30561-09-2Relevant academic research and scientific papers
Synthesis and structure-activity relationships of N3-pyridylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists
Hartz, Richard A.,Ahuja, Vijay T.,Schmitz, William D.,Molski, Thaddeus F.,Mattson, Gail K.,Lodge, Nicholas J.,Bronson, Joanne J.,Macor, John E.
scheme or table, p. 1890 - 1894 (2010/07/06)
A series of N3-pyridylpyrazinones was investigated as corticotropin-releasing factor-1 receptor antagonists. It was observed that the binding affinity of analogues containing a pyridyl group was influenced not only by the substitution pattern on the pyridyl group, but also by the pKa of the pyridyl nitrogen. Analogues containing a novel 6-(difluoromethoxy)-2,5-dimethylpyridin-3-amine group were among the most potent N3-pyridylpyrazinones synthesized. The synthesis and SAR of N3-pyridylpyrazinones is described herein.
Synthetic Strategies toward the Synthesis of 2,4-Dimethoxypyrrolopyrimidine
Cupps, Thomas L.,Wise, Dean S.,Townsend, Leroy B.
, p. 1060 - 1064 (2007/10/02)
Two approaches to prepare 2,4-dimethoxypyrrolopyrimidine (1) are described. 2,4-Dimethoxy-6-methyl-5-nitropyrimidine (2) was converted to 6-(cyanomethyl)-2,4-dimethoxy-5-nitropyrimidine (6) in two steps.Subsequent catalytic hydrogenation of 6 produced 1.In a second approach, 2 was formylated, giving rise to 6--2,4-dimethoxy-5-nitropyrimidine (7).Hydrogenation of 7 resulted in the formation of 1.Reduction of 2 provided 5-amino-2,4-dimethoxy-6-methylpyrimidine (10).Reaction of compound 10 with triethyl orthoformate produced 2,4-dimethoxy-5--6-methylpyrimidine (11).Reaction of 11 with lithium diisopropylamide gave 2,4-dimethoxy-5-isocyano-6-methylpyrimidine (12).
