156 results about "Dichlofopmethyl" patented technology

The invention relates to the field of pesticide bactericides, and discloses a difluoromethyl thiazole amide-containing compound and application thereof as a bactericide. The difluoromethyl thiazole-containing amide compound has a structure as shown in a formula (I), and the difluoromethyl thiazole-containing amide compound with efficient activity on diseases such as rice sheath blight disease is designed by introducing a difluoromethyl thiazole-containing structure and a diphenyl ether fragment. The compound can be used as a brand new succinate dehydrogenase inhibitor or bactericide. # imgabs0 #

The invention relates to a crystal form of a compound (S)-1-((2 ', 6-bis (difluoromethyl)-[2, 4'-bipyridyl]-5-yl) oxy)-2, 4-dimethyl pent-4-ene-2-amine as shown in a formula (I) and a salt thereof, a preparation method of the crystal form, and application of the crystal form in a pharmaceutical composition and medicine of the compound (S)-1-((2 ', 6-bis (difluoromethyl)-[2, 4'-bipyridyl]-5-yl) oxy)-2, 4-dimethyl pent-4-ene-2-amine and the salt thereof. # imgabs0 #

The invention discloses an N-phenyl phenothiazine super-crosslinked polymer catalyst and a preparation method and application thereof.The method comprises the steps that Friedel-Crafts reaction is utilized, N-phenyl phenothiazine (I), dimethyl formal (II) and lewis acid are dissolved in a solvent, the mixture is stirred to react for 12-36 hours at the temperature of 60-120 DEG C, cooling and filtering are conducted, then extraction is conducted for 12-24 hours through a Soxhlet extractor, cooling and filtering are conducted again, and the N-phenyl phenothiazine super-crosslinked polymer catalyst is obtained. And drying the obtained solid to obtain the N-phenyl phenothiazine super-crosslinked polymer catalyst. The prepared N-phenyl phenothiazine super-crosslinked polymer catalyst can be applied to photocatalytic synthesis of 6-difluoromethyl phenanthridine derivatives, the reaction condition is mild, the catalytic efficiency is high, the selectivity is good, the catalyst can be recycled for multiple times, and the method is simple and easy to operate and has wide application potential.

The invention relates to the technical field of organic synthesis, in particular to a synthesis method of a pesticide intermediate difluopyrazole acid.The difluopyrazole acid is generated through CO2 carboxylation reaction of 3-difluoromethyl-1-methylpyrazole, bromination reaction is not needed, generation of toxic waste liquid is reduced, and the synthesis method is environmentally friendly. The method has the advantages of high reaction yield, high product purity, certain industrial application prospect, full utilization of CO2, and contribution to reduction of CO2 emission and mitigation of greenhouse effect.

This disclosure provides processes of preparing compounds of Formula (I), such as (R)-1-(2-aminopyrimidin-5-yl)-3-(1-(5,7-difluoro-3-methylbenzofuran-2-yl)-2,2,2-trifluoroethyl)urea (Compound 1), and salts and / or solvates thereof, that inhibit phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) isoform alpha (PI3Kα).

The invention discloses a method for preparing a heavy metal-free pharmaceutical intermediate difluoromethyl ether proline derivative, which belongs to the technical field of organic synthesis and is suitable for industrial large-scale production. Difluorocarbene is produced by using a cheap base free of heavy metals as an additive, and the difluoromethylation of the proline derivative is completed to obtain an important difluoromethyl ether proline derivative pharmaceutical intermediate. Compared with existing synthesis methods, the method has mild reaction conditions, does not require the participation of heavy metals, can produce a large amount of fluorine-free products, uses inexpensive and readily available reagents, and has a high yield.

The present application relates to a kind of preparation method of trifluoromethyl pyrazole compound, belong to the technical field of organic synthesis.The specific method is: (1) trifluoroacetyl ethyl acetate is first with hydrazine hydrate cyclization reaction and generates compound of formula III;(2) under the catalysis of base, compound of formula III is reacted with difluoromethylation reagent and generates compound of formula II;(3) compound of formula II is reacted with methylating agent and obtains compound of formula I;The difluoromethylation reagent is difluoro-monochloromethane or sodium difluoro-monochloroacetate;The methylating agent is chloromethane, bromomethane, iodomethane, dimethyl sulfate or dimethyl carbonate.The present application is prepared by changing reaction route, and the higher-priced raw material methylhydrazine is replaced, and isomer impurity is no longer generated in the product prepared.Not only raw material cost is reduced, but also the purity of product is improved.

