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US 5,393,886 AGranted
Intermediates for the synthesis of anthrapyrazolone anticancer agents
AssigneeThe Du Pont Merck Pharmaceutical Company
InventorsLin-Hua Zhang, Joseph Auerbach
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Abstract
This invention relates to compounds, including 5-chloro-2-[2-[[(4-methylphenyl)sulfonyl]oxy]ethyl]-7-[2,4,6-trimethylphen yl)methoxy]anthra[1,9-cd]pyrazol-6(2H)-one and analogs thereof, which are useful as intermediates for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone. This invention also relates to methods for the synthesis of anthrapyrazolone anticancer agents, including losoxantrone.
Claims8
A compound of formula (I):
- ##STR21## or a pharmaceutically acceptable salt form thereof, wherein:
- R.sup.1 is H or a hydroxyl protecting group;
- X is selected from:
- (a) F, Cl, Br, I,
- (b) methanesulfonyloxy,
- (c) toluenesulfonyloxy,
- (d) trifluoromethanesulfonyloxy, or
- (e) --OH;
- Y is selected from:
- (a) Cl, Br, I,
- (b) --OSO.sub.2 R.sup.2, or
- (c) --OH;
- R.sup.2 is selected from:
- (a) C.sub.1 -C.sub.4 alkyl,
- (b) C.sub.v F.sub.2v+1 where v is 1 to 4, or
- (c) phenyl or phenyl optionally substituted with from 1 to 3 of the groups selected from Cl, F, Br, NO.sub.2, --OR.sup.6, or C.sub.1 -C.sub.4 alkyl;
- R.sup.6 is selected from:
- H, C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.4 -C.sub.8 cycloalkylmethyl, C.sub.6 -C.sub.10 aryl, or C.sub.7 -C.sub.11 arylalkyl;
- with the proviso that when:
- X is Cl then Y can not be --OH.
17 more elements
Dependencies are inferred from the claim text.