57144-06-6Relevant articles and documents
Synthesis method of alkyl acid testosterone
-
Paragraph 0033-0034; 0049-0050, (2020/12/10)
The invention discloses a synthesis method of alkyl acid testosterone, and belongs to the technical field of synthesis and processing of medicines. The method comprises the following steps of: taking4-androstenedione (4AD) as an initial raw material, firstly, carrying out enol ether protection on the keto group at the site 3, and reducing carbonyl at the site 17 into hydroxyl; or taking 4-androstenedione (4AD) as an initial raw material, firstly carrying out enol ether protection on the keto group at the site 3, then reducing carbonyl at the site 17 into hydroxyl, then carrying out hydrolysison the site 3 to obtain testosterone, and carrying out esterification and third-site hydrolysis to obtain the testosterone ester after testosterone third-site ketal protection. According to the method disclosed by the invention, the third site is protected during esterification reaction, the generation of impurities can be reduced, and an esterification reaction solvent is a water-insoluble organic solvent, so that after the reaction is completed, products can be directly extracted in a layered manner, a large amount of water does not need to be added to separate out the products, the amountof wastewater is reduced, the solvent can be recycled, and the process is more suitable for industrial production.
The invention relates to a raw material synthetic stone androstenedione cholic acid (by machine translation)
-
Paragraph 0017; 0018, (2019/01/08)
The invention discloses a high-purity stone of cholic acid synthesis method, comprises the following steps: to androstenedione as the starting material, through the 3 bit enol ether protection, wittig reaction, 3 bit vinyl alcohol the ether escapes protection, 17 site side chain addition, 3 bit carbonyl reduction, saponification reaction, seven-step reaction of catalytic hydrogenation to obtain high-purity of target substance. The method of the invention uses cheap and easily obtained androstenedione as raw materials, innovative synthetic lithocholic, simple process route, each step the reaction yield is high, and the cost is low, the large-scale production of stone cholic acid difficult problem, is suitable for industrial production. (by machine translation)
Preparation method of melengestrol intermediate
-
Paragraph 0045; 0059; 0073; 0087; 0101; 0115, (2017/09/01)
The invention discloses a preparation method of a melengestrol intermediate. According to the preparation method, a product compound VII, namely a melengestrol intermediate is prepared through etherification, methylenenation, cyano substitution, silicon alkoxy protection, internal nucleophilic substitution and reduction reaction of a compound 4-androstene-3,17 diketone. The used raw material 4-androstene-3,17 diketone is cheap and available. The whole process route is reasonable and optimal in design, and the synthesized product is few in impurities, good in quality, high in yield, simple in operation, mild in reaction condition, low in cost, safer and suitable for industrialization.