Aryl-2-thiohydantoin compound intermediate, preparation method and applications thereof

The invention relates to an aryl-2-thiohydantoin compound represented by a formula IV-a, and a preparation method thereof, and a method for preparing a compound represented by a formula V-a by using the compound represented by the formula IV-a as a key intermediate. The preparation method comprises:...

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Hauptverfasser: MA LIJIN, GAO LIHONG, CHEN XIAODONG, NIU MINGYU, MIAO JINPENG, DENG HONGGUI, MA ZHENQIAN, SHI DENGJIAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to an aryl-2-thiohydantoin compound represented by a formula IV-a, and a preparation method thereof, and a method for preparing a compound represented by a formula V-a by using the compound represented by the formula IV-a as a key intermediate. The preparation method comprises: carrying out acylating chlorination and substitution on an amino acid used as a starting raw material, carrying out cyclization by using a thio-source cyclization reagent to obtain a compound represented by a formula IV-a, and carrying out a coupling reaction on the compound represented by the formula IV-a and a compound represented by a formula IV-A to prepare a second-generation androgen receptor signal inhibitor. According to the present invention, the process route has characteristics of mild reaction and simple operation, avoids the use of cyanides or cyano compounds in the traditional process, and is suitable for process production. 本发明涉及一种式Ⅳ-a所示的芳基-2-硫代海因类化合物,及其制备方法,以及式Ⅳ-a化合物作为关键中间体制备式Ⅴ-a化合物的方法。首先,以氨基酸为起始原料