| 摘要 |
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, R<SP>10</SP> being H or Me, or double, R<SP>10</SP> being Me; the 6,7-bond is single, R<SP>7</SP> being H, mercapto, acylthio, alkylthio, cycloalkylthio or aralkylthio, or double, R<SP>7</SP> being H; and the 16,17-bond is single or double. Compounds I (R<SP>7</SP>=H) are prepared (a) from the corresponding #<SP>5</SP> (or #<SP>5,16</SP>)-3#-ols by oxidation to give a #<SP>4</SP>, #<SP>4,6</SP> or #<SP>1,4,6</SP>-3-oxo grouping, e.g. with CrO 3 , DCC/DMS, SO 3 /py, Br 2 /LiBr/Li 2 CO 3 /DMF or with Al(OPr<SP>i</SP>) 3 or Al(OBu<SP>t</SP>) 3 optionally in the presence of DDQ; or (b) from the corresponding #<SP>5(10)</SP> or #<SP>5(10)</SP>,<SP>16</SP>-3- ones by acid or base #<SP>5(10)</SP>##<SP>4</SP> isomerization; and are interconvertible by chemical or microbial 1,2- and/or 6,7-dehydrogenation. Compounds I (R<SP>7</SP> is other than H) are prepared from the corresponding 6,7-dehydro compounds (where R<SP>7</SP>=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. |
