- Preparation method for tiaprofenic acid
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The invention relates to a preparation method for tiaprofenic acid. The method comprises the following steps: by taking 2-thiophenecarboxaldehyde as an initial raw material, reacting with methyl magnesium bromide, thereby compounding 1-(2-thienyl) alcohol; reacting with thionyl chloride for substituting chlorine group, cyaniding and hydrolyzing; and finally, performing Friedel-Crafts acylation reaction on the acquired product and benzoyl chloride, thereby acquiring tiaprofenic acid. The preparation method for tiaprofenic acid has the advantages that the common, low-cost and safe raw materialsare adopted for replacing rare, precious and dangerous raw materials, so that the serious pollution problem is avoided and the production cost is greatly lowered, besides, the process route adopted bythe invention is simple, the reaction period is short, the reaction condition is stable, the yield is high and reaches up to 90% or above, the purity of the acquired product after the reaction is high and the purity can reach up to 99% or above, so that the preparation method is suitable for industrial production.
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- Preparation method of non-steroidal anti-inflammatory drug tiaprofenic acid
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The invention relates to a preparation method of non-steroidal anti-inflammatory drug tiaprofenic acid. The preparation method includes: taking 2-chloromethyl thiophene as a starting raw material; synthesizing thiophene-2-acetonitrile by allowing 2-chloromethyl thiophene to react with trimethylsilyl cyanide; allowing thiophene-2-acetonitrile to react with dimethyl carbonate for methylation prior to cyan-hydrolysis; finally, performing benzoyl chloroformylation reaction to obtain tiaprofenic acid. The preparation method has the advantages that rare, valuable and dangerous materials are replacedwith common, cheap and safe raw materials, serious pollution problems are avoided, and production cost is greatly reduced; in addition, the process adopted in the method is short in route, short in reaction period, stable in reaction condition and high in yield which can be up to 90%, the product obtained is high in purity which can reach above 99%, and the preparation method is applicable to industrial production.
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- Synthetic process of tiaprofenic acid
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The invention relates to a synthetic process of tiaprofenic acid. The synthetic process comprises the following steps: adopting 2-thiotolene as a starting raw material, enabling 2-thiotolene to reactwith trimethylsilyl cyanide to synthesize 2-thiopheneacetonitrile by virtue of bromation, then enabling the 2-thiopheneacetonitrile to react with dimethyl carbonate to be methylated, hydrolyzing cyanogroups, and finally performing F-K reaction with benzoyl chloride, and preparing tiaprofenic acid. The synthetic process has the advantages that the conventional safe raw materials low in price are used for substituting the rare expensive and dangerous raw materials, so that the severe pollution problem is avoided, and the production cost is greatly decreased; and in addition, the process route adopted by the invention is simple, the reaction period is short, the reaction condition is stable, the yield is high and can reach more than 90 percent, the produce obtained after the reaction is highin purity, and the purity can reach more than 99 percent, so that the synthetic process is suitable for the industrialized production.
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- Synthetic process for non-steroidal anti-inflammatory drug tiaprofenic acid
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The invention relates to a synthetic process for a non-steroidal anti-inflammatory drug tiaprofenic acid. The synthetic process comprises the following steps: with thiophene as a starting material, subjecting thiophene to a reaction so as to prepare 2-(1-chloroethyl)thiophene; then reacting 2-(1-chloroethyl)thiophene with trimethylsilyl cyanide for cyanidation and hydrolysis of cyano groups; and finally carrying out a Friedel-Crafts reaction with benzoyl chloride so as to prepare tiaprofenac acid. The synthetic process has the following advantages that ordinary, cheap and safe raw materials are used for replacing rare, expensive and dangerous raw materials, so the problem of serious pollution is avoided, and production cost is greatly reduced; and the synthetic process is simple in process route, short in reaction period, stable in reaction conditions and high in yield, wherein the yield is up to 90% or more, tiaprofenic acid obtained after the reactions has a high purity of up to 99% or more, so the synthetic process is suitable for industrial production.
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- Novel preparation of tiaprofenic acid
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A new synthesis of the nonsteroidal anti-inflammatory drug tiaprofenic acid starting from thiophene is described. The sequence involves five steps, and the acylation with benzoyl chloride was catalysed by zinc oxide under solventfree conditions at room temperature. This method uses a much cheaper starting material and has a higher total yield (78.4%) than other methods. It is suitable for industrial production.
- Zhang, Shuguang,Huang, Shuang,Feng, Chengliang,Cai, Jin,Chen, Junqing,Ji, Min
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p. 406 - 408
(2013/09/12)
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- Process for the preparation of α-methyl-2-thiopheneacetic acid derivatives
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Process for the preparation of derivatives having general formula (I) STR1 wherein the meaning of R will be defined in the text, characterized by the reaction between a compound having formula STR2 wherein X is an halogen, and an alkaline salt of a methyl dialkylmalonate.
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- Process for the preparation of alpha-methyl-2-thiopheneacetic acid derivatives
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Process for the preparation of derivatives having general formula (I) wherein the meaning of R will be defined in the text, characterized by the reaction between a compound having formula wherein X is an halogen, and an alkaline salt of a methyl dialkylmalonate.
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- Esters and amides containing the 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetyl moiety
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Compounds of the formula STR1 wherein each X, which may be identical or different from the other X, is oxygen or imino; R1 is hydrogen, fluorine, chlorine or bromine; R2 and R3, which may be identical or different from each other, are each hydrogen; unsubstituted or mono-substituted alkyl of 1 to 6 carbon atoms, where the substituent is phenyl or dialkylamino with 1 to 3 carbon atoms in each alkyl moiety; pyridyl; or cycloalkyl of 5 to 7 carbon atoms; R2 and R3, together with each other and the nitrogen atoms to which they are attached, are pyrrolidino, piperidino, hexamethyleneimino, morpholino, N-aryl-piperazino or N-(alkyl of 1 to 3 carbon atoms)-piperazino; A is cycloalkylene of 5 to 7 carbon atoms; unsubstituted or substituted alkylene of 2 to 10 carbon atoms, where the substituents are one to two alkyls of 1 to 3 carbon atoms each, one to two carbalkoxys of 2 to 4 carbon atoms each, one to two phenyls, one to four hydroxyls, one halomethyl, one hydroxymethyl, one alkanoyloxy of 1 to 18 carbon atoms, one alkanoyloxymethyl of 1 to 18 carbon atoms in the alkanoyl moiety or one STR2 where R1, R2 and R3 have the meanings previously defined; or alkylene of 2 to 10 carbon atoms interrupted by oxygen, sulfur, sulfoxide, sulfonyl, phenyl, cyclohexyl, pyridyl, piperazino or unsubstituted or substituted imino, where the substituent on the imino group is alkyl of 1 to 6 carbon atoms, phenyl or phenylalkyl of 1 to 3 carbon atoms in the alkyl moiety; B is the acyl residue of an antiphlogistic carboxylic acid; and their non-toxic, pharmacologically acceptable acid addition salts. The compounds as well as their salts are useful as anti-inflammatories.
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- Novel α-thio-alkanoic acid derivatives
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Novel α-thio-alkanoic acid derivatives and a process for their preparation. These novel compounds can be easily converted to useful medicines.
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