Disclosed herein are (6-(4-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, (6-(4-(difluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine, and (6-(2-(trifluoromethyl)pyridin-3-yl)pyridazin-3-yl)octahydrocyclopenta[c]pyrrol-5-amine compounds, useful as antagonists of the muscarinic acetylcholine receptor M4 (mAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions.

The invention discloses a preparation method of a difluoromethyl reagent and application of the difluoromethyl reagent in synthesis of a nickel-catalyzed alkyl difluoromethyl compound. The preparation method of the difluoromethyl reagent comprises the following steps: in an inert gas atmosphere, adding potassium iodide, cuprous iodide and a water-containing dimethylformamide solution into a reaction container, heating, dropwise adding difluorochloroacetic acid of DMF (Dimethyl Formamide) into a reaction system, collecting difluoroiodomethane, and supplementing a 1-methyl-2-pyrrolidone NMP (N-Methyl Pyrrolidone) solution into the system. The invention provides a difluoromethyl reagent which is simple and convenient to operate, low in cost, high in yield, environment-friendly and beneficial to large-scale preparation and application of the reagent in synthesis of difluoromethyl substituted alkane compounds.

The invention discloses a preparation method of 5-(difluoromethoxy) pyrazine-2-amine. The 5-(difluoromethoxy) pyrazine-2-amine is used as a raw material. The preparation method comprises the following specific steps: (1) taking a compound 1 as an initial raw material, and carrying out difluoromethylation reaction to prepare a compound 2; and (2) carrying out Ullmann coupling reaction on the compound 2 to prepare a target product, namely the 5-(difluoromethoxy) pyrazine-2-amine. The preparation method provided by the invention is short in process route, convenient to operate, mild in reaction condition, easy to control, relatively low in cost, suitable for process amplification, easy in product purification and relatively high in yield.

The invention discloses a preparation method of a fluorine-containing ester-containing triazole compound, which comprises the following steps of: reacting fluorine-containing ester-containing p-toluenesulfonylhydrazone prepared from cheap and easily available starting raw materials (ketone containing trifluoromethyl or difluoromethyl functional groups) with an aromatic amine compound in tert-butyl hydroperoxide and acetonitrile under the promotion condition of iodine to obtain the fluorine-containing ester-containing triazole compound. And the fluorine-containing ester-containing triazole compound is obtained by a cyclization reaction and a'one-pot method '. In the preparation process, an expensive metal catalyst or ligand does not need to be used, so that the problem of toxicity or use safety caused by metal residues or azide compounds in a pharmaceutical process does not exist; in addition, the raw materials used in the process are bulk, cheap and easily available, the reaction system is green and environment-friendly, and the method has the advantages of simple operation steps and post-treatment process and high yield; the subsequent conversion research of the process can be applied to the synthesis of medical intermediates or related similar compounds.

The invention provides a green synthesis method of a sulfentrazone dichloride intermediate, which is characterized in that 2-chlorphenyl-4-difluoromethyl-4, 5-dihydro-3-methyl-1hydrogen-1, 2-4-triazole-5 (1H) ketone (intermediate I) is used as a reaction raw material, and chlorine and an oxidizing agent are matched to carry out chlorination reaction. The method has the advantages of simple and convenient process route, mild reaction conditions, simple and convenient operation process, reduced chlorine usage amount, high chlorine atom utilization rate, short reaction time, less waste gas generation amount, low production cost and easy industrialization realization, and is suitable for industrial production. The technical problems of low chlorine utilization rate, more three wastes, low safety and the like in the dichlorination reaction in the existing production technology are solved.

The invention provides a preparation method of a difluoromethyl heteroaromatic compound, which comprises the following steps: by taking a heteroaromatic compound and iododifluoromethyl phenyl sulfone as raw materials, reacting for a certain time under the action of a palladium catalyst, a ligand, alkali, an organic solvent and temperature, thereby obtaining the difluoromethyl heteroaromatic compound. A series of difluoromethyl heteroaromatic compounds are generated; the heteroaromatic compound is an indole compound 1 or a pyrrole compound or a thiourea compound. The invention provides a novel method for generating the difluoromethyl heteroaromatic compounds by using palladium catalytic reaction under mild conditions, the method uses iodine difluoromethyl phenyl sulfone as a difluoromethylation reagent, the wide substrate compatibility is shown, and the excellent yield is obtained.

This application relates to processes and intermediates for the preparation of the PD-1 / PD-L1 inhibitor (R)-1-((7-cyano-2-(3′-((2-(difluoromethyl)-7-((3-hydroxypyrrolidin-1-yl)methyl)pyrido[3,2-d]pyrimidin-4-yl)amino)-2,2′-dimethyl-[1,1′-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)piperidine-4-carboxylic acid, and salts and crystalline forms thereof, where the PD-1 / PD-L1 inhibitor and solid forms and salt forms thereof are useful in the treatment of various diseases including infectious diseases and cancer.

