Process for the preparation of 4-amino-.DELTA..sup.4 -3-ketosteroids via 4-nitro-.DELTA..sup.4 -3-ketosteroids
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United States of America Patent
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Oct 12, 1999
Issued Date -
N/A
app pub date -
Jan 22, 1998
filing date -
May 2, 1994
priority date (Note) -
Expired
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Abstract
The invention discloses 3-ketosteroids of the following formula used to inhibit steroid C.sub.17-20 lyase: ##STR1## wherein R is OH, C.sub.1 -C.sub.6 alkanoyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.4 alkanol, COCH.sub.2 OH, CO.sub.2 H, CONR.sub.7 R.sub.8, cyclopropyloxy, cyclopropylamino, acetylthioalkane, 2,2-dimethyldioxolan4-yl, 1,2-dihydroxyethyl and C.sub.1-4 alkylthiol; R.sub.1 is hydrogen, hydroxy or C.sub.1-6 alkyl; R and R.sub.1 together may indicate .dbd.O, that is an oxygen double bonded to the 17 carbon; R.sub.2, R.sub.3, and R.sub.4 are each independently hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.5 and R.sub.6 are each independently hydrogen or OH; R.sub.5 and R.sub.6 together may indicate .dbd.O, that is an oxygen double bonded to the 11 carbon; R.sub.7 is hydrogen or C.sub.1 -C.sub.8 alkyl; R.sub.8 is C.sub.1 -C.sub.8 alkyl; and with the proviso that, when R is OH, then R.sub.1 is hydrogen; and with the proviso that, when R.sub.5 is OH, then R.sub.6 is hydrogen.
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