Process for producing 3-hemisulphate-17.alpha.-hydroxy steroids

C - Chemistry – Metallurgy – 07 – J

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260/28

C07J 31/00 (2006.01)

Patent

CA 1047483

ABSTRACT OF THE DISCLOSURE A 3-hemisulphate sodium salt of a 17.alpha.-hydroxy steroid which is estrogenically effective, and having the general formula Image is produced by treating a 3-hydroxy-17-acyloxy steroid of the general formula Image with sulphur trioxide or a sulphur trioxide-containing agent in an organic nitrogen compound, preferably pyridine, and converting the resulting product into the corresponding sodium salt by treat- ment with an alkali, preferably sodium alcoholate or sodium hydrox- ide in a lower alcohol, with simultaneous saponification. In the above formulae R1 represents hydrogen, methyl or ethyl and R2 represents an acyl radical containing up to 15 carbon atoms, and the rings B and C can contain additional double bonds. For example, 17.alpha.-acetoxy-1,3,5(10)-estratrien-3-ol is treated with sulphur trioxide in the presence of pyridine, and the resulting product is treated with sodium methylate/methanol to produce 17.alpha.- estradiol-3-hemisulphate sodium.

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