15262-77-8Relevant articles and documents
Method for preparing delmadinone acetate product
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Paragraph 0051; 0059-0060; 0063; 0071; 0072; 0075; 0083-0084, (2019/03/06)
The invention provides a method for preparing a delmadinone acetate product. The method comprises the following steps: by taking IDD (1,4-Androstadienedione) as a raw material, firstly, enabling 17-site ketone in IDD molecules to react with acetone cyanohydrins in a first organic solvent under catalysis of an alkali, and introducing beta-hydroxyl and alpha-cyan into the 17-site so as to obtain hydroxyl cyanogens; preparing 1,6-bidehydrogenation-17a-hydroxyl progesterone from the hydroxyl cyanogens in the presence of methyl magnesium halide, a second organic solvent and an acid; further synthesizing a 6-site epoxy substance, further synthesizing 6-site chloride so as to obtain delmadinone, and finally carrying out 17-site esterification so as to obtain delmadinone acetate; and further carrying out heating backflow decoloring and recrystalization on the obtained delmadinone acetate with activated carbon in lower-carbon alcohol with the carbon number of smaller than 4, thereby obtaining the delmadinone acetate product. Compared with a conventional synthesis method, the method provided by the invention has multiple advantages of being simple and convenient in process operation, economic and environmental-friendly in production, high in total synthesis yield, high in product quality, low in production cost, and the like.
Combined antiestrogens and antigonadotropically effective antiandrogens for the prophylaxis and therapy of hyperplasia of the prostate
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, (2008/06/13)
A pharmaceutical composition comprising an anti-estrogen and an antigonadotropically effective anti-androgen, e.g., in a weight ratio of anti-estrogen to anti-androgen of essentially 2:1 to 1:10 is effective for the prophylaxis and therapy of prostate hyperplasia. Suitable anti-estrogens include, for example, tamoxifen. Antigonadotropically active anti-androgens preferably are steroids having anti-androgenic and progestational properties, e.g., cyproterone acetate.