Merck Sharp + Dohme B.v.

Msd Oss B.v.

N.v. Organon

Martin Ostendorf

Henricus Johannes Franciscus Maas

Lambertus Gerardus Maria Willems

Johannes Stoelwinder

Lambertus Gm Willems

Henricus Jf Maas

Van Patrick Buggenum

The present invention relates to a synthesis route and to steroid derivatives of general formula VI and VII useful in the synthesis of desogestrel and etonogestrel. 

Combined synthesis route for desogestrel and etonogestrel

Process for the preparation of a compound of general formula (II) wherein Rand Rindependently are hydrogen or a hydroxy- or hydrocarbyl group; or wherein Rand Rtogether are a double bonded oxygen; Ris hydrogen; R'is a nitrobenzophenone group; and Rand Rindependently are hydrogen or a hydroxy- or hydrocarbyl group; from a compound of general formula (I) wherein, R, RR, Rand Rare as defined above and Ris hydrogen; wherein the compound of formula (I) is reacted under alkaline conditions with 2-chloro-5-nitrobenzophenone in the presence of an alkanolic solvent and the compound of formula (II) is directly crystallized from this alkanolic solvent. Complex of an alkanol and a compound of general formula (II) obtainable from the above process and processes wherein the above process or complex are used. 

Process for the preparation of estrone and/or estradiol-derivatives

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Oss, Netherlands

Martin Ostendorf