156 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 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 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.

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.

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 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.

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 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.

The invention provides a method for chiral resolution of (trans)-2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid. The method comprises the steps of: (a) treating (trans)-2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid with a chiral base selected from the list consisting of: quinine, R )-1-cyclohexylethan-1-amine, S )-1-cyclohexylethan-1-amine and L )-leucinamide, in an organic solvent to form a suspension, (b) separating the desired enantiomer and diastereomeric salt of the chiral base from the suspension, and (c) optionally, treating the separated diastereomeric salt with an acid to obtain the desired enantiomer of 2,2-dichloro-3-(3-chloro-4-fluorophenyl)cyclopropane-1-carboxylic acid.

The invention relates to a polymorphic form of hydrobromide or hydrochloride of 5-(6-(4-(cyclopropylmethyl) piperazine-1-yl)-2-methylpyridine-3-yl)-N-((4, 6-dimethyl-2-oxo-1, 2-dihydropyridine-3-yl) methyl)-3-(N-ethylcyclopropanecarboxamide)-2-methylbenzamide, a pharmaceutical composition of the polymorphic form and application of the polymorphic form and the pharmaceutical composition of the hydrobromide or hydrochloride of the 5-(6-(4-(cyclopropylmethyl) piperazine-1-yl)-2-methylpyridine-3-yl)-N-(4, 6-dimethyl-2-oxo-1, 2-dihydropyridine-3-yl)-3-(N-ethylcyclopropanecarboxamide.

High temperature lubricants for magnetic media include a plurality of segments according to general formula (I):where Rd is any linker chemistry and each Re may be a reactive end-group and anchoring group containing at least one constituent configured for at least one of tribochemical, thermochemical, or optochemical bonding. The at least one constituent can be cyclopropane or cyclobutane.

The disclosure is in part directed to crystalline forms of N-(4-((3-methoxy-4-(1-(methyld3)- 1H-1,2,4-triazol-3-yl)pyridin-2-yl)amino)-5-propionylpyridin-2-yl)cyclopropane carboxamide hydrogen fumarate, pharmaceutical compositions thereof, and methods of use.

Disclosed is crystalline Form A 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 A is a neat crystalline form. Characterization data for Form A are disclosed.

The invention provides a cyclopropane TLR7 and / or 8 inhibitor (or antagonist) which can be used for preventing and / or treating inflammatory and autoimmune diseases and the like.

The invention relates to a compound with a cyclopropane carboxylic acid pyrazole ester structure and application thereof, and belongs to the technical field of pesticides. The structure of the compound is shown in the specification. The invention further provides application of the compound shown in the formula I in prevention and control of agricultural pests. The compound represented by the formula I provided by the invention shows an excellent effect on various pests, especially on prevention or control of pests such as aleyrodidae, aphididae, tetranychidae and glophidae, and the compound has low toxicity.

The application discloses a kind of biological ligand for chromium-free metal tanning agent, it is formed by the following steps reaction: step one: taking the biological compound containing hydroxyl group, dissolved in solvent, adding catalyst step two: the solution is carried out ice bath, and the halogenated hydrocarbon containing epoxy group and the halogenated hydrocarbon containing aldehyde group are reacted;Step three: after the reaction product is washed, organic phase is collected, solvent is spun dry, and biological ligand is obtained by chromatographic column.In the application, mainly castor oil is used as biological carrier, (2-chloroethoxy) cyclopropane, 6-chloropyridine-3-formaldehyde is reacted with castor oil, (2-chloroethoxy) cyclopropane, 6-chloropyridine-3-formaldehyde has halogenated group, and castor oil has a large number of hydroxyl groups, so that the reaction occurs, so that castor oil molecules have a large number of epoxy groups and aldehyde groups, so as to be used as pre-kneading agent for pre-kneading leather.

Processes for preparing (1S,3R)-3-(4-((R)-2-chloro-8-methyl-8-(trifluoromethyl)-7,8- dihydro-6H-pyrazolo[1,5-a]pyrrolo[2,3-e]pyrimidin-6-yl)phenyl)-2,2-difluoro-1-methyl-N- ((trans)-3-(methylsulfonyl)cyclobutyl)cyclopropane-1-carboxamide are described, which are useful for commercial manufacturing. The compound may be useful for the treatment of a disease, syndrome, condition, or disorder, particularly a MALT1- related disease, syndrome, condition, or disorder, including but not limited to, cancer and immunological diseases.

The invention is suitable for the technical field of gene engineering, and provides inactivated mutants of soybean GmAH1 and GmAH2, and the inactivated mutants of soybean GmAH1 and GmAH2 are respectively GmAH1 [delta] 145D 146A and GmAH2 [delta] 145D 146A 147L, and the inactivated mutants of soybean GmAH1 and GmAH2 are respectively GmAH1 [delta] 145D 146A and GmAH2 [delta] 145D 146A. The amino acid sequence of the GmAH1 delta 145D 146A is as shown in SEQ ID NO. 1, and the amino acid sequence of the GmAH2 delta 145D 146A 147L is as shown in SEQ ID NO. 2. The 1-aminocyclopropane-1-carboxylic acid synthase activity and the C-S lyase activity of the two mutants are all lost, novel targets and gene resources are provided for creation of soybean stress-resistant varieties, and the two mutants have wide application prospects and important economic values in stress-resistant soybean molecular breeding.