Conjugates of Catecholamines. 5. Synthesis and β-Adrenergic Activity of N-(Aminoalkyl) norepinephrine Derivatives

AB Reitz, E Sonveaux, RP Rosenkranz…

文献索引：Reitz, Allen B.; Sonveaux, Etienne; Rosenkranz, Roberto P.; Verlander, Michael S.; Melmon, Kenneth L.; et al. Journal of Medicinal Chemistry, 1985 , vol. 28, # 5 p. 634 - 642

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被引用次数: 7

摘要

We first examined derivatization of the aromatic ring of isoproterenol (I). Direct substitution on the ring, however, in most cases eliminated@-adrenergic activity, making this approach unattractive for attachment to carriers. l% b Substitution by an ether linkage to the benzylic hydroxyl has been reported to result in the loss of activity! When we prepared and rigorously purified the P-ethyl ether derivative of isoproterenol, we also observed virtually complete ...