1289942-55-7Relevant articles and documents
Preparation method of enzalutamide of formula (VIII)
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, (2019/05/02)
The invention discloses a preparation method of enzalutamide of formula (VIII). The method comprises the following steps: carrying out a condensation reaction on a compound of formula (I) and an aminoprotecting group PG-containing compound of formula (II) to produce a compound of formula (III); carrying out a protecting group PG removal reaction on the compound of formula (III) to form a compoundof formula (IV); carrying out a coupling reaction on the compound of formula (IV) and a compound of formula (V) at 25-160 DEG C to form a compound of formula (VI); and converting the compound of formula(VI-a) into a compound of formula (VII) when W is a C1-8 alkoxy group, and converting the compound of formula (VI-b) into into the compound of the formula (VIII) when the W is a methylamino group.The method has the advantages of high yield, omitting of the production of an intermediate isothiocyanate with poor stability, mild reaction conditions, simplicity in operation, and cheap and easily available reagents, is suitable for small-scale preparation in the laboratory, and is also suitable for large-scale industrial production.
Preparation method of enzalutamide
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Paragraph 0058; 0060, (2017/02/28)
The invention provides a preparation method of enzalutamide. The method comprises the following steps: condensing an initial raw material 2-((3-fluoro-4-(methylcarbamoyl)phenyl)amino)-2-methylpropioric acid and enol to obtain an intermediate I, and reacting the intermediate I with The method has the advantages of simple operation, suitableness for industrial production, high yield and high purity.
PROCESSES FOR THE SYNTHESIS OF DIARYLTHIOHYDANTOIN AND DIARYLHYDANTOIN COMPOUNDS
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, (2011/09/30)
Processes are provided for the synthesis of diarylthiohydantoin and diarylhydantoin compounds, such as compounds of the formula: wherein X, Y1, Y2, R1, and R2 are as defined herein. Medicinal products containing the same find particular use in treating prostate cancer, including castration-resistant prostate cancer and/or hormone-sensitive prostate cancer.