Progesterone production method

Abstract

The invention discloses a progesterone production method, which comprises the following steps: carrying out acid catalysis reaction on 4-androstenedione and triethoxymethane in a low-carbon alcohol organic solvent to obtain 3-ethoxy-androstane-3, 5-diene-17-ketone; under the condition of strong alkali, enabling 3-ethoxy-androstane-3, 5-diene-17-ketone and p-methylbenzenesulfonyl methyl isocyanide to react in an organic solvent to obtain 3-ethoxy-17beta-cyanoandrostane-3, 5-diene; reacting 3-ethoxy-17beta-cyanoandrostane-3, 5-diene with a Grignard reagent to obtain an intermediate product; and hydrolyzing the intermediate product to obtain progesterone. According to the invention, progesterone can be prepared by taking 4-androstenedione as a raw material through four-step reaction, wherein the raw material is low in price and easy to obtain, the process is simple and environment-friendly, the synthesis route is short, the reaction conditions are easy to control, the production cost is effectively reduced, the yield of the progesterone prepared by the method can reach 94-98%, and compared with the existing preparation process, the progesterone prepared by the method is higher in yield and good in product quality, and the method is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of preparation technology of steroid hormone drugs, in particular to a production method of progesterone. Background technique [0002] Progesterone, also known as progesterone hormone and luteinizing hormone, is an endogenous progesterone in the human body and plays an important role in the process of human fertility. Clinically, it is mainly used for habitual abortion, dysmenorrhea, menorrhagia or blood collapse, amenorrhea, etc. Oral large doses are also used for diseases caused by insufficient progesterone, such as premenstrual syndrome, menstrual disorders caused by cessation of ovulation, and benign breast disease. Vaginal administration can be used instead of oral administration, especially for patients with liver disease. Progesterone can also be used for benign prostatic hyperplasia and sleep apnea syndrome. [0003] The traditional synthesis method of progesterone is to extract diosgenin from ya...

AI Technical Summary

Problems solved by technology

[0003] The traditional synthesis method of progesterone is to extract diosgenin from yam plant, diosgenin is protected, oxidatively cracked, and eliminated, and the intermediate acetic acid gestational dienolone is obtained as a raw material, and the raw material is subjected to catalytic hydrogenation, hydrolysis, and austenitic oxidation The three-step reaction produces progesterone; among them, processes such as extraction of diosgenin, oxidative cracking, and epoxidation of dienes produce more waste water, are not easy to handle, and cause great environmental pollution; the Oxide oxidation process for progesterone production, Using steam distillation, water consumption and energy consumption are large; using active nickel or palladium carbon catalytic hydrogenation, there are potential safety hazards

In addition, with the depletion of wild yam plant resources, and the artificial planting of yam plants, the production costs of saponin and dienes have doubled due to the increasing cost of labor and chemical fertilizers, resulting in the production cost of progesterone and the market price. Substantial growth

Another production method of progesterone is to obtain saponin from turmeric extract as raw material through multi-step reactions, but the current price of saponin is more than 800,000 yuan / ton, and various steroids are synthesized from saponin Compounds, the general steps are longer, the yield is about 80%, and the cost is higher

And the yield is low, not suitable for industrialized production

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