- METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID
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Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)- 2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives.
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Paragraph 0291-0296
(2021/04/23)
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- METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID
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Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)- 2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives. Also described herein are novel reaction intermediates.
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Paragraph 0248; 0249
(2021/04/23)
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- METHODS FOR THE PREPARATION OF 5-BROMO-2-(3-CHLORO-PYRIDIN-2-YL)-2H-PYRAZOLE-3-CARBOXYLIC ACID
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Described herein are novel methods of synthesizing 5-Bromo-2-(3-chloro-pyridin-2-yl)- 2H-pyrazole-3-carboxylic acid from pyrazole or pyrazole derivatives. Also described herein are novel reaction intermediates.
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Paragraph 0194; 0195
(2021/04/23)
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- A halogenated nitrogen-containing unsaturated cyclic hydrocarbon preparation method
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The invention discloses a halogenated nitrogen-containing unsaturated cyclic hydrocarbon of the preparation method, the steps of: (1) the nitrogen-containing unsaturated cyclic hydrocarbon dissolved in hydrochloric acid or hydrobromic acid, addition of an oxidizing agent, the reaction system halogenated reaction, in the reaction process timing sampling detection, when detecting the target product quality of a halide accounted for is a reaction system in the total of the organic matter of 70% - 95% when, added to the reaction system in the terminator to terminate reaction, to obtain containing nitrogen-containing unsaturated cyclic hydrocarbon feed; (2) to the liquid mixed into the organic solvent extraction, extraction to obtain the organic phase, the organic phase temperature is reduced to make the solid precipitation or distilling the organic solvent to obtain a liquid product to be deducted, the resulting solid or liquid product is halogenated nitrogen-containing unsaturated cyclic hydrocarbon. The method solves the problem of the nitrogen-containing unsaturated cyclic hydrocarbon over [...] reaction problems.
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Paragraph 0017
(2018/05/16)
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- Strategy to Prepare 3-Bromo- and 3-Chloropyrazoles
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A general strategy to prepare substituted 3-bromo- and 3-chloropyrazoles is described. The three-step method involves condensation of crotonates or β-chloro carboxylic acids with hydrazines, followed by halogenation and oxidation. Several condensation and oxidation protocols were developed to enable preparation of a wide variety of 3-halopyrazoles with good to excellent yields and regiocontrol.
- Fox, Richard J.,Schmidt, Michael A.,Eastgate, Martin D.
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p. 2830 - 2839
(2018/03/09)
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- EPOTHILONE ANALOGS, METHODS OF SYNTHESIS, METHODS OF TREATMENT, AND DRUG CONJUGATES THEREOF
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In one aspect, the present disclosure provides epothilone analogs of the formula (I) wherein the variables are as defined herein. In another aspect, the present disclosure also provides methods of preparing the compounds disclosed herein. In another aspect, the present disclosure also provides pharmaceutical compositions and methods of use of the compounds disclosed herein. Additionally, drug conjugates with cell targeting moieties of the compounds are also provided.
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Page/Page column 64; 65
(2017/05/02)
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- Method of controlling particular insect pests by applying anthranilamide compounds
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This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a benzoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.
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Page/Page column 41; 42
(2015/09/23)
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- Anthranilamide arthropodicide treatment
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This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.
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Page/Page column 40; 41
(2015/11/27)
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- HETEROCYCLIC COMPOUND
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The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
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Paragraph 0583
(2015/01/18)
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- HETEROCYCLIC HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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A hydrazide compound represented by the formula (I), an N-oxide thereof or suitable salt thereof: has excellent pesticidal activity.
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Page/Page column 391-392
(2008/12/08)
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- Rynaxypyr: A new insecticidal anthranilic diamide that acts as a potent and selective ryanodine receptor activator
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Rynaxypyr is a highly potent and selective activator of insect ryanodine receptors with exceptional activity on a broad range of Lepidoptera. A strong correlation between insecticidal activity and ryanodine receptor activation is observed along with selective activity against insect over mammalian receptors. The synthesis and biological results are presented.
- Lahm, George P.,Stevenson, Thomas M.,Selby, Thomas P.,Freudenberger, John H.,Cordova, Daniel,Flexner, Lindsey,Bellin, Cheryl A.,Dubas, Christine M.,Smith, Ben K.,Hughes, Kenneth A.,Hollingshaus, J. Gary,Clark, Christopher E.,Benner, Eric A.
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p. 6274 - 6279
(2008/03/14)
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- HYDRAZIDE COMPOUND AND PESTICIDAL USE OF THE SAME
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A hydrazide compound represented by the formula (1): has excellent pesticidal activity.
