| 摘要 |
The present invention relates to a process for preparing 5,8-dihydronaphtoquinone derivatives represented by general formula (T) in which R1 represents alkyl or alkenyl, R2 represents hydrogen, alkyl or a group -C(O)R wherein R represents alkyl, alkenyl, aryl, aralkyl or aralkenyl, which can be substituted or unsubstituted with one or more halogen atom(s), and R3 represents hydrogen or alkyl,characterized in that (A) a compound having general formula (II) in which R1, R2 and R3 are defined as previously described and R4 represents alkyl, is oxidized with cerium(IV) ammonium nitrate in a suitable solvent, or (B) a compound having general formula (Ia) in which R1 and R2 are defined as previously described and R3a represents alkyl, is dealkylated to prepare a compound having general formula (Ib) in which R1 and R2 are defined as previously described, or (C) a compound having general formula (Ic) in which R1 and R3 are defined as previously described, is reacted with a compound of formula RCOOH wherein R is defined as previously described, in the presence of an organic base and dicyclohexylcarbodiimide to prepare a compound having general formula (Id) in which R1, R3 and R are defined as previously described. In addition, the present invention relates to a novel 5,8-dihydronaphtoquinone derivative of formula (I) wherein when R2a is hydrogen or a group -C(O)R and R3 is hydrogen, R1 is other than 3-methyl-2-butenyi; and when R2a and R3 independently of one another represent hydrogen or methyl, R1 is other than 3-methylbutyl, and its use as an anticancer agent.
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