53473-35-1Relevant articles and documents
Intramolecular Büchner reaction and oxidative aromatization with SeO2 or O2
Morita, Shunya,Yoshimura, Tomoyuki,Matsuo, Jun-ichi
, p. 729 - 732 (2019/07/31)
Intramolecular Büchner reaction of 1-diazo-5-phenylpentan-2-ones followed by oxidation with SeO2 or O2 in the presence of silica gel regioselectively gave 8-formyl-1-tetralones or one-carbon-lacking 1-tetralones, respectively.
Asymmetric catalytic aziridination of dihydronaphthalenes for the preparation of substituted 2-aminotetralins
Aaseng, Jon Erik,Melnes, Silje,Reian, Gard,Gautun, Odd R.
experimental part, p. 9790 - 9797 (2011/02/22)
An enantioselective synthesis of substituted 2-aminotetralins from dihydronaphthalenes in four steps is described. The key step is the Jacobsen's (diimine)copper-catalyzed asymmetric aziridination of dihydronaphthalenes to the respective aziridines in 33-82% yields and 60-87% enantiomeric excess. The enantioselectivity and the yield were dependent on the properties of the nitrene precursor. pTsNIPh appeared in general to give better results than pNsNIPh. Aziridines were ring-opened in the benzylic position by catalytic hydrogenolysis in quantitative yields, and deprotected in two steps to the respective 2-aminotetralins in 66-85% yields. The synthesis of (S)-2-aminotetralin (>98% ee) and (S)-2-amino-7-methoxytetralin (56% ee) were accomplished in 30 and 52% overall yields, respectively.
2-Aminothiazoles: A new class of agonist allosteric enhancers of A1 adenosine receptors
Chordia, Mahendra D.,Murphree, Lauren J.,Macdonald, Timothy L.,Linden, Joel,Olsson, Ray A.
, p. 1563 - 1566 (2007/10/03)
This report describes the synthesis and structure-activity relationships of a new class of A1 adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC50 of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 μM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC50 of 38 μM.
