| 摘要 |
PURPOSE:The difference in properties of the salt formed from 2,5,9-trimetyl-6,7- benzomorphane is utilized to separate 9-alpha-methyl isomer and 9-beta-methyl isomer, resulting in high-yield collection of the 9-alpha-methyl isomer. CONSTITUTION:Two kinds of stereoisomers of the compound of formula I on the methyl group in the 9-position [cis isomer (alpha-isomer) of formula I and trans isomer (beta-isomer) of formula I )in the form of their mixture are converted into their salts with an acid such as fumaric, benzenesulfonic or p-toluenesulfonic acid. The resultant salt mixture of these isomers are separated utilizing the difference in their properties, e.g., by partition crystallization, then the cis isomer of formula I is obtained in high yiled and high efficiency. The isolated product is used as an intermediate of a compound of formula II (alpha-isomer) acting as a nonaddictive analegesic.
|
