80382-23-6Relevant articles and documents
Synthesis method of loxoprofen sodium
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, (2019/06/07)
The invention discloses a synthesis method of loxoprofen sodium, which comprises the following steps of: step 1), preparing N-(1-cyclopentenyl) morpholine; step 2), preparing 2-(4-bromomethyl phenyl)methyl propionate, the method also comprises the following step 3), preparing loxoprofen sodium by an enamine alkylation method: first dissolving 2-(4-bromomethyl phenyl) methyl propionate in a solvent, adding N-(1-cyclopentenyl) morpholine and the solvent in a container, dropwise adding 2-(4-bromomethyl phenyl) methyl propionate solution under reflux conditions; continuing reacting under reflux conditions after the completion of the dropwise addition; adding alkali solution after obtained reaction liquid is cooled, hydrolysising and separating to obtain an organic phase and an aqueous phase respectively, extracting the aqueous phase with an extractant to obtain extract liquid and the aqueous phase after extraction respectively, and post-treating the aqueous phase after extraction to obtain loxoprofen sodium. The preparation of loxoprofen sodium by the above method has the advantages of simple reaction steps, high yield of loxoprofen sodium and low production cost.
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 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.