The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 2-Bromo-5-methylpyrazine( cas:98006-90-7 ) is researched.SDS of cas: 98006-90-7.Kers, Inger; Macsari, Istvan; Csjernyik, Gabor; Nyloef, Martin; Skogholm, Karin; Sandberg, Lars; Minidis, Alexander; Bueters, Tjerk; Malmborg, Jonas; Eriksson, Anders B.; Lund, Per-Eric; Venyike, Elisabet; Luo, Lei; Nystroem, Jan-Erik; Besidski, Yevgeni published the article 《Phenethyl nicotinamides, a novel class of NaV1.7 channel blockers: Structure and activity relationship》 about this compound( cas:98006-90-7 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: nicotinamide arylethyl heteroaryl preparation sodium channel blocker. Let’s learn more about this compound (cas:98006-90-7).
The NaV1.7 ion channel is an attractive target for development of potential analgesic drugs based on strong genetic links between mutations in the gene coding for the channel protein and inheritable pain conditions. The (S)-N-chroman-3-ylcarboxamide series was used as a starting point for development of new channel blockers resulting in the phenethyl nicotinamide series I (X = CH, CF, N; R1 = 3-pyridyl, 2-methoxy-5-pyrimidinyl, 5-methoxy-2-pyrazinyl, etc.; R2 = H, Cl, F, Me, etc.; R3 = R4 = H, F; R3 = Me, R4 = H; R5 = F3CCH2CH2O, F3CCH2OCH2, etc.). The structure and activity relationship for this series was established and the metabolic issues of early analogs were addressed by appropriate substitutions. Compound I (X = CH; R1 = 5-methoxy-2-pyrazinyl; R2 = H; R3 = R4 = F; R5 = F3CCH2OCH2) displayed acceptable overall in vitro properties and in vivo rat PK profile.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics