Conessine derivatives,申请号GB19660032946-传众专利搜索

Conessine derivatives

申请公布号：GB1105237(A)

申请号：GB19660032946

申请日期：1966.07.22

申请公布日期：1968.03.06

申请人：

KONINKLIJKE NEDERLANDSCHE GIST SPIRITUSFABRIEK N.V.

分类号：C07J71/00;C12P33/00

主分类号：C07J71/00

摘要：The novel steroids 9a -hydroxyconessine and 12a -hydroxyconnesine are prepared by microbiological hydroxylation of conessine with enzymes of Botryodiplodia theobromae Pat. They may be converted to acid-addition salts and quaternary ammonium compounds, and they may be separated via the hemi-succinate of the 12a -ol which is formed at pH 9.5, unlike the 9a -ol which does not form such a salt. The 12a -ol may be oxidized to the 12-ketoconessine and acetylated to the 12a -acetoxy-conessine. The 9a -ol may be dehydrated to D 9(11)-conessine, which is also prepared by dehydration of 11a -hydroxy-conessine. The 9a -ol may be hydrogenated to 9a - hydroxy - 3b - dimethylaminoconanine which is also prepared by hydrogenating 11a - hydroxy - conessine to 11a - hydroxy - 3b -dimethylaminoconanine, dehydrating this to 3b - dimethylamino - D 9(11) - conenine, oxidizing this to 3b -dimethylamino-9a ,11a -epoxy-conanine 3-N-oxide and reducing this. Quaternary ammonium derivatives of the steroids of the invention, which are stated to be useful as muscular relaxing agents, may be made up into pharmaceutical compositions with suitable carriers. Suitable quaternizing agents are the esters of aliphatic and araliphatic alcohols with strong acids.