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.Reference of 2-Bromo-5-methylpyrazine.Szewczyk, Jason W.; Acton, John; Adams, Alan D.; Chicchi, Gary; Freeman, Stanley; Howard, Andrew D.; Huang, Yong; Li, Cai; Meinke, Peter T.; Mosely, Ralph; Murphy, Elizabeth; Samuel, Rachel; Santini, Conrad; Yang, Meng; Zhang, Yong; Zhao, Kake; Wood, Harold B. published the article 《Design of potent and selective GPR119 agonists for type II diabetes》 about this compound( cas:98006-90-7 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: GPR119 agonist antidiabetic preparation structure activity. Let’s learn more about this compound (cas:98006-90-7).
Screening of the Merck sample collection identified compound 1 (I) as a weakly potent GPR119 agonist (hEC50 = 3600 nM). Dual termini optimization of I led to compound II having improved potency, selectivity, and formulation profile, however, modest phys. properties (PP) hindered its utility. Design of a new core containing a cyclopropyl restriction yielded further PP improvements and when combined with the termini SAR optimizations yielded a potent and highly selective agonist III suitable for further preclin. development.
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Reference:
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics