- Azulene sulfonamide synthesis method
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The invention discloses an azulene sulfonamide synthesis method, which comprises: 1, adding sodium azulene sulfonate and thionyl chloride to a flask filled with an organic solvent, and carrying out astirring reaction process for a period of time at a temperature of 0 DEG C in an ice bath to obtain a solution containing a compound 1, wherein a compound 2 is p-phenylenediamine protected by an aminoprotection agent, 2, adding the compound 2 into the solution of the compound 1, and reacting for a period of time to obtain a solution containing a compound 3, and 3, adding trifluoroacetic acid intothe solution of the compound 3, reacting for a period of time, recovering the organic solvent under reduced pressure, and carrying out column chromatography separation to obtain a blue final productcompound 4, namely azulene sulfonamide. The yield of azulene sulfonamide prepared by the synthesis method disclosed by the invention is increased, the separation and purification method of sodium azulene sulfonate is simple and rapid, byproducts of separation and purification of azulene sulfonamide are reduced, and the yield is increased. The separation and purification method provided by the invention is more efficient.
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- N-SUBSTITUTED ISOPROPYLDIMETHYL AZULENE SULFONAMIDE DERIVATIVES, AND PREPARATION METHOD AND USE THEREOF
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The present invention provides an N-substituted isopropyldimethyl azulene sulfonamide derivative as represented by formula (I), and preparation method and uses thereof, wherein R1 is an alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, amino, or a substituted alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, and amino. The N-substituted isopropyldimethyl azulene sulfonamide derivative can be used in treating gastric ulcer.
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- Synthesis and antigastric ulcer activity of novel 5-isoproyl-3,8- dimethylazulene derivatives
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5-Isoproyl-3,8-dimethylazulene derivatives were synthesized and evaluated for antigastric ulcer activity in vivo. Some of them possess the best activity against gastric ulcer with ulcer index values lower than the drug reference (omeprazole). The structure-activity relationship (SAR) shows that the lipophilic flat structure contributes to quite potent antigastric ulcer activity.
- Zhang, Lu-Yun,Yang, Fang,Shi, Wan-Qi,Zhang, Ping,Li, Ying,Yin, Shu-Fan
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p. 5722 - 5725
(2011/10/18)
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