Pharmaceutical intermediates Raw material powder Exemestane

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Exemestane Powder Usage and Synthesis.

Exemestane is a steroid aromatase inactivator, whose structure is similar to the natural substrate of aromatase, androstenedione, and is the pseudo-substrate of aromatase. Since estrogen in postmenopausal women is mainly produced by the conversion of androgens (produced by the adrenal cortex) in the peripheral tissues under the action of aromatase, this product inactivates it by irreversibly binding to the active site of the aromatase, thus significantly reducing the level of estrogen in the blood circulation of postmenopausal women.

This product has no significant effect on the biosynthesis of adrenal corticosteroids, even if the concentration is 600 times higher than that of inhibiting aromatase, it has no significant effect on other enzymes in the corticosteroid production pathway. The oral absorption of this product is rapid, the absorption is affected by food, and the oral bioavailability is 42%. The absorption rate of postmenopausal women was higher than that of healthy subjects. The peak blood concentration was reached 2 ~ 4 hours after oral administration of this product, and the average peak time was 1.2 hours, which was shorter than that of healthy subjects (2.9 hours). It mainly binds to α1-acid glycoprotein and protein, and the total protein binding rate is 90%. The metabolite is inactive 17-hydrogen exemestane with a clearance half-life of 24 hours. It is mainly excreted in urine or feces, each accounting for 42% of the dose.

Uses of Exemestane.

The pharmaceutical raw material is an irreversible steroid aromatase inactivator, which can inhibit estrogen synthesis and reduce the level of estrogen in blood circulation. It is suitable for postmenopausal advanced breast cancer patients who progress after tamoxifen treatment. Second generation aromatase inhibitors are used for the treatment of metastatic breast cancer and as adjuvant therapy for early breast cancer.

In vitro study of Exemestane.

Product Method of Bulk Exemestane Powder.

Androstene-4-ene-3, 17-dione and triethyl orthoformate were dissolved in tetrahydrofuran and anhydrous ethanol, reacted in the presence of p-toluenesulfonic acid, and then added to n-methylaniline and formaldehyde solutions to continue the reaction. The Mannich reaction product was dissolved in benzoic acid and anhydrous dichethanes, and exemestane was obtained under the action of DDQ with a total yield of 45%.

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