Salts of the AAK1 inhibitor (S)-1-((2′,6-bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine and solid forms thereof are disclosed, as are pharmaceutical formulations comprising them and methods of their preparation.

The invention relates to a synthesis method of a difluoroalkyl sulfone compound and / or a difluoroalkyl sulfoxide compound. The synthesis method comprises the following steps: taking a compound 1 and a compound 2 as raw materials, adding alkali, reacting in a solvent, oxidizing and decarboxylating; the structure of the compound 1 is shown as a formula (I-1) or a formula (I-2); the structures of the difluoroalkyl sulfone compound and the difluoroalkyl sulfoxide compound are respectively shown as a formula (II) and a formula (III); ; wherein M is selected from Na, K, NH4 or a hydrogen atom; r1 is selected from C1-C8 straight chain or straight chain alkyl; r2 is selected from a C1-C8 straight chain or branched chain alkylene group; r is selected from C1-C8 linear chain or branched chain alkyl; the structural general formula of the compound 2 is ClRf; and Rf is selected from a linear chain or branched chain alkyl group containing a difluoromethyl group of C1-C15. The one-pot method is adopted, the alkyl sulfone and the alkyl sulfoxide are prepared by using the same synthetic route, the synthetic reaction is simple, the substrate limitation is less, the cost is low, the reaction is fast, the yield is high, and the industrial production can be realized.

The invention relates to the technical field of organic synthesis, and in particular to a method for synthesizing difluoropyrazole acid, a pesticide intermediate. The difluoropyrazole acid is prepared by subjecting 3-difluoromethyl-1-methylpyrazole to a CO2 carboxylation reaction. The method does not require a bromination reaction, thereby reducing the generation of toxic waste liquid, and has relatively high reaction yield and product purity. The method has certain industrial application prospects, and fully utilizes CO2, thereby contributing to reducing CO2 emissions and alleviating the greenhouse effect.

To provide: compounds useful in treating central nervous system diseases and other diseases; pharmaceutical compositions; and processes for the manufacture of the same.SOLUTION: The present invention relates to: difluoromethyl-pyridin-2-yl triazoles of general formula (I), which are modulators of GABAA receptors containing the α5 subunit; pharmaceutical compositions containing the compounds; and processes for the manufacture of the compounds.SELECTED DRAWING: None

The present application provides a crystal which is at least one crystal selected from the group consisting of a Ra1-type crystal, a Ra2-type crystal and a Ra3-type crystal each having the diffraction peaks described in the specification in powder X-ray diffraction based on Cu-Kα rays, of 3-(difluoromethyl)-1-methyl-N-(1,1,3-trimethyl-2,3-dihydro-1H-inden-4-yl)-1H-pyrazole-4-carboxamide.

The present invention relates to an emulsion concentrate (EC) formulation of succinate dehydrogenase inhibitor fungicides, the manufacture of such a formulation, and the use of its diluted form for the control of fungal pathogens, in particular in crops of useful plants. More specifically, the present invention relates to an emulsion concentrate of-difluoromethyl-1-methyl-1H-pyrazol-4-methoxyl-[1-methyl-2-(2, 4, 6-trichlorophenyl)-ethyl]-amide comprising a blend of at least three surfactants and an aromatic ester solvent.

The present invention discloses an α-difluoromethylstyrene derivative and a preparation method thereof. The structure of the α-difluoromethylstyrene derivative of the present invention is as shown in formula (I), and the α-difluoromethylstyrene derivative is formed by reacting 3,3-difluoroallyl hydrazine, a transition metal salt and an additive in a solvent. The α-difluoromethylstyrene derivative of the present invention contains both gem-difluoromethylene and double bond structural units, and can be used as a potential pharmaceutical lead compound or a synthetic intermediate of a drug active molecule, providing an opportunity for the synthesis of macromolecular drugs. At the same time, the present invention provides a preparation method of the compound. The method is direct, simple, efficient, has a wide range of substrate applicability, and the raw materials are economically available and easy to obtain, and is suitable for large-scale production of α-difluoromethylstyrene derivatives.

Provided is a resist composition which generates an acid upon exposure to light, and the solubility of which in a developer solution is changed by the action of the acid. The present invention contains: a resin component (A1), the solubility of which in a developer solution is changed by the action of an acid; an acid generator component (B) which generates an acid upon exposure to light; and a surfactant (G01). The acid generator component (B) and the surfactant (G01) do not contain a difluoromethyl group or a trifluoromethyl group. However, cases where the structure is represented by formula (np1), (np2) or (np3) are excluded. X1 represents -OR1, -N(R2)R1, or -N(R1)2. X2 represents a methyl group or the like. X3 represents a methylene group or the like. R1 and R1 each represent a methylene group or the like.

