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.
Succinic acid δ S-metoprolol of the crystal and its preparation method and application
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Paragraph 0034; 0035, (2016/10/17)
The invention discloses a crystal form delta of metoprolol succinate. The crystal form comprises the following characteristic peaks shown in an X-ray powder diffraction pattern when the reflection angle is 2theta: 3.98+/-0.1, 7.95+/-0.1, 10.92+/-0.1, 12.28+/-0.1, 14.66+/-0.1, 16.02+/-0.1, 18.39+/-0.1, 19.77+/-0.1 and 20.99+/-0.1. The crystal form is good in stability and slow in dissolving rate. The invention also provides a preparation method and application of the crystal form. The method for preparing the crystal form delta of metoprolol succinate has the characteristics of high repeatability and strong operationality. The crystal form delta of metoprolol succinate is applicable to prepare pharmaceutical compositions and has important application meaning on preparation of medicines for treating hypertension.
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.
