207983-04-8Relevant articles and documents
Method for continuously synthesizing metoprolol and salts thereof
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Paragraph 0032-0047, (2021/04/14)
The invention discloses a method for continuously synthesizing metoram, which comprises the following steps: (1) carrying out vacuum rectification on a 1-(2, 3-epoxypropoxy)-4-(2-methoxyethyl)benzene raw material to obtain a pure product with the purity of more than 99%, and preparing the pure product into an ethanol solution; (2) uniformly mixing the ethanol solution obtained in the step (1) with isopropylamine, feeding the mixture into a pipeline reactor, and reacting to obtain a metoprolol reaction solution; and (3) depressurizing the reaction liquid, and recovering isopropylamine in a rectifying tower, wherein the tower bottom liquid contains high-purity metoprolol. The purity of the raw materials reaches 99% or above through the rectification step, and colored impurities are also removed; when metoprolol is synthesized, a rapid reaction method of large excess of isopropylamine in the pipeline reactor is adopted, so that secondary condensation side reactions are obviously reduced, and the purity of metoprolol reaches 98% or above; and after metoprolol is salified with succinic acid, a crude drug finished product with the purity larger than 99.5% can be obtained through crystallization. The method is high in yield, low in cost and easy to operate, and is an environment-friendly process route capable of realizing industrial production.
Method for preparing metoprolol salt
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Paragraph 0054; 0055, (2017/05/12)
The invention relates to a method for preparing a metoprolol salt which is simple to operate, high in yield, good in quality, low in cost and good in environmental-friendliness. According to the method provided by the invention, an acetone/water mixed solvent system is adopted, and an adverse dropping mode, that is, a mode that metoprolol is dropped into an organic acid solution, is adopted, so that the organic acid can be sufficiently dissolved, and a reaction can be sufficiently implemented, the reaction time can be greatly shortened, and the reaction conversion rate and the yield can be increased. The operation procedures are simplified, the time is shortened, the cost is lowered, and moreover, the quality of a product is greatly improved.
SYNTHESIS AND PREPARATIONS OF METOPROLOL AND ITS SALTS
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Page/Page column 4, (2009/10/06)
The invention relates to an improved process for preparing metoprolol and its salts.
