610279-04-4Relevant articles and documents
6-ethoxy-3, 4-dihydro-2, 7-naphthyridine-1 (2H)-ketone and synthesis method thereof
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Paragraph 0020-0022; 0031-0033; 0042-0044, (2020/12/05)
The invention belongs to the technical field of organic synthesis, and relates to 6-ethoxy-3, 4-dihydro-2, 7-naphthyridine-1 (2H)-ketone and a synthesis method thereof. The method for preparing the compound comprises the following steps of: taking 2, 5-dibromo-4-methylpyridine as a raw material; preparing 6-ethoxy-3, 4-dihydro-2, 7-naphthyridine-1 (2H)-ketone through five steps of reactions including substitution, Suzuki coupling, carbonyl insertion reaction, amidation and dehydration reaction; the synthetic route is simple, the cost is low, the efficiency is high, and the obtained pyridine derivative 6-ethoxy-3, 4-dihydro-2, 7-naphthyridine-1 (2H)-ketone can be used as a medical intermediate.
Piperazine oxadiazole inhibitors of acetyl-CoA carboxylase
Bourbeau, Matthew P.,Siegmund, Aaron,Allen, John G.,Shu, Hong,Fotsch, Christopher,Bartberger, Michael D.,Kim, Ki-Won,Komorowski, Renee,Graham, Melissa,Busby, James,Wang, Minghan,Meyer, James,Xu, Yang,Salyers, Kevin,Fielden, Mark,Véniant, Murielle M.,Gu, Wei
supporting information, p. 10132 - 10141 (2014/01/17)
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the piperazine oxadiazoles were overcome by blocking predicted sites of metabolism, resulting in compounds with suitable properties for further in vivo studies. Compound 26 was shown to inhibit malonyl-CoA production in an in vivo pharmacodynamic assay and was advanced to a long-term efficacy study. Prolonged dosing with compound 26 resulted in impaired glucose tolerance in diet-induced obese (DIO) C57BL6 mice, an unexpected finding.