| 摘要 |
Optically active hexahydrobenzo¢a!phenanthridines of formula (I) wherein R is hydrogen or C1-C4 alkyl; R1 is hydrogen or a phenol protecting group, X is fluoro, chloro, bromo, iodo or a group of the formula OR5, and R2, R3, and R4 are independently selected from the group consisting of hydrogen, C1-C4alkyl, phenyl, fluoro, chloro, bromo, iodo, or a group -OR1 are disclosed. The method of resolving the racemic trans-hexahydrobenzo¢a!phenanthridines into their component enantiomers is also disclosed. Pharmacological evidence reveals that only one of the enantiomers of a preferred phenanthridine, dihydrexidine, the (6aR, 12bS)-(+)-isomer, is active in binding to both D1-like and D2-like dopamine receptors. Various other compounds, compositions, and methods of using the optically active stereoisomers are likewise disclosed.
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