- 5-chloro-3-thiophenecarboxylic acid preparation method
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The present invention discloses a 5-chloro-3-thiophenecarboxylic acid preparation method comprising the following steps: (1) adding 3-thiophenecarboxylic acid and an organic solvent into a reaction vessel, reducing the temperature to 0 DEG C to -30 DEG C, adding dropwise sulfuryl chloride into the reaction vessel, and after the addition is complete, heating slowly to 0 DEG C-20 DEG C for reaction for 1 to 3 hours; (2) after completion of the reaction, pouring the reaction solution into ice water, layering the reaction solution, separating an organic layer, drying the organic layer, filtering and concentrating to obtain a crude 5-chloro-3-thiophenecarboxylic acid product; (3) using methyl tert-butyl ether for recrystallizing the crude 5-chloro-3-thiophenecarboxylic acid product obtained in the step (2), filtering to obtain a crystal solid, and drying the crystal solid to obtain a pure 5-chloro-3-thiophenecarboxylic acid product. The novel 5-chloro-3-thiophenecarboxylic acid preparation method is provided, and a 5-chloro-3-thiophenecarboxylic acid product with a purity of 97% can be obtained.
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Paragraph 0020; 0021
(2016/11/24)
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- ANTIVIRAL COMPOUNDS
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The present invention discloses compounds of Formula I wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the pre
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Page/Page column 39
(2014/09/29)
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- Novel thienopyrrole glycogen phosphorylase inhibitors: Synthesis, in vitro SAR and crystallographic studies
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Two series of novel thienopyrrole inhibitors of recombinant human liver glycogen phosphorylase a (GPa) which are effective in reducing glucose output from rat hepatocytes are described. Representative compounds have been shown to bind at the dimer interface site of the rabbit muscle enzyme by X-ray crystallography.
- Whittamore, Paul R.O.,Addie, Matthew S.,Bennett, Stuart N.L.,Birch, Alan M.,Butters, Michael,Godfrey, Linda,Kenny, Peter W.,Morley, Andrew D.,Murray, Paul M.,Oikonomakos, Nikos G.,Otterbein, Ludovic R.,Pannifer, Andrew D.,Parker, Jeremy S.,Readman, Kristy,Siedlecki, Pawel S.,Schofield, Paul,Stocker, Andy,Taylor, Melvyn J.,Townsend, Linda A.,Whalley, David P.,Whitehouse, Jennifer
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p. 5567 - 5571
(2007/10/03)
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- NEW COMPOUNDS
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The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.
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- Phosphorylamides, their preparation and use
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A phosphorylamide derivative represented by the general formula (I): STR1 wherein R represents an amino group that may be substituted, or a salt thereof, possesses potent antibacterial activity against Helicobacter bacterium, especially Helicobacter pylori, and is useful for prevention or treatment of digestive diseases caused by Helicobacter bacterium, solely or in combination with an antacid or an acid secretion inhibitor.
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- Antiparasitic agents
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The invention provides novel compounds having the formula: STR1 wherein R when taken individually is H; R1 when taken individually is H or OH; R and R1 when taken together represent a double bond; R2 is an alpha-branched C3 -C8 alkyl, alkenyl, alkynyl, alkoxyalkyl or alkylthioalkyl group; a C3 -C8 cycloalkyl, C5 -C8 cycloalkenyl or C5 -C8 cycloalkylalkyl group, any of which may be substituted by methylene or one or more C1 -C4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be substituted by one or more C1 -C4 alkyl groups or halo atoms; R3 is hydrogen or methyl; R4 is H or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy with the proviso that when R2 is alkyl it is not isopropyl or sec-butyl; when R4 is H, each of R and R1 is H, and R2 is not methyl or ethyl; and when R4 is H, R is H, R1 is OH, and R2 is not 2-buten-2-yl, 2-penten-2-yl or 4-methyl-2-penten-2-yl. The compounds are broad spectrum antiparasitic agents having utility as anthelmintics, ectoparasiticides, insecticides and acaricides. The invention also provides a process for producing the novel avermectin and milbemycin derivatives by adding a carboxylic acid or derivative thereof to a fermentation of an avermectin or milbemycin producing organism.
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- Herbicidal Thienylureas, I
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Syntheses of the title substances as potential herbicides are described by a modified Curtius degradation of corresponding thiophene carboxylic acids, obtained in turn by haloform reaction of appropriate acetyl thiophenes.Regioselective substitution reactions of thiophenes were key steps for the construction of desired substitution patterns.Structure-activity considerations show that especially the 3-thienyl ureas 36 and 38 exhibit significant herbicidal activity comparable with commercial products. - Keywords: Curtius degradation; Herbicides; Thiophenes; Ureas; Urethanes
- Stanetty, Peter,Puschautz, Erhard,Friedbacher, Gernot
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