Richter Gedeon Vegyeszeti Gyar Rt

Richter Gedeon Nyrt.

Endréné Magyari

Zoltán Tuba

Sándor Mahó

János Csörgei

László Terdy

Lajosné Dancsi

György Visky

Csaba Molnár

János Kiss

Sándor Maho

A new industrial process for the synthesis of solvate-free 17&#x3b1;-acetoxy-11&#x3b2;-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione [CDB-2914] of formula (I) which is a strong antiprogestogene and antiglucocorticoid agent. The invention also relates to compounds of formula (VII) and (VIII) used as intermediates in the process.

Industrial process for the synthesis of 17&#x3b1;-acetoxy-11&#x3b2;-[4-(N,N-dimethyl-amino)-phenyl]-19-norpregna-4,9-diene-3,20-dione and new intermediates of the process

The invention relates to a process for the synthesis of d-(17&#x3b1;)-13-ethyl-17-hydroxy-18,19-dinorpregn-4-ene-20-yn-3-one-oxime (also known as norelgestromin) via acetylation of d-norgestrel at position 17; oximation of the oxo group at position 3 of the obtained d-(17&#x3b1;)-13-ethyl-17-(acetyloxy)-18,19-dinorpregn-4-ene-20-yn-3-one; and then hydrolyzing the acetyloxy group at position 17 of the obtained d-(17&#x3b1;)-13-ethyl-17-(acetyloxy)-18,19-dinorpregn-4-ene-20-yn-3-oxime derivative, thereby obtaining norelgestromin.

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Albertirsa, Hungary

Endréné Magyari