CAS: 184766-45-8; 2-Methyl-5-(2-Methyl-1,3-Dioxolan-2-yl)Pyridine

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CAS号36357-38-7 5-乙酰基-2-甲基嘧啶 | CAS号107-21-1 乙二醇 | CAS号5470-70-2 6-甲基烟酸甲酯 | CAS号21683-58-9 ethyl 3-(2-meth... | CAS号184766-50-5 5-(2-甲基-1,3-二氧杂... | CAS号184766-55-0 4-[2-(5-(2-METH... | CAS号184766-66-3 5-[4-[2-[5-(2-M...

📜6-甲基烟酸甲酯置于硫酸,Sodium Hydride,对甲苯磺酸体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 12.5H,反应生成3-(2-甲基-1,3-二氧戊烷-yl)-6-甲基吡啶
参考文献:Synthesis And Biological Activity Of Metabolites Of The Antidiabetic,Antihyperglycemic Agent Pioglitazone
标题:Synthesis And Biological Activity Of Metabolites Of The Antidiabetic,Antihyperglycemic Agent Pioglitazone
摘要:Pioglitazone (5-(4-(2-(5-Ethyl-2-Pyridyl)Ethoxy)Benzyl)-2,4-Thiazolidinedione,2) Is A Prototypical Antidiabetic Thiazolidinedione That Had Been Evaluated For Possible; Clinical Development. Metabolites 6-9 Have Been Identified After Dosing Of Rats And Dogs. Ketone 10 Has Not Yet Been Identified As A Metabolite But Has Been Added To The List As A Putative Metabolite By Analogy To Alcohol 6 And Ketone 7. We Have Developed Improved Syntheses Of Pioglitazone (2) Metabolites 6-9 And The Putative Metabolite Ketone 10. These Entities Have Been Compared In The Kka(Y) Mouse Model Of Human Type-Ii Diabetes To Pioglitazone (2). Ketone 10 Has Proven To Be The Most Potent Of These Thiazolidinediones In This In,Vivo Assay. When 6-10 Were Compared In Vitro In The 3T3-L1 Cell Line To 2,For Their Ability To Augment Insulin-Stimulated Lipogenesis,10 Was Again The Most Potent Compound With 6,7,And 9 Roughly Equivalent To 2. These Data Suggest That Metabolites 6,7,And 9 Are Likely To Contribute To The Pharmacological Activity Of Pioglitazone (2),As Had Been Previously Reported For Ciglitazone (1).
Doi:10.1021/jm9605694