- Straightforward synthesis of 2-acetyl-substituted benzo[b]thiophenes
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Described herein is a green one-step protocol for the preparation of substituted 2-acetylbenzo[b]thiophenes from commercially available aromatic halides. This efficient method has the advantage of using water as the reaction medium, resulting in a high yield of pure cyclized products. Two scaffold types have been prepared using this general procedure: 2-acetylbenzo[b]thiophenes and 2-acetyl-3-aminobenzo[b]thiophenes, both crystallized directly from the reaction mixture, due to their low solubility with water, and without the need for an additional purification step. Georg Thieme Verlag Stuttgart · New York.
- Debray, Julien,Lemaire, Marc,Popowycz, Florence
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- 2-Acetylthienopyridine Synthesis via Thiolation and Copper-Catalyzed Cyclization of o-Propynol Fluoropyridine Using Xanthate as a Thiol Surrogate
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2-Acylthienopyridines and related heterocycles are readily prepared in moderate to good yields under mild conditions by a nucleophilic thiolation, copper-catalyzed cyclization, and an oxidation cascade process using potassium xanthate as the thiol source.
- Li, Yibiao,Luo, Xianglin,Shao, Yan,Chen, Lu
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- Method for synthesizing 2-carbonyl thienopyridine compound
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The invention discloses a method for synthesizing 2-carbonyl thienopyridine compound. According to the method provided by the invention, 2-halo-3-alkynol pyridine as shown in formula (I) and sulfur sources are mixed; and with the aid of a catalyst, after reacting in a solvent for a while, 2-carbonyl thienopyridine compound as shown in formula (II) is prepared after purification treatment. The sulfur sources are selected from one or more of elemental sulphur, ammonium sulfide, thiourea, sodium sulfide, and ethyl potassium xanthate, and the catalyst is selected from one of copper acetate, cuprous iodide, cuprous bromide, cuprous chloride, copper chloride, cupric acetylacetonate, palladium chloride, and copper trifluoromethanesulfonate. The technical scheme of the invention has the advantagesof less reaction steps, simple operation method, wide source of reaction substrate, low costs and easy availability of the catalyst, high product yield and the like, and the technical scheme is verysuitable for industrial mass production. The formulas are shown in the description.
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Paragraph 0023; 0024; 0025; 0026; 0027; 0028
(2019/01/08)
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- Metal free coupling of heteroaryl N-tosylhydrazones and thiols: Efficient synthesis of sulfides
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A metal free coupling of heteroaromatic N-tosylhydrazones with thiols is presented. A convenient synthetic route to synthesize heteroaryl N-tosylhydrazones is also showed. Valuable thioethers with pyrroles, pyridines, thieno[2,3-b]pyridines, imidazo[1,2-a]pyridines, and 6H-thieno[2,3-b]pyrroles derivatives were synthesized in good yields. This coupling reaction can be carried out in a one-pot fashion and scaled up to the gram scale by using heteroaryl aldehydes, without the need to isolate the N-tosylhydrazone.
- García-Carrillo, Mario Alfredo,Guzmán, ángel,Díaz, Eduardo
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supporting information
p. 1952 - 1956
(2017/04/27)
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- DIHYDROISOXAZOLE COMPOUNDS, PARASITICIDAL USES AND FORMULATIONS THEREOF
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Provided are dihydroisoxazole compounds useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier.
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Page/Page column 52; 53
(2012/12/13)
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- PARASITICIDAL COMPOUNDS, METHODS, AND FORMULATIONS
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Provided are dihydroisoxazole compounds useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
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Page/Page column 57
(2012/12/13)
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- PARASITICIDAL DIHYDROISOXAZOLE COMPOUNDS
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Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.
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Page/Page column 56; 57
(2012/12/13)
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