The Hetero Ring Is A Cyclic Anhydride (i.e., Containing -c(=x)-o-c(=y)- As Part Of The Ring, Wherein X And Y Are Chalcogen; E.g., 5,8-maleic Anhydride Adduct Of 5,7,9(11)-pregnatrien-3,20-di-one, Etc.) Patents (Class 540/60)
Abstract: The invention describes 14,17-C.sub.2 -bridged steroids of general formula (I), ##STR1## wherein the various R groups are as defined in the specification, and wherein said steroids are in contrast, with the disclaimed compound, the new compounds are available even after peroral administration with high gestagenic action and are suitable for the production of pharmaceutical agents.
Type:
Grant
Filed:
August 18, 1998
Date of Patent:
October 26, 1999
Assignee:
Schering Akitengesellschaft
Inventors:
Klaus Schollkopf, Wolfgang Halfbrodt, Joachim Kuhnke, Wolfgang Schwede, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
Abstract: A process for the production of a compound of formula (II), which comprises reacting an epoxy compound of formula (I) with an alcohol, wherein the reaction is carried out under a basic condition. ##STR1## R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as defined in the specification. The compounds are useful intermediates for the production of vitamin D.sub.3 derivatives.
Abstract: A process for the production of medrogestone, in which, in an intermediate step, the solvate 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17.alpha.-methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17.alpha.-methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6.beta.-hydroxy-6.alpha.,17.alpha.-dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.