- Synthesis method of methoxamine hydrochloride
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The invention discloses a method for synthesizing methoxamine hydrochloride, and belongs to the technical field of organic synthesis. According to the technical scheme, 2, 5-dimethoxybenzaldehyde serves as an initial raw material, 3-(2, 5-dimethoxyphenyl)-3-hydroxy-2-methylpropanamide is obtained through (a) hydrolysis after a Grignard reaction or (b) ammonolysis after a Reformatsky reaction or (c) the Reformatsky reaction, then the prepared 3-(2, 5-dimethoxyphenyl)-3-hydroxy-2-methylpropanamide is subjected to a Hofmann degradation reaction and then salified, and the 3-(2, 5-dimethoxyphenyl)-3-hydroxy-2-methylpropanamide is obtained. The methoxamine hydrochloride is obtained; according to the technical scheme, 2, 5-dimethoxybenzaldehyde which is simple and easy to obtain is adopted as a starting raw material, any one of three reaction routes of (a)-(c) can be selected to synthesize a key intermediate 3-(2, 5-dimethoxyphenyl)-3-hydroxy-2-methylpropanamide, then the key intermediate is subjected to Hofmann degradation and salification, and methoxamine hydrochloride is obtained. The provided reaction conditions are mild, the reaction process is safe and controllable, the total reaction yield is high, the purity is high, and the method can be used for large-scale production.
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- MAO inhibition by arylisopropylamines: The effect of oxygen substituents at the β-position
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Twenty-nine arylisopropylamines, substituted at the β-position of their side chain by an oxo, hydroxy, or methoxy group, were evaluated in vitro as MAO-A and MAO-B inhibitors. The oxo derivatives ('cathinones') were in general less active as MAO-A inhibitors than the corresponding arylisopropylamines, but exhibited an interesting MAO-B inhibiting activity, which was absent in the hydroxy, methoxy, and β-unsubstituted analogues. These results suggest that selective affinity for the two MAO isoforms in this family of compounds is modulated not only by the aryl substitution pattern but also by the side-chain substituents on the arylalkylamine scaffold.
- Osorio-Olivares, Mauricio,Rezende, Marcos Caroli,Sepulveda-Boza, Silvia,Cassels, Bruce K.,Fierro, Angelica
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p. 4055 - 4066
(2007/10/03)
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- Patch and production method thereof
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The present invention relates to a patch containing a substrate, a non-crosslinked adhesive layer (A) containing a drug laminated on one surface of the substrate and a crosslinked adhesive layer (B) laminated on the adhesive layer (A). According to the present invention, the percutaneous absorbability of the drug can be improved, and a patch free of problems such as adhesive residue and adhesive bleed can be provided.
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