- Preparation method of isoproterenol hydrochloride
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The invention relates to the technical field of raw material medicine synthesis, in particular to a preparation method of isoproterenol hydrochloride. According to the preparation method, water, N, N-dimethylformamide or an aqueous solution of N, N-dimethylformamide is used as a solvent, borohydride is used as a reducing agent to carry out reduction reaction on isopropyladrenolone or salt thereof, the reaction conditions are mild, compared with a conventional hydrogenation reduction process, the production safety is remarkably improved, the production cost is greatly reduced, the usage amount of borohydride is small, and the environmental protection is improved to a certain extent. The product obtained by the preparation method is very high in purity, is suitable for industrial production of isoprenaline hydrochloride as a medicine raw material medicine product, and can effectively avoid toxic and side effects caused by impurities.
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- Hydrochloric acid isopropyl adrenergic preparation method
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The invention discloses a hydrochloric acid isopropyl adrenergic preparation method, comprises the following steps: through the catechol with glycine in the role of the catalyst [...] reaction to obtain 2 - amino - 1 - (3, 4 - dihydroxy-phenyl) - ethyl ketone; through the 2 - amino - 1 - (3, 4 - dihydroxy-phenyl) - ethanone with 2 - chloro propane reaction preparation isopropyl adrenergic ketone bodies hydrochloride; through the isopropyl adrenergic ketone bodies hydrochloride in the catalytic reduction of the palladium-carbon under the action of hydrochloric acid isopropyl adrenergic. Selects the glycin, zinc chloride the reaction system, which not only reduces the costs of environmental protection, also improves the reaction yield, is favorable for industrial production; mild reaction conditions, less catalyst levels, the process is simple; it has obvious economic and environmental benefits.
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- Method for preparing isoproterenol sulfate
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The invention discloses a method for preparing isoproterenol sulfate. The method comprises the following steps: (1) performing hydrogenation reduction on isoproterenol ketone in a methanol solvent in the presence of sodium borohydride at room temperature, so as to obtain isoproterenol; (2) performing negative pressure concentration on the solvent methanol, adding water, extracting with ethyl acetate, regulating the pH value of the system to be acidic by using 60% of sulfuric acid, raising the temperature to reflux for 30 minutes, and clarifying; (3) freezing overnight to obtain a white powdered crystal; (4) filtering, washing, drying, and recrystallizing with ethanol, thereby obtaining the isoproterenol sulfate. According to the method disclosed by the invention, hidden danger of high-pressure hydrogenation is avoided, and the reaction is safe by adopting sodium borohydride for reduction; with the adoption of a normal pressure reaction, usage of a metal high-pressure reactor is avoided; the raw materials are readily available, and the process is simple and reasonable.
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Paragraph 0010; 0011; 0012; 0013; 0014
(2018/03/13)
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- Metaproterenol, isoproterenol, and their bisdimethylcarbamate derivatives as human cholinesterase inhibitors
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Metaproterenol and isoproterenol are bronchodilators that provide a structural basis for many other bronchodilators currently in use. One of these structurally related bronchodilators is terbutaline; it is administered as a prodrug, bambuterol, and is metabolized (bioconverted) into terbutaline by butyrylcholinesterase (BChE). The metabolism rate can be affected by BChE gene polymorphism in the human population and BChE stereoselectivity. The aim of our study was to investigate inhibition of human BChE and acetylcholinesterase (AChE) with metaproterenol, isoproterenol, and newly synthesized racemic bisdimethylcarbamate derivatives of metaproterenol (metacarb) and isoproterenol (isocarb) and their (R)-enantiomers to see if their bioconversion is affected by BChE inhibition in the same way as that for bambuterol. Metacarb and isocarb proved to be selective BChE inhibitors, as they progressively inhibited AChE 960 to 80 times more slowly than BChEUU. All studied cholinesterases displayed poor affinity for metaproterenol and isoproterenol, yet BChE UU had an affinity about five times higher than that of AChE.
- Bosak, Anita,Smilovi?, Ivana Gazi?,?inko, Goran,Vinkovi?, Vladimir,Kovarik, Zrinka
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body text
p. 6716 - 6723
(2012/09/22)
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- The acid-catalysed racemisation mechanism of catecholamines
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The racemisation rates of (-)-adrenaline (1), ()-isoprenaline (2), (-)-2-(3,4-dimethoxyphenyl)-2-hydroxy-N-isopropylamine (3), (+)-2-(4-meethoxyphenyl)-2-hydroxy-N-isopropylethylamine (4), (+)-2-phenyl-2-hydroxy-N-isopropylehylamine (5), ()-phenylephrine(6), and (+)-1-phenylethanol(7) were compared. The racemisatton rates decreased in the following order: 7> 1 ≈ 2 > 3 ≈ 4 ? 5, 6. In general, the reactivity of the series of the phenylethanolamine compounds (1) - (6) was seen to increase sharply as the electron-releasing ability of the p-substituent of the aromatic nucleus increases. The results strengthen the notion that the acid-catalysed racemisation of catecholamines proceeds via a quinonoid-type intermediate.
- Venter, Daniel P.
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p. 5019 - 5024
(2007/10/02)
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- Polyprenylcarboxylic acid amides
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There is disclosed a polyprenylcarboxylic acid amide of the formula: STR1 wherein R1 represents a hydrogen atom or a lower alkyl group, R2 represents a hydrogen atom or a group of the formula: --COOR4 in which R4 represents a lower alkyl group, R3 represents a hydrogen atom or an OH group and n represents an integer of 1 to 6.
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