- Preparation method of 7-piperazinyl benzothiophene or salt thereof
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The invention discloses a preparation method of 7-piperazinyl benzothiophene or salt thereof, comprising the following steps: (1) carrying out substitution ring closing reaction on a compound 3 and acompound 4 to obtain a compound 5; (2) carrying out hydr
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- Method for preparing benzothiophene derivative
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The invention relates to a method for preparing a benzothiophene derivative. The method comprises the following steps: taking 7-nitrothiophene as a raw material, and forming a thiophene derivative through nucleophilic substitution. The method provided by the invention has the advantages of mild reaction conditions, simple operation, controllable post-treatment and convenient quality control, and is beneficial to large-scale industrial production.
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- Compounds useful in treating cytokine mediated diseases
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Disclosed are amide compounds of formula(I): wherein Ar1, Q, Y and R3-R6 of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating d
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- 7-Substituted Benzothiophenes and 1,2-Benzisothiazoles. Part 2. Chloro and Nitro Derivatives
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The 7-chloro and 7-nitro derivatives of benzothiophene and 1,2-benzisothiazole have been prepared from readily available precursors, which for each substituent are common to both ring systems. 7-Chlorobenzothiophene has been obtained from 3-chloro-2-mercaptobenzoic acid via 7-chlorobenzothiophen-3(2H)-one, or from 2,3-dichlorobenzaldehyde, either via β-(2,3-dichlorophenyl)-α-mercaptoacrylic acid (16) or, preferably, via 7-chlorobenzothiophene-2-carboxylic acid.Hexamethylphosphoric triamide is a particularly useful solvent in which to effect the selective nucleophilic replacement of the 2-chloro substituent in 2,3-dichlorobenzaldehyde. 7-Chloro-1,2-benzisothiazole is available by treatment of 3-chloro-2-mercaptobenzaldehyde with chloramine (57percent), or by heating 2,3-dichlorobenzaldehyde with sulphur and aqueous ammonia (46percent). 7-Nitrobenzothiophene has been obtained by treatment of 2-bromo-3-nitrobenzaldehyde with mercaptoacetic acid under alkaline conditions, followed by decarboxylation of the resulting 2-carboxylic acid.Cyclisation of 2-(n- or t-butylthio)-3-nitrobenzaldoxime with polyphosphoric acid gives 7-nitro-1,2-benzisothiazole in high yield. 3-Nitro-2-t-bytylthiobenzaldehyde behaves unexpectedly with chloramine, to give what is believed to be 7-nitro-2-t-butyl-1,2-benzothiazolium chloride (24) (73percent).
- Rahman, Loay K. A.,Scrowston, Richard M.
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p. 385 - 390
(2007/10/02)
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