- A hydrochloric acid flupentixol preparation method
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The invention provides a preparation method of flupentixol dihydrochloride, which comprises the following steps: reacting and dehydrating 10-hydroxy-10-(3-dimethylaminopropyl)-2-trifluoromethyl thioxanthene and sulfoxide chloride or acetic anhydride to prepare high-content Z-type 10-[3-(EZ)-dimethylaminopropyl]-2-trifluoromethyl thioxanthene, reacting with N-hydroxyethyl piperazidine to prepare flupentixol base, and finally, introducing sufficient hydrochloric acid gas into the flupentixol base to prepare the high-content Z-type flupentixol dihydrochloride. The method has the advantages of fewer steps, high yield and high product purity, is simple to operate, and does not use any extremely toxic substance to pollute the environment. The Z-type flupentixol dihydrochloride content in the flupentixol dihydrochloride prepared by the method is 42-52%, and conforms to the quality standard specification for flupentixol dihydrochloride in European Pharmacopoeia.
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Paragraph 0038-0043
(2020/02/08)
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- Preparation containing flupentixol pharmaceutical compositions
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The present invention provides a method for preparing a flupenthixol-containing drug composition. The method comprises that: 1) (9RS)-9-[3-dimethylamino-propyl]-2-(trifluoromethyl)-9H-thioxanthen-9-ol reacts with an acid so as to be subjected to dehydration; 2) the obtained material and N-(hydroxyethyl)piperazine are subjected to an amine exchange reaction to produce 2-[4-[3-[(EZ)-(trifluoromethyl)-9H-thioxanthen-9-ylidene]-propyl]-piperazin-1-yl]-ethanol base, and 3) the 2-[4-[3-[(EZ)-(trifluoromethyl)-9H-thioxanthen-9-ylidene]-propyl]-piperazin-1-yl]-ethanol base is subjected to precipitation to produce 2-[4-[3-[(EZ)-(trifluoromethyl)-9H-thioxanthen-9-ylidene]-propyl]-piperazin-1-yl]-ethanol dihydrochloride (flupenthixol dihydrochloride), wherein the method is characterized in that the step 1) and the step 3) are performed under an inert gas, and the step 2) is performed under vacuum.
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Paragraph 0059-0061
(2017/10/11)
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- Preparation method of medicinal flupentixol dihydrochloride
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The invention discloses a preparation method of medicinal flupentixol dihydrochloride. The preparation method comprises that 1), 2-trifluoromethyl-9-allylthioxanthenol, methyl tertiary-butyl ether and hydrochloric acid are uniformly mixed and undergo a reaction to produce 2-trifluoromethyl-9-(2-propenylidene)thiaxanthene, 2), 2-trifluoromethyl-9-(2-propenylidene)thiaxanthene and N-(2-hydroxyethyl)piperazine undergo an addition reaction in an organic solution at a reaction temperature of 100-150 DEG C for 5-20h to produce 9-[3-(4-ethoxy-1-piperazinyl)propylidene]-2-trifluoromethylthiaxanthene, 3), a flupentixol dihydrochloride crude product is prepared, and 4), the flupentixol dihydrochloride crude product is purified. The preparation method has simple processes and a short technical route, produces less by-products in the reaction, has a high yield, realizes high product purity and is suitable for industrial production.
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Paragraph 0085; 0086
(2016/10/07)
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- PROCESS FOR THE PREPARATION OF Z-FLUPENTIXOL
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The present invention relates to a process for the separation of flupentixol isomers, particularly, a process for the preparation of Z-flupentixol and the decanoate ester and novel synthetic intermediates thereof.
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Page/Page column 13
(2010/02/11)
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