DeBernardis J F, Kerkman D J, Arendsen D L, Buckner S A, Kyncl J J, Hancock A A
J Med Chem. 1987 Jun;30(6):1011-7. doi: 10.1021/jm00389a009.
(+/-)-2-(5,6-Dimethoxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline has been resolved into its (+) and (-) enantiomers, and the absolute configuration was established by single-crystal X-ray diffraction studies. The more active isomer has been assigned the R absolute configuration. Cleavage of the respective (+)- and (-)-dimethyl ethers with boron tribromide provided the corresponding (+)- and (-)-2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthl)imidazoline hydrobromides and these were pharmacologically characterized. In various preparations, the R enantiomer has been shown to be an extremely potent alpha agonist with preferential activity at the alpha 2-adrenergic receptor.
（±）-2-（5,6-二甲氧基-1,2,3,4-四氢-1-萘基）咪唑啉已被拆分为其（+）和（-）对映体，并且通过单晶X射线衍射研究确定了绝对构型。活性更高的异构体被指定为R绝对构型。用三溴化硼裂解相应的（+）-和（-）-二甲醚，得到相应的（+）-和（-）-2-（5,6-二羟基-1,2,3,4-四氢-1-萘基）咪唑啉氢溴酸盐，并对其进行了药理学表征。在各种制剂中，R对映体已被证明是一种极其有效的α激动剂，对α2-肾上腺素能受体具有优先活性。
