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A production method, exemestane technology, applied in the field of organic synthesis, can solve the problems of unsuitability for industrial production, unstable quality, low yield, etc., and achieve the effect of cheap raw material sources, easy control of process operation, and high yield
Active Publication Date: 2016-12-21
NANJING CHENGONG PHARM CO LTD
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Problems solved by technology
However, the current production method is difficult to control the process operation, the yield is low, the quality is unstable, and it is not suitable for industrial production.
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Embodiment 1
[0011] 1. Preparation of intermediate YXMT01:
[0012] Add 4Kg of 1,4-androsdienedione, 4L of triethyl orthoformate, 104g of p-toluenesulfonic acid, 26L of tetrahydrofuran, and 4L of absolute ethanol, raise the temperature to 40--45°C and stir for 12 hours to detect that the remaining raw materials do not exceed 5.0 % stop, then filter, add 15L ethanol for recrystallization, obtain 3.45Kg white solid intermediate YXMT01, purity 98.5%, yield range 78.3%, intermediate YXMT01 structural formula is as follows:
[0013]
[0014] 2. Preparation of intermediate YXMT02:
[0015] Add 3.45KgYXMT01, 10L tetrahydrofuran, 10L ethanol, 1.76Kg N-methylaniline and 0.87Kg37% formaldehyde and stir for 10 hours under the condition of at least 40--45°C, check that the remaining raw materials do not exceed 3.0%, stop, distill off the solvent, and drop directly One-step reaction, without refining, obtain 3.25Kg intermediate YXMT02, purity 98.9%, yield range 73.5%, intermediate YXMT02 structural...
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Abstract
An industrial production method of exemestane comprises the following steps: adding androsta-1,4-diene-3,17-dione, anhydrous ethanol, triethyl orthoformate and p-toluenesulfonic acid into a reactor, stirring above added materials, carrying out rotary drying, and crystallizing the obtained dried mixture to obtain an intermediate YXMT01; sequentially adding the intermediate YXMT01, anhydrous ethanol, tetrahydrofuran, 37% formaldehyde, N-toluidine and p-toluenesulfonic acid into the reactor, and carrying out rotary drying to obtain an intermediate YXMT02; sequentially adding the intermediate YXMT02, ethyl acetate and hydrochloric acid into the reactor, precipitating, carrying out suction filtration to obtain white solid, and re-crystallizing the white solid with toluene to obtain an intermediate YXMT03; and sequentially adding the intermediate YXMT03, toluene and IBX into the reactor, stirring the added substances, cooling the obtained substance, concentrating the obtained filtrate, and re-crystallizing the obtained concentrate to obtain white solid YXMT. The method has the advantages of avoiding of uncontrollability of a one-kettle method in industrial production, cheap sources of raw materials, easiness in control of the process operation, high yield, stable quality, and suitableness for industrial production.
Description
technical field [0001] The invention relates to the technical field of organic synthesis, in particular to an industrial production method of exemestane. Background technique [0002] Exemestane, referred to as YXMT, Chinese name: 1,4-diene-3,17-dione-6-methyleneandrostane, exemestane is an irreversible steroidal aromatase inactivator, Structurally similar to the enzyme's natural substrate androstenedione, it is a pseudo-substrate for aromatase that can be inactivated by irreversibly binding to the active site of the enzyme (this effect is also known as "self-destructive inhibition") "), thereby significantly reducing the level of estrogen in the blood circulation of postmenopausal women, but has no significant effect on the biosynthesis of corticosteroids and aldosteroids in the adrenal gland, and when it is higher than 600 times the concentration that inhibits the action of aromatase, the steroidogenic pathway No significant effect on other enzymes, it can block estrogen ...
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