571-92-6Relevant articles and documents
Synthesis method of 6-ketoestradiol
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Paragraph 0030-0031, (2020/01/25)
The invention belongs to the technical field of preparation of steroid hormone intermediate, and particularly relates to a synthesis method of 6-ketoestradiol. According to the synthesis method, a compound 1 is taken as a raw material to obtain the 6-ketoestradiol through the following reaction route (please see the specifications for the reaction route). Different from estrone, the raw materialsin the synthesis method are low in price, wide in source and low in cost. By optimizing the reaction route, when 6-site carbanyl groups are introduced, the 6 site is the only active site, selectivityof oxidation is greatly improved, and the reaction condition is also environmentally friendly. The brand-new synthesis route of the 6-ketoestradiol is provided, the technological condition is mild, environment friendliness is achieved, and the synthesis method is suitable for industrial production.
PROCESS FOR THE PREPARATION OF FULVESTRANT
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, (2015/11/16)
The present invention relates to an improved process for the preparation of Fulvestrant (I). Also, provided is novel intermediate of Fulvestrant and a process for the preparation of the same.
Synthesis, anti-oxidant activity, and cytotoxicity of salicyloyl derivatives of estra-1, 3, 5(10)-triene and androst-5-ene
Gasi, Katarina Penov,Djurendic, Evgenija,Dojcinovic-Vujaskovic, Sanja,Gakovic, Andrea,Jovanovic-Santa, Suzana,Kojic, Vesna,Sakac, Marija
, p. 284 - 294 (2012/08/28)
Since many estrane and androstane derivatives exhibit cytotoxic, anti-oxidant, or anti-hormone activity, new steroidal derivatives were synthesised from appropriate estrogen or androgen precursors in order to obtain potential therapeutics for the treatment of steroid-dependent diseases. Starting from estradiol (I ), 6-oxo derivatives V and VII were prepared. 17β-Salicyloyl-6-oxo derivatives VI and VIII were synthesised by the reaction of compounds V or VII with methyl salicylate in the presence of sodium. 17β-Salicyloyloxy estradiol IX was prepared from estradiol. Beckmann fragmentation of 16-oxyimino alcohols XII and XIII with methyl salicylate yielded corresponding Dseco derivatives XIV and XV. Simultaneous fragmentation and acylation of compound XII resulted in 3β-salicyloyl-D-seco derivative XVI which was also obtained from compound XIV. Anti-oxidant assays of the newly synthesised compounds V-IX, XIV, and XVI indicated a stronger capacity for hydroxyl radical scavenging, and a weaker capacity for DPPH radical scavenging, compared with the standard anti-oxidants BHA and BHT. Compounds V, XIV, and XVI showed higher or the same activity as BHT. The cytotoxicity of new compounds was evaluated against human breast and prostate carcinoma cells. Compound VI exhibited strong cytotoxicity against MDA-MB-231 cells; compound XIV exhibited strong cytotoxicity against PC-3 cell line, while compound VII moderately inhibited the growth of PC-3 cells.
