1H-NMR、MS確證了結(jié)構(gòu),質(zhì)量分?jǐn)?shù)為99.8%,該路線的總收率為22.5%。結(jié)論 該合成工藝原料廉價(jià)易得、操作簡(jiǎn)單,適于工業(yè)化生產(chǎn)。;Objective To improve the process for synthesis of vilazodone hydrochloride. Methods The key intermediate 5-(1-piperazinyl)benzofuran-2-carboxamide was prepared from 4-(4-acetylpiperazine-1-yl)phenol by Duff reaction, substitution, cyclization, deprotection, and amidation. Vilazodone hydrochloride was synthesized from 5-(1-piperazinyl)benzofuran-2-carboxamide and 3-(4-chlorobutyryl)-1H-indole-5-carbonitrile by substitution and salification. Results The target compound vilazodone hydrochloride was synthesized and characterized by 1H-NMR and MS. The purity was 99.8%, and the total yield of this synthetic route was 22.5%. Conclusion The synthetic process with facile material and simple operation simplified method is applicable to industrial production."/>

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首頁(yè) > 過(guò)刊瀏覽>2017年第32卷第3期 >2017,32(3):361-364. DOI:10.7501/j.issn.1674-5515.2017.03.001
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鹽酸維拉佐酮的合成工藝改進(jìn)研究

Improvement of synthetic process of vilazodone hydrochloride

發(fā)布日期:2017-04-08