60034-93-7Relevant academic research and scientific papers
Manganese-catalyzed directed methylation of C(sp2)-H bonds at 25 °C with high catalytic turnover
Sato, Takenari,Yoshida, Takumi,Al Mamari, Hamad H.,Ilies, Laurean,Nakamura, Eiichi
supporting information, p. 5458 - 5461 (2017/11/06)
We report here a manganese-catalyzed C-H methylation reaction of considerable substrate scope, using MeMgBr, a catalytic amount of MnCl2· 2LiCl, and an organic dihalide oxidant. The reaction features ambient temperature, low catalyst loading, typically 1%, high catalytic turnover reaching 5.9 × 103, and no need for an extraneous ligand and illustrates a unique catalytic use of simple manganese salts for C-H activation, which so far has relied on catalysis by manganese carbonyls.
Isochromanone-based urotensin-II receptor agonists
Lehmann, Fredrik,Currier, Erika A.,Olsson, Roger,Hacksell, Uli,Luthman, Kristina
, p. 3057 - 3068 (2007/10/03)
A series of analogues of the selective non-peptide urotensin II (UII) receptor agonist 3-(4-chlorophenyl)-3-(2-dimethylaminoethyl)-isochroman-1-one (AC-7954, 1) was synthesized and evaluated for UII agonist activity using a functional cell-based assay. The introduction of a methyl group in the 4-position resulted in a complete loss of activity, whereas substituents in the aromatic rings were beneficial. Sterically demanding amino groups were also detrimental to the activity. Several potent agonists were identified, six compounds being equally or more potent than 1. The most potent compound in the series was the 6,7-dimethyl analogue of 1 (16, pEC50 6.87). The racemate of 16 was resolved into the pure enantiomers using preparative straight phase HPLC. It was shown that the potency resides in the (+)-enantiomer (pEC50 7.11). The synthesized compounds seem to be selective for the UII receptor as no activities were observed at the closely related SSTR3 and 5 receptors.
UROTENSIN II RECEPTOR MODULATORS
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Page 39, (2010/02/04)
Disclosed are compounds of Formula I, or salts or prodrugs thereof, complexed with a human urotensin II receptor as defined herein. Also disclosed are compounds of Formula II, or salts or prodrugs thereof, as defined herein. Also disclosed are methods of modulating the activity of a urotensin II receptor using a compound of Formula I, or a compound of Formula II, or salts or prodrugs thereof. In addition, methods of treating diseases related to the activity of urotensin II receptors are disclosed.
Fused pyridine derivatives
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Example 228, (2010/01/30)
The present provides a condensed pyridine compound (I) represented by the following formula: (wherein, R2represents ring A represents benzene ring, pyridine ring, thiophene ring or furan ring; and B represents its pharmaceutically acceptable salt or hydrates thereof, which is a clinically useful medicament having a serotonin antagonism, in particular, that for treating, ameliorating or preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.
