132813-14-0Relevant articles and documents
Method for preparing blonanserin intermediate (BN-04)
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Paragraph 0025-0035, (2019/12/25)
The invention discloses a preparation method of a key Bnanserin intermediate (BN-04). The method comprises the following steps: reacting 4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocyclooctanopyridine-2(1H)-ketone (BN-03) with a chlorinating reagent hydrochloric acid in acetic anhydride at a low temperature, and after the reaction, recovering a solvent under reduced pressure; cooling to below 50 DEGC, adding dichloromethane and water, adjusting the pH value with ammonia water, layering, drying with anhydrous sodium sulfate, and recovering the dichloromethane to be clean under reduced pressure; adding a proper amount of ethanol to be completely dissolved, cooling, crystallizing and filtering to obtain 2-chloro-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocyclooctanopyridine (BN-04). Compared withthe prior art, cheap and high-quality hydrogen chloride is taken as a chlorinating reagent, a high-temperature (170 DEG C) reaction is avoided, the generation of impurities is reduced, repeated recrystallization in the refining process is avoided, and acetic anhydride can be repeatedly used as a reaction solvent. Green, safe and environment-friendly modern production can be realized.
Blonanserin and preparation method thereof
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Paragraph 0087; 0088; 0093; 0098; 0103; 0108, (2017/07/21)
The invention relates to Blonanserin and a preparation method thereof. The preparation method comprises the following specific steps that firstly, the compound shown in the formula III is reacted with a chlorinating agent, namely phosphenylic oxychloride, and the compound shown in the formula II is obtained; secondly, in the presence of potassium iodide, the compound shown in the formula II is reacted with N-ethylpiperazine, and the compound shown in the formula I, namely Blonanserin, is obtained. The preparation method has the advantages shown in the description.
Method for Preparing Blonancerin with Mild Condition
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Paragraph 0046; 0047; 0048, (2016/10/10)
The present invention provides a novel producing method of blonanserin. A producing method of the present invention has mild reaction temperature and short reaction time, can produce high-purity and high-yield blonanserin and is suitable for mass producti