Androgen Anabolic Steroids

Group blon - purpose

Most anabolic hormones have their effects through the action of testosterone, such as Anabolism, and virilization. Examples of assimilative effects: promote protein biosynthesis from amino acids, increase muscle size and strength, increase appetite, promote bone iliac growth, stimulate bone marrow, promote red blood cell production. Prosynthesis was more potent in increasing muscle girth than testosterone or booster.

Cyprone is a synthetic triene 19- desteroidal compound with complex properties. Its antiestrogen and antiprogesterone activity can be very strong or very weak. Acts on the hypothalamus. The pituitary axis reduces gonadotropin release and the preovulation peak disappears, thereby inhibiting ovulation. Animal experiments show that it can inhibit the secretion of progesterone, but also has the effect of progesterone on endometrium, so that the endometrium and the cells of ectopic lesions deactivate and degenerate, resulting in the atrophy of ectopic lesions. Its antifertility effect may be inhibiting ovulation and endometrial development, changing the nature of cervical mucus, affecting the ovum operation speed and antagonizing the endometrial progesterone receptor, thus interfering with the implantation of pregnant eggs. It is clinically used to treat endometriosis by atrophy and absorption. As it has a strong role in promoting protein synthesis, with the large-scale and intensive development of animal husbandry, a small number of production enterprises and breeders, operators in order to seek maximum profits, regardless of national laws and regulations, abuse or illegal use of hormones and other illegal drugs. As an assimilative hormone additive, it often leads to excessive residue in animal food. When people eat excessive residue of animal food, it will accumulate in the human body, produce a variety of adverse consequences, directly endanger human health and life

. Method 1: A high yield synthesis method of acetic acid demethylandrotrienolone:

1) etherification reaction: put 80kg alcohol into 500L reaction tank to cool down to 0℃, open stirring, drop 10kg acetyl chloride, control temperature 0 ~ 10℃. After dropping, 10kg of estrogens 4,9 diene 3,17 -- dione was added and stirred at 10 ~ 13℃ for 2 hours. After heat preservation, the material liquid is pumped into sodium carbonate aqueous solution, and the temperature is controlled at 20-25 ℃. After dropping, the temperature is controlled at 20-25 ℃ and stirred for 30 minutes, the material is pumped and filtered, and a large amount of water is washed until neutral and centrifuged, and the wet material is obtained.

2) Reduction hydrolytic dehydrogenation reaction: 100kg methanol was pumped into the 500L reaction tank, and the wet material was put into the previous step, and the temperature was cooled to 0℃. 5kg potassium borohydride was added, and the temperature was controlled at 0 ~ 5℃. After finishing, the mixture was kept for 1.5 hours. After the point plate is qualified, add glacial acetic acid to adjust the PH value to neutral, decompress and concentrate to oil-like substance. After concentration, dissolve the oil-like substance with 200kg methylene chloride, wash the oil-like substance with 150kg tap water for about three times after full dissolution, and then concentrate to oil-like substance after washing. After concentration, the oily substance was added with 70kg methanol, dissolved and completely dissolved, then the temperature was lowered to below 10℃, 5kg of reagent hydrochloric acid was added, PH1 ~ 2 was adjusted, and the temperature was kept at 10 ~ 15℃ for 2 hours, and the plate was pointed. After the plate is qualified, add NaOH water to adjust the PH value to neutral, and then concentrate to dry. Add 200kg methylene chloride to dissolve. After complete dissolution, add 150kg water to wash three times each time. After washing, add 10kg anhydrous magnesium sulfate for dehydration. After dehydration, anhydrous magnesium sulfate was pumped out and the filter cake was rinsed with appropriate amount of dichloromethane. After filtration and rinsing, 9kg DDQ was added at 0 ~ 5℃ for 3 hours during filtration night. Point plate, point plate qualified, filter, wash DDQ rinse with appropriate amount of dichloromethane, dichloromethane layer add 200kg30% sodium carbonate water. After layering, the organic layer was repeated for two times, and the organic layer was washed three times with 1000kg tap water. After washing, decompression concentration to thick paste, cooling to 0 ~ 5℃ centrifuge, drying at 90100℃, methandrotrienolone can be removed.

3) acylation reaction: in the glass lining reaction pot of 300L, open the vacuum valve, extract the benzene 100㎏, pyridine 10㎏. Then open the feeding port and put 10kg demethylandrotrienolone (demethylandrotrienolone), 0.5kg4DMAP, drop 10kg acetyl chloride, the temperature is controlled at 0 ~ 10℃, the drop is controlled within 1 hour, keep warm for 0.5 hours. After the point plate is qualified, add acid and water to stir for 30 minutes, layer the plate, add 100kg water for three times each time, after washing, decompress and concentrate to dry. 10kg ethyl acetate was added to dissolve, and 25kg petroleum ether was added to cool down to 0 ~ 5℃ for centrifugation.

Method 2: a synthesis method of demethylandrotrienolone acetate (demethylandrotrienolone), characterized in that it includes the following steps.

Step 1) reduction reaction: 4,9 ring openers (I) were dissolved in methanol, potassium and borohydride were added in stages at 20 ~ 25℃, followed by heat preservation reaction until TLC was used to analyze the reaction of raw materials, and compound (II) was obtained.

Step 2) Hydrolysis reaction: The reaction system to complete the step 1) add dilute acid to adjust pH value to neutral, 20 ~ 25 ℃ temperature control, add dilute sulphuric acid into the reaction system, drops, mixing reaction and TLC analysis raw material completely, the reaction solution with sodium carbonate solution to water, stir until completely solid precipitation, control temperature in 50 ℃ under reduced pressure to concentrate without the distillate, 17β -hydroxy-estrogen-5 (10), 9(11) -diene-3-one (III) were obtained by stirring with water, centrifuging and drying.

Step 3) Dehydrogenation reaction: Compound (III) was dissolved in dichloromethane, DDQ(dichlorodicyanobenzoquinone) was added, the temperature was controlled at 20-25 ℃, and the reaction was stirred until TLC was used to analyze the raw material and the reaction was complete. The filtrate was washed with alkaline reductant solution and alkali solution, combined with water layer, and extracted with dichloromethane. After combining all dichloromethane layers, dehydration, decompression and concentration to no distillate, adding ethyl acetate to entrap distillate residual dichloromethane, distilling all dichloromethane, adding ethyl acetate, cooling crystallization, centrifugation. After drying, the methyandrotrienolone (IV) is obtained.

Step 4) Esterification reaction: methylotrienolone (V) was dissolved in dichloromethane, DMAP(4-dimethylaminopyridine) and acetic anhydride were added, and the reaction was stirred at 20 ~ 25℃ until the reaction of TLC analysis raw materials was complete. Sodium carbonate solution was added and washed to pH8 ~ 9, and the water layer was combined with dichloromethane to extract the water layer. Combined with all dichloromethane layer, anhydrous sodium sulfate dehydration, filtration, decompression concentration to distillate, adding isopropyl ether entrainer distillate residual dichloromethane, distillate all dichloromethane and then adding isopropyl ether, cooling crystallization, centrifugation, drying, acetic acid demethylandrotrienolone (demethylandrotrienolone);