26614-48-2Relevant articles and documents
Synthesis method of alkyl acid testosterone
-
Paragraph 0037; 0039; 0043; 0045; 0053; 0055; 0059; 0061, (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.
PROCESS FOR PREPARATION OF TESTOSTERONE
-
Page/Page column 6-7, (2017/06/21)
The present invention relates to a process for purification of 4-androsten-3,17-dione (II) and its conversion to testosterone (I) having purity > 99 % as measured by HPLC.
1,2-Dehydrogenation of steroidal 6-methylen derivatives. Synthesis of exemestane
Marcos-Escribano, Andrés,Bermejo, Francisco A.,Bonde-Larsen, Antonio Lorente,Retuerto, Jesús Iglesias,Sierra, Ignacio Herráiz
supporting information; experimental part, p. 7587 - 7590 (2009/12/04)
The development of an efficient dehydration method of steroidal 4-en-3-ones by using chloranil and BSTFA in the presence of triflic acid in refluxing toluene allowed us, starting from testosterone, to set a large-scale procedure for the synthesis of the anti-cancer drug exemestane in 70% overall yield.