📜(1S)-(+)-2-氮杂双环[2.2.1]庚-5-烯-3-酮置于lithium Aluminium Tetrahydride,Mercury(II) Diacetate,水,N,N-二异丙基乙胺体系中,化学反应生成6-羟基-2-氮杂-双环[2.2.1]庚烷-2-羧酸叔丁酯
参考文献:Discovery Of A Nortropanol Derivative As A Potent And Orally Active Gpr119 Agonist For Type 2 Diabetes
标题:Discovery Of A Nortropanol Derivative As A Potent And Orally Active Gpr119 Agonist For Type 2 Diabetes
摘要:The Lead Optimization Studies Of A Series Of Gpr119 Agonists Incorporating A Nortropanol Scaffold Are Described. Extensive Structure-Activity Relationship (Sar) Studies Of The Lead Compound 20F Led To The Identification Of Compound 36J As A Potent,Single Digit Nanomolar Gpr119 Agonist With High Agonist Activity. Compound 36J Was Orally Active In Lowering Blood Glucose Levels In A Mouse Oral Glucose Tolerance Test And Increased Plasma Insulin Levels In A Rat Hyperglycemic Model. It Showed Good To Excellent Pharmacokinetic Properties In Rats And Monkeys And No Untoward Activities In Counter-Screen Assays. Compound 36J Demonstrated An Attractive In Vitro And In Vivo Profile For Further Development. (C) 2011 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2011.04.035