| 摘要 |
Biologically active (z)-azabicyclo oxime ethers may be isolated without chromatographic separation, and in high yield and Z/E purity, through the coupling of an azabicycloketone of formula (a) with an O-substituted hydroxylamine of formula (b) in acidic aqueous solution. Neutralization and subsequent isolation of the free base followed by precipitation of the salt allows separation of the Z-isomer with purity in excess of 98%. In formula (b): R is optionally substituted C4-12 aryl or heteroaryl, wherein the substituents are selected from alkoxy, halo, nitro, cyano, C1-8 lower alkyl, C2-8 alkenyl or alkynyl, C3-C8 cycloalkyl, C4-C8 cycloalkenyl, or substituted lower alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkynyl.
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