80382-23-6Relevant articles and documents
Loxoprofen derivative
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Paragraph 0036; 0037; 0039; 0044, (2019/01/23)
The invention provides a Loxoprofen derivative shown in the following formula (I). R1 is hydrogen atoms or substituted or non-substituted alkyl, R2 is substituted or non-substituted alkyl, the Loxoprofen derivative has low gastrointestinal tract side effects, and the bioavailability can be improved. The formula (I) is shown in the specification.
Loxoprofen sodium preparation method
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Paragraph 0022-0029, (2019/05/11)
The invention discloses a loxoprofen sodium preparation method, which comprises: directly carrying out alkylation on 2-(p-bromomethyl)isophenylpropionic acid as a starting raw material under a NaOH and DMF system, carrying out hydrolysis decarboxylating to obtain a crude product, separating the by-product produced in the reaction through high-vacuum distillation to obtain loxoprofen acid, and carrying out salt forming to obtain the loxoprofen sodium. According to the present invention, the method has characteristics of less synthesis step, mild reaction condition, reasonable price and easy purchase of the raw material, low pollution and low production cost, and is suitable for industrial production, wherein the product content can reach more than 99.8%, and the single impurity is less than0.05%.
Loxoprofen sodium dihydrate crystal form and preparation method thereof
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Paragraph 0034-0041, (2019/01/10)
The invention relates to a loxoprofen sodium dihydrate crystal form preparation method thereof. The loxoprofen is dissolved in a dissolving solvent and reacted with sodium-containing base to prepare loxoprofen sodium, and after adding water, the seed crystal may or may not be added to prepare the loxoprofen sodium dihydrate crystal form. The crystal form preparation method obtains the high-puritycrystal form, and the novel crystal form has good fluidity and appearance.