Afatinib analog as well as preparing method and application

The invention discloses an afatinib analog, as shown in formula I. In addition, the invention also discloses a preparation method of a high-purity of the analog. The preparation method of the high-purity of the analog comprises: using a trans-4-dimethylamino crotonic acid hydrochloride as a raw mate...

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Hauptverfasser: SHI YING, DAI HUASHAN, XU JINGREN, DONG ZHIKUI, WANG SHIKANG, YIN LIXIAN, ZHAI JIAPING, LIANG HUIXING, HU TAO, CAI WEI, XIA YU, LIU XU
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses an afatinib analog, as shown in formula I. In addition, the invention also discloses a preparation method of a high-purity of the analog. The preparation method of the high-purity of the analog comprises: using a trans-4-dimethylamino crotonic acid hydrochloride as a raw material to form trans-4-dimethylamino-2-butene-acyl chloride hydrochloride under the condition of thionyl chloride; and then reacting with N4-(3-chloro-4-fluoro-phenyl)-7-(S)-tetrahydrofuran-3-yloxy)quinazoline-4,6,-diamine, and obtaining the compound of formula I after purifying. The preparation method provided by the invention has the advantages that the raw material is easy to obtain, the operation is simple, the condition is mild, and the repeatability is good; and the preparation method is suitable for the production of the high-purity of the compound of the formula I. In addition, the compound of the formula I is used as a reference material for the research of the related substance, andcan be applied to the afa