The present invention relates to soluble guanylate cyclase (sGC) activators, preferably (3S)-3-(4-chloro-3-{[(2S,3R)-2-(4-chlorophenyl)-4,4,4-trifluoro-3-methylbutanoyl]amino}phenyl)-3-cyclopropylpropanoic acid (luncacyguat) and / or substituted pyrazolopiperidinecarboxylic acids, preferably 1-[1-{4-chloro-4’-[4-(2-methylpropyl)piperazin-1-yl][1,1’-biphenyl]-2-yl}piperidin-3-yl]-5-(difluoromethyl)-1H-pyrazole-4-carboxylic acid, 1-{3(R)-1-{4-chloro-4’-(4-isobutylpiperazin-1-yl)[biphenyl]-2-yl]piperidin-3-yl}-5-(difluoromethyl)-1H-pyrazole-4-carboxylic acid, 1-{3(R)-1-[4-chloro-4’-(4-isobutylpiperazin-1-yl)[biphenyl]-2-yl]piperidin-3-yl}-5-(difluoromethyl)-1H-pyrazole-4-carboxylic acid hydrochloride, 1-{3(R)-1-[4-chloro-4’-(4-isobutylpiperazin-1-yl)[biphenyl]-2-yl]piperidin-3-yl}-5-(difluoromethyl)-1H-pyrazole-4-carboxylic acid hydrochloride hemihydrate or 1-[1-{4-chloro-4’-[4-(2-methylpropyl)piperazin-1-yl][1,1’-biphenyl]-2-yl}piperidin-3-yl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid hydrochloride (enantiomer 1), for the treatment and / or prevention of heart failure with preserved ejection fraction (HFpEF) in women, and to their use for the preparation of a medicament for use in the treatment and / or prevention of heart failure with preserved ejection fraction (HFpEF) in women.

The present application relates to a kind of 7-difluoromethyl-5-aryl pyrazolopyrimidine compound and preparation and application, the structural general formula of the compound is as shown in formula a, it is a kind of compound with inhibiting HIF-2 alpha activity, can block HIF-2 alpha / ARNT dimerization and play the role of HIF-2 transcription inhibition.The present application is proved by multiple experiments, the synthesized compound all has excellent HIF-2 transcription inhibition effect, in human renal clear cell carcinoma cell strain 786-O, show good VEGF protein inhibitory activity.The compound described in the present application can be applied in the preparation of hypoxia-inducible factor-2 alpha (HIF-2 alpha) inhibitor for treating VHL deletion or / and HIF-2 alpha abnormal expression disease.This kind of compound can inhibit the overexpression and activation of HIF-2 alpha, to achieve the treatment and prevention of target disease, such as VHL deletion or / and HIF-2 alpha abnormal expression disease.

The application discloses a synthesis method of 3-difluoromethyl-1-methylpyrazole-4-methyl ethyl formate. The synthesis method is to synthesize 3-difluoromethyl-1-methylpyrazole-4-methyl ethyl formate by taking 5-difluoromethyl-1-methylpyrazole-4-methyl ethyl formate and dimethyl carbonate as raw materials and under the action of a porous organic polymer catalyst with solidified Lewis acid. The porous organic polymer catalyst with solidified Lewis acid comprises a porous organic polymer, and the porous organic polymer is solidified with Lewis acid. In the synthesis method, under the action of the porous organic polymer catalyst with solidified Lewis acid, not only a high reaction conversion rate can be obtained at normal temperature, but also a large number of side reactions caused by high temperature can be effectively avoided, thereby the impurity content can be obviously reduced, and the synthesis method has the advantages of simple operation, good catalyst activity, mild reaction condition, few side reactions, fast reaction rate, high yield and the like, is suitable for industrial application, and has a good market prospect.

Provided are a method for preparing a metalloenzyme inhibitor compound 1-cyclopropyl-2-(6-(difluoromethyl)pyridazin-4-yl)-5,6-difluoro-1H-benzo[d]imidazole, and an important intermediate for preparing the compound.

Solid forms comprising (4S,5S)-1-({6-[4-(difluoromethyl)-2-fluorophenoxy]pyridin-3-yl}methyl)-4-hydroxy-5-methylpyrrolidine-2-one (Compound (I)), compositions comprising the same, and methods of making and using the same, for example, in the prevention or treatment of a central nervous system disease.