| 摘要 |
17 beta -Thiocarboxylic acid esters of 4-halo-3-oxoandrost-4-enes of the formula:
<CHEM>
wherein
X<1> is fluoro, chloro or bromo;
X<2> is fluoro, chloro or hydrogen;
X<3> is fluoro, chloro, bromo or hydrogen;
X<4> is =C=O or
<CHEM>
or may also be
<CHEM>
when X<3> is chloro;
R is alkyl or 1 to 6 carbon atoms or phenyl or benzyl optionally substituted with one substituent on the phenyl ring chosen from the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms and halo;
R<1> is hydrogen or alkanoyl of 2 to 6 carbon atoms when R<2> is hydrogen, alpha -methyl or beta -methyl, or OR<1> and R<2> together are isopropylidenedioxy; and
the solid and broken lines between C-1 and C-2 represent a double or a single bond;
are useful as anti-inflammatory agents. They can be prepared by treating the corresponding 17 beta -carboxylic acid with a suitable base salt of RSH. The 17 beta -hydroxy compounds can be esterified to produce the 17 beta -alkanoyloxy compound. The double bond at the 4,5 position can be produced by contacting the corresponding DELTA <5> compound with a base. |
