Methods of obtaining 2-methoxyestradiol of high purity

C - Chemistry – Metallurgy – 07 – J

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C07J 1/00 (2006.01) A61K 31/565 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2376297

2-methoxyestradiol having greater than 98% purity is obtained by synthetic or purification methods. This highly pure 2-methoxy estradiol, lacking estrogenic components, is particularly suitable for clinical use in humans. The purification methods of the invention involve the use of liquid-solid chromatography (LSC) to separate 2-ME2 from other compounds. The chromatographic media is preferably silica. The solvent system comprises a non- polar solvent, such as chloroform, and a polar solvent, such as methanol.

L'invention concerne du 2-méthoxyestradiol d'une pureté supérieure à 98 %, obtenu par des procédés de synthèse ou de purification. Ce 2-méthoxyestradiol très pur, exempt de constituants oestrogéniques, convient particulièrement à une utilisation clinique chez l'homme. Les procédés de purification de l'invention utilisent la chromatographie liquide-solide afin de séparer 2-ME2 des autres composés. Le milieu chromatographique est, de préférence, la silice. Le système solvant comprend un solvant non polaire, tel que le chloroforme, et un solvant polaire, tel que le méthanol.

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