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Page/Page column 488-489
(2008/06/13)
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- MIXTURES OF ANTHRANILAMIDE INVERTEBRATE PEST CONTROL AGENTS
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Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-cyano-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, an N-oxide, or a salt thereof, Formula (1) and (b) at least one invertebrate pest control agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and salts of the foregoing. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a mixture or composition of the invention.
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Page/Page column 19; 24
(2008/06/13)
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- METHOD FOR PREPARING FUSED OXAZINONES
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A method for preparing a fused oxazinone is disclosed in which (1) a carboxylic acid is contacted with a sulfonyl chloride in the presence of an optionally substituted pyridine compound, the nominal mole ratio of sulfonyl chloride to carboxylic acid being from about 0.75 to 1.5; (2) the mixture prepared in (1) is contacted with an ortho-amino aromatic carboxylic acid in the presence of an optionally substituted pyridine compound, the nominal mole ratio of the ortho-amino aromatic carboxylic acid to carboxylic acid charged in (1) being from about 0.8 to 1.2; and (3) additional sulfonyl chloride is added to the mixture prepared in (2), the nominal mole ratio of additional sulfonyl chloride added in (3) to carboxylic acid charged in (1) being at least about 0.5. Also disclosed is a method for preparing a compound of Formula III, using a compound of Formula 1a that is characterized by preparing the fused oxazinone of Formula 1a by the method above, using a compound of the formula LS(O)2Cl as the sulfonyl chloride, a compound of Formula 2' as the carboxylic acid, and a compound of Formula 5' as the ortho-amino aromatic carboxylic acid (FORMULA 1a) (FORMULA III) (FORMULA 2') (FORMULA 5') wherein L, X, Y and R1 through R9 are as defined in the disclosure.
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- CYANO ANTHRANILAMIDE INSECTICIDES
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This invention provides compounds of Formula (I), N -oxides and suitable salts thereof INSERT FORMULA I HERE wherein R1 is Me, Cl, Br or F; R2 is F, Cl, Br, C1-C4 haloalkyl or C1-C4 haloalkoxy; R3 is F, Cl or Br; R4 is H or C1-C4 alkyl,C3-C4 alkenyl, C3-C4 alkynyl, C3-C5 cycloalkyl, or C4-C6 cycloalkylalkyl, each optionally substituted with one substituent selected from the group consisting of halogen, CN, SMe S(O)Me, S(O)2Me and OMe; R5 is H or Me; R6 is H, F or Cl; and R7 is H, F or Cl. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula (I), anN-oxide thereof or a suitable salt of the compound (e.g., as a composition described herein). This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula (I), an N-oxide thereof or a suitable salt of the compound and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent.
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- Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
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The present application describes lactam-containing compounds and derivatives thereof of Formula I: or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
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- PYRAZOLECARBOXAMIDE INSECTICIDES
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This invention provides compounds of Formula (I), N-oxides and salts thereof wherein: A is O or S; B is a phenyl ring or a pyridine ring, each ring optionally substituted with 1 to 5 R; J is a pyrazole or a pyrrole heterocyclic ring system as defined herein; and; R1 is H; or C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl or C3-C6 cycloalkyl each optionally substituted with one or more substituents selected from the group consisting of halogen, CN, NO2, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkylsulfinyl, C1-C4 alkylsulfonyl, C2-C4 alkoxycarbonyl, C1-C4 alkylamino, C2-C8 dialkylamino and C3-C6 cycloalkylamino.Also disclosed are methods for controlling at least one invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of at least one compound of Formula I, an N-oxide or a salt thereof (e.g., as a composition described herein). This invention also pertains to a composition comprising at least one compound of Formula I, an N-oxide or a salt thereof; and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent.
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- Synthesis and Reactions of 3,4-Bis(trimethylsilyl)-1-pyrazolines
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1,3-Dipolar cycloaddition of diazomethane to the trans-1,2-bis(trimethylsilyl)ethenes 1 a-c affords the trans-3,4-bis(trimethylsilyl)-1-pyrazolines 2 a-c.Thermolysis of 2 a-c yields stereospecifically the trans-1,3-bis(trimethylsilyl)propenes 7 b, c and d.The pyrazoline 2 c is dehalogenated with Zn to give 3(5),4-bis(trimethylsilyl)pyrazole (8).Reaction of 2 a with tetrachloro-o-benzoquinone and of 2 b and c with methanolic NaOH leads to dehydrosilylation and elimination of halogenotrimethylsilane, respectively, with formation of the pyrazoles 9 - 11. 10 and 11 can be desilylated by treatment with acid to yield 12 and 13, resp.
- Birkofer, Leonhard,Kuehn, Thomas
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p. 2293 - 2299
(2007/10/02)
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