Document Type and Number:
Japanese Patent JPS5058054
Kind Code:
A
Abstract:
1450884 D-homosteroids F HOFFMANNLA ROCHE & CO AG 25 Sept 1974 [26 Sept 1973] 41706/74 Heading C2U The invention comprises compounds of formula wherein the 1,2-bond is single, R10 being H or Me, or double, R10 being Me; the 6,7-bond is single, R7 being H, mercapto, acylthio, alkylthio, cycloalkylthio or aralkylthio, or double, R7 being H; and the 16,17-bond is single or double. Compounds I (R7 =H) are prepared (a) from the corresponding #5 (or #5,16 )-3#-ols by oxidation to give a #4 , #4,6 or #1,4,6 -3-oxo grouping, e.g. with CrO 3 , DCC/DMS, SO 3 /py, Br 2 /LiBr/Li 2 CO 3 /DMF or with Al(OPri ) 3 or Al(OBut ) 3 optionally in the presence of DDQ; or (b) from the corresponding #5(10) or #5(10) ,16 -3- ones by acid or base #5(10) ##4 isomerization; and are interconvertible by chemical or microbial 1,2- and/or 6,7-dehydrogenation. Compounds I (R7 is other than H) are prepared from the corresponding 6,7-dehydro compounds (where R7 =H) by reacting with H 2 S, a mercaptan or a thiocarboxylic acid, optionally followed by 1,2-dehydrogenation. The starting materials are prepared as described in Specifications 1,450,885 and 1,450,886. Compounds I are said to affect body mineral reserves, and may be made up with carriers into pharmaceutical compositions for oral, parenteral rectal and topical administration.
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Application Number:
JP10892474A
Publication Date:
May 20, 1975
Filing Date:
September 24, 1974
Export Citation:
International Classes:
A61K31/56; A61K31/585; C07J63/00; (IPC1-7): A61K31/58; C07J63/00