Synthesis of anti-estrogenic and other therapeutic steroids from 21-hydroxy-19-norpregna-4-en-3-one

   
   

Syntheses of steroids such as 3-hydroxy-7.alpha.-methyl-21-[2'-methoxy-4'-(diethylaminomethyl)-phenoxy]- 19-norpregna-1,3,5(10)triene citrate ("SR 16234") and analogs thereof are provided, wherein 21-hydroxy-19-norpregna-4-en-3-one serves as a starting material or intermediate. The latter compound may be readily prepared from estrone-3-methyl ether. Certain intermediates in these syntheses also have value as therapeutic agents, for example in the treatment of prostate disorders such as prostatic cancer.

Sintesi degli steroidi quale 3-hydroxy-7.alpha.-methyl-21-[2'-methoxy-4'-(diethylaminomethyl)-phenoxy ] - 19-norpregna-1,3,5(10)triene il citrato ("SR 16234") e gli analoghi di ciò sono forniti, in cui 21-hydroxy-19-norpregna-4-en-3-one serve da prodotto base o intermediario. Il residuo posteriore può essere preparato prontamente dall'etere di estrone-3-methyl. Gli intermediari sicuri in queste sintesi inoltre hanno valore come agenti terapeutici, per esempio nel trattamento dei disordini della prostata quale cancro prostatic.

 
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