3290-06-0Relevant articles and documents
N-(Substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof
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Paragraph 0657; 0659-0663, (2019/04/17)
The invention relates to an N-(substituted sulfonyl)benzamide derivative and preparation method and pharmaceutical application thereof, in particular to an N-(substituted sulfonyl)benzamide derivativeshown as general formula (I), preparation method thereof, medicinal salts of the derivative, and their application as therapeutics, especially as Nav1.7 inhibitors, wherein substituents in the general formula (I) shown in the description are defined the same as in the description.
Synthesis method for herbicide oxaziclomefone intermediate 3,5-dichlorobenzyl chloride
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Paragraph 0008; 0026-0048, (2019/02/04)
The invention discloses a synthesis method for herbicide oxaziclomefone intermediate 3,5-dichlorobenzyl chloride, and belongs to the field of pesticide preparation. The synthesis method is characterized in that 3,5-dichlorobenzoic acid, a composite hydrog
Pyrazole derivatives
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, (2008/06/13)
This invention relates to the use of pyrazole derivatives of the formula and pharmaceutically acceptable salts and solvates thereof, in the manufacture of a reverse transcriptase inhibitor or modulator, to certain novel such pyrazole derivatives and to processes for the preparation of and compositions containing such novel derivatives.
Binding activity of substituted benzyl derivatives of chloronicotinyl insecticides to housefly-head membranes, and its relationship to insecticidal activity against the housefly Musca domestica
Nishiwaki, Hisashi,Nakagawa, Yoshiaki,Takeda, David Y.,Okazawa, Atsushi,Akamatsu, Miki,Miyagawa, Hisashi,Ueno, Tamio,Nishimura, Keiichiro
, p. 875 - 881 (2007/10/03)
Variously substituted benzyl derivatives of chloronlcotinyl insecticides were synthesized with a wide range of substituents including halogens, NO2, CN, CF3 and small alkyl and alkoxy groups at the ortho, meta and para positions, as well as multiple-substituted benzyl analogues. Their binding activity to the α-bungarotoxin binding site in housefly (Musca domestica) head membrane preparations was measured. Among the compounds tested, the activity of the meta-CN derivative was the highest, being 20-100 times higher than those of imidacloprid, acetamiprid and nitenpyram. The synergized insecticidal activity against houseflies was also measured for selected compounds with the metabolic inhibitor, NIA16388 (propargyl propyl phenylphosphonate). For the nitromethylene analogues, including both benzyl and pyridylmethyl analogues, higher binding activity usually resulted in higher insecticidal activity. (C) 2000 Society of Chemical Industry.
Insecticidal substituted-2,4-diamino-5,6,7,8-tetrahydroquinazolines
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, (2008/06/13)
There is provided an insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a tetrahydroquinazoline compound of the formula STR1 wherein R, R1, R2, R3, R5, R6, R7, R8, and R9 are as defined herein, and methods of using the same. Certain novel substituted-phenyl tetrahydroquinazoline compounds per se are also identified.
An Improved Procedure for the Preparation of 1-Benzyl-1H-1,2,3-triazoles from Benzyl Azides.
Cottrell, Ian F.,Hands, David,Houghton, Peter G.,Humphrey, Guy R.,Wright, Stanley H. B.
, p. 301 - 304 (2007/10/02)
A procedure for the preparation of substituted 1-benzyl-1H-1,2,3-triazoles from benzyl azides under very mild conditions is described.The method provides improved yields and extends the scope of the Dimroth Reaction to other types of active methylene compound to those previously used.Benzyl azides react with active methylene compounds in dimethyl sulphoxide catalysed by potassium carbonate at 35-40 deg C to give 1H-1,2,3-triazoles usually in good yield.Acetonitrile derivatives gave 5-amino-1H-1,2,3-triazoles whereas diethyl malonate gave 5-hydroxy-1H-1,2,3-triazoles. 1H-1,2,3-Triazole-4-carboxylate esters and 1H-1,2,3-triazole-4-ketones were obtained from ethyl acetoacetate and β-diketones respectively.Benzyl methyl ketone reacted to give 5-methyl-4-phenyl-1H-1,2,3-triazole, but acetone and acetophenone failed to react.Other active methylene compounds which did not react under these reaction conditions included ethyl cyanoacetate, ethyl fluoroacetate and ethyl nitroacetate.
Pharmacologically active CNS compound
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, (2008/06/13)
The invention provides a series of compounds of formula (I) and salts thereof, wherein for example,R1 and R2, which may be the same or different each represent -NR13R14 where R13 and R14 may each independently represent hydrogen or alkyl or, taken together with the nitrogen atom to which they are attached form a heterocyclic ring, optionally substituted by one or more alkyl or arylalkyl groups and optionally containing a further heteroatom;, R3 is hydrogen, haloalkyl, alkoxymethyl or alkyl;, R4 is hydrogen, nitro or halo;, R5 is hydrogen or halo;, R6 is hydrogen, halo, nitro, amino, alkylamino or dialkylamino;, R7 is hydrogen or halo;, R8 is hydrogen or halo; The compounds may be used for the treatment or prophylaxis of a neurodegenerative or other neurological disorder of the CNS, the aetiology or which includes excessive release of the neurotransmitter glutamate.
METABOLISM OF CHLOROPHENYLALANINES IN CROP AND WEED PLANTS IN RELATION TO THE FORMATION OF POTENTIAL HERBICIDAL END PRODUCTS
Taylor, David C.,Wightman, Frank,Kazakoff, Clem W.
, p. 51 - 72 (2007/10/02)
Metabolism of 12 synthetic D,L-chlorophenylalanines has been examined in several crop and weed plants.Twenty-five gram samples of excised shoots or leaves of bushbean, soybean, corn, pigweed, lambsquarters, and giant foxtail were allowed to metabolize 10-4 M solutions of the D,L-chlorophenylalanines for 24 hr in continuous light.The plant samples were then extracted in 80percent methanol and the soluble acidic metabolites fractionated into ether.Each ether concentrate was partially purified by fractional elution from a PrepSep C18 coloumn and then analysed by HPLC.Collected fractions were esterified with pentafluorobenzylbromide and examined by GC-MS to demonstrate the presence of PFB-esters of chlorophenylacetic, chlorobenzoic and/or chlorocinnamic acids.Since certain of these metabolites are known to be potent plant growth-regulators and herbicides, the results are discussed in relation to the potantial herbicidal action of certain chlorophenylalanines by the mechanism of 'lethal synthesis'.Key Word Index - Phaseolus vulgaris; Glycine max.; Leguminosae; Zea mays; Amaranthus retroflexus; Chenopodium album; Setaria faberii; metabolism; D,L-chlorophenylalanines; chlorophenylacetic acids; chlorobenzoic acids; chlorocinnamic acids; growth regulators.