78907-19-4Relevant articles and documents
Simple and efficient synthesis of 4,7-dimethoxy-1(H)-indene
Zhang, Xiang,Thimmaiah, Muralidhara,Fang, Shiyue
, p. 1873 - 1877 (2008/02/03)
Stirring 4,7-dimethoxy-1-indanol in chloroform at room temperature in the presence of a catalytic amount of p-toluenesulfonic acid gave 4,7-dimethoxy-1(H)-indene in quantitative yield. Other solvents, including benzene, which was the most frequently used one for this reaction, gave mostly polymeric materials. The new method was also effective for dehydration of other electron-rich benzylic alcohols. Copyright Taylor & Francis Group, LLC.
α-Adrenergic Agents. 1. Direct-Acting α1 Agonists Related to Methoxamine
DeMarinis, R. M.,Bryan, W. M.,Shah, D. H.,Hieble, J. P.,Pendleton, R. G.
, p. 1432 - 1437 (2007/10/02)
A series of phenylethylamines related to methoxamine has been prepared and evaluated for direct α1-receptor agonist activity.It has been observed that for open-chain compounds such as methoxamine, in which the amine-containing portion is free to adopt numerous conformations, an hydroxyl group is necessary for direct α1-adrenergic activity.When the hydroxyl is removed, however, the direct component of activity is greatly reduced unless the amine is incorporated into a more sterically defined structure.From our studies we have concluded that in order for a phenylethylamine to be active as a direct α1-receptor agonist it should have a β nitrogen in a fully extended conformation relative to a substituted phenyl ring.For optimum potency, the nitrogen should be exocyclic to a saturated six-membered ring.It may be further incorporated exocyclic or endocyclic into an additional ring so long as the amine occupies a well-defined region of space relative to the aromatic portion of a molecule.The ED50 values of some of the more potent compounds as α1-receptor agonists are on the order of 1 * 10-7 M.
