluorocyclopropane derivative and sec-nitro alkane as raw materials, carrying out ring opening on gem-difluorocyclopropane under the catalysis of transition metal to generate a fluorine allyl-metal complex; and then reacting with sec-nitro alkane to obtain the straight-chain fluorine-containing allyl tert-nitro alkane compound. The method has obvious advantages in the aspects of synthesis conditions and practicability, has the advantages of simple synthesis steps, simplicity and convenience in operation, cheap and easily available raw materials, good compatibility to functional groups, high chemical selectivity, high reaction efficiency and the like, and is more in line with green and sustainable chemistry concepts; and reference and reliable technical support are provided for efficient synthesis of the fluorine-containing allyl tertiary nitro alkane compound.

The application discloses a preparation method of a cyclopropane compound and application of the cyclopropane compound in nematode killing activity. The application uses an electrochemical method to quickly cyclopropanate a methylene compound by using a cheap and easily available sulfide. The synthesis method is simple, clean, efficient, short in reaction time, low in energy consumption, and cheap and easily available in raw materials, and is suitable for mass production and better research. Through activity testing, the cyclopropane compound has strong activity against pine wood nematode disease, and relevant research provides a good basis for strong biological activity, anticancer activity, antibacterial activity and anti-inflammatory activity.

A pharmaceutical composition comprising Compound 1, (3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid), and at least one excipient selected from: a filler, a disintegrant, a surfactant, a binder, and a lubricant, the composition being suitable for oral administration to a patient in need thereof to treat a CFTR mediated disease such as Cystic Fibrosis. Processes of preparing pharmaceutical compositions comprising Compound 1 are also disclosed.

The present invention is directed to processes for preparing stable 1-amino-1-cyclopropanecarboxylic acid (“ACC”) water-soluble granules comprising the steps of mixing a composition comprising ACC and water at a concentration ratio at about 2.0:1 or less to create a wet mass, extruding the wet mass to create an extrudate and drying the extrudate to create the water-soluble ACC granules, wherein the concentration of ACC and water is weight by total weight of the wet mass. The present invention is further directed to ACC granules produced by processes of the present invention.

The invention provides a preparation method of tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone, and belongs to the technical field of heterocyclic compounds. The preparation method comprises the following steps: adding a palladium catalyst, a ligand, alkali and bicyclo [1.1. 0] butyramide into an organic solvent, reacting at 50-70 DEG C for 10-14 hours, and performing post-treatment to obtain tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone. The preparation method has the advantages of simple operation, cheap and easily available initial raw materials, high reaction efficiency and good substrate compatibility, and can realize one-step efficient and rapid synthesis of tetrahydrocyclopropane [3, 4] cyclopenta [1, 2-c] quinoline-(5H)-ketone.

The present application belongs to the technical field of drugs, and relates to a new crystal form of a nitrogen-containing tricyclic compound and a use thereof. Specifically, the present application relates to a new crystal form of 2-((5-cyclopropyl-3-(2,6-dichlorophenyl)isoxazol-4-yl)methoxy)-10H-spiro[benzo[6,7]oxepino[3,2-b]pyridine-11,1'-cyclopropane]-7-carboxylic acid, which is a crystal form N. The present application also relates to a pharmaceutical composition comprising the crystal form. The crystal form or the pharmaceutical composition can be used for preventing, treating or alleviating a disease mediated by FXR in a patient.