Synthesis method of prucalopride impurities

The invention discloses a synthesis method of a prucalopride impurity, and relates to the technical field of organic synthesis of medicines. 4-amino-5-chloro-2, 3-dihydro-N-[1-(3-methoxypropyl)-4-piperidyl]-7-benzofuranformamide is used as a raw material, the target product is prepared by taking eas...

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Hauptverfasser: FENG YISI, FENG HUIYI, XIE DALE, HE YONG
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a synthesis method of a prucalopride impurity, and relates to the technical field of organic synthesis of medicines. 4-amino-5-chloro-2, 3-dihydro-N-[1-(3-methoxypropyl)-4-piperidyl]-7-benzofuranformamide is used as a raw material, the target product is prepared by taking easily available N-hydroxyphthalimide, butylated hydroxytoluene (BHT) and tetramethylpiperidine nitrogen oxide (TEMPO) as catalysts through a one-pot method, a high-purity reference substance is provided for detection and content control of the two impurities in the prucalopride product, and the methodis short in reaction time, high in yield, high in purity and suitable for industrial production. 本发明公开了一种普芦卡必利杂质的合成方法,涉及药物有机合成技术领域,本发明以4-氨基-5-氯-2,3-二氢-N-[1-(3-甲氧基丙基)-4-哌啶基]-7-苯并呋喃甲酰胺作为原料,以原料易得N-羟基邻苯二甲酰亚胺、二丁基羟基甲苯(BHT)和四甲基哌啶氮氧化物(TEMPO)作为催化剂,一锅法制备目标产物,为普芦卡必利产品中这两种杂质的检测和含量控制提供了高纯度的对照品,反应时间短,收率高,纯度高,适合工业化生产。