119169-78-7Relevant articles and documents
Improved Syntheses of Epristeride, a Potent Human 5α-Reductase Inhibitor
Baine, Neil H.,Owings, Franklin F.,Kline, Donald N.,Resnick, Theodore,Ping, Li-Jen,et al.
, p. 5987 - 5989 (1994)
Two improved syntheses of a potent human 5α-reductase inhibitor, epristeride, SK&F 105657, are described.The first synthesis starts from methyl 3-oxoandrost-4-ene-17β-carboxylate (1), which is converted to epristeride (5) in four synthetic steps in 44percent overall yield.The second synthesis starts from commercially available 3-oxoandrost-4-en-17β-carboxylic acid (7), which is converted to epristeride (5) in two synthetic steps in 63percent overall yield.Both syntheses are suitable for large scale production and have been employed to produce kilograms supplies of epristeride in high purity.
Palladium and nickel catalyzed hydroxycarbonylation of a steroidal bromodiene in the synthesis of episteride, a potent 5α-reductase inhibitor
McGuire, Michael A.,Sorenson, Edmund,Klein, Donald N.,Baine, Neil H.
, p. 1611 - 1615 (1998)
Androst-4-en-3-one-17β-carboxylic acid 1 was converted to 3-bromo-N- (l,1-dimethylethyl) androsta-3,5-diene-17-β-carboxamide 2 by reaction with DMF/oxalyl bromide and quenching into t-butylamine. 2 was converted to 3 (R=H) by nickel cyanide catalyzed hydr
Epristeride intermediate, preparation method of Epristeride intermediate, and preparation method of Epristeride
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, (2018/03/24)
The invention relates to the field of medicine, in particular to an Epristeride intermediate, a preparation method of the Epristeride intermediate, and a preparation method of Epristeride. The preparation method of the Epristeride intermediate comprises the following steps that a compound 3 takes a sulfonation reaction with an alkaline reagent to produce a compound 4; the reaction conversion is single; the column chromatography isolation is avoided; the alkaline reagent used in the reaction process can be easily obtained; the reaction conditions are mild. The unit operation is reduced; the production period is shortened; the production efficiency is improved; the production efficiency is high; the economic benefits are improved.
Method of treatment for prostatic cancer
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, (2008/06/13)
Disclosed is a new treatment for men with prostatic cancer involving combination therapy of a 5α-reductase inhibitor, i.e., a 17β-substituted 4-azasteroid, a 17β-substituted non-azasteroid, 17β-acyl-3-carboxyandrost-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylamino-phenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an antiandrogen, i.e. flutamide. Pharmaceutical compositions useful for treatment are also disclosed.
