The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 2-Amino-4,6-dichloro-5-methylpyrimidine(SMILESS: CC1=C(N=C(N)N=C1Cl)Cl,cas:7153-13-1) is researched.Safety of 3-Hydroxy-3-phenylpropanenitrile. The article 《Structure-Activity Studies on a Series of a 2-Aminopyrimidine-Containing Histamine H4 Receptor Ligands》 in relation to this compound, is published in Journal of Medicinal Chemistry. Let’s take a look at the latest research on this compound (cas:7153-13-1).
A series of 2-aminopyrimidines, e.g. I (R1 = H, Me, OMe, NH2, Ph; R2 = H, Cl, I, NHMe, NMe2, Ph, 2-MeOC6H4, 1-naphthyl, 4-pyridyl, etc.), was synthesized as ligands of the histamine H4 receptor (H4R). Starting from a pyrimidine hit that was identified in an HTS campaign, SAR studies were carried out to optimize the potency, which led to compound I (R1 = H; R2 = t-Bu). This compound was further studied by systematically modifying the core pyrimidine moiety, the methylpiperazine at position 4, the NH2 at position 2, and positions 5 and 6 of the pyrimidine ring. The pyrimidine 6 position benefited the most from this optimization, especially in analogs in which the 6-tert-Bu was replaced with aromatic and secondary amine moieties. The highlight of the optimization campaign was compound I (R1 = H; R2 = 4-NCC6H4), which was potent in vitro and was active as an anti-inflammatory agent in an animal model and had antinociceptive activity in a pain model, which supports the potential of H4R antagonists in pain.
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Reference:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics