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2-甲氧基-5-硝基-6-甲基吡啶置于盐酸,水体系中,用97%的收率获得2-羟基-5-硝基-6-甲基吡啶
参考文献:Synthesis And Structure-activity Relationships Of N3-Pyridylpyrazinones As Corticotropin-Releasing Factor-1 (Crf1) Receptor Antagonists
标题:Synthesis And Structure-activity Relationships Of N3-Pyridylpyrazinones As Corticotropin-Releasing Factor-1 (Crf1) Receptor Antagonists
摘要:A Series Of N-3-Pyridylpyrazinones Was Investigated As Corticotropin-Releasing Factor-1 Receptor Antagonists. It Was Observed That The Binding Affinity Of Analogues Containing A Pyridyl Group Was Influenced Not Only By The Substitution Pattern On The Pyridyl Group,But Also By The Pk(A) Of The Pyridyl Nitrogen. Analogues Containing A Novel 6-(Difluoromethoxy)-2,5-Dimethylpyridin-3-Amine Group Were Among The Most Potent N-3-Pyridylpyrazinones Synthesized. The Synthesis And Sar Of N-3-Pyridylpyrazinones Is Described Herein. (C) 2010 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2010.01.129

专利信息

专利号:EP-2084147-B1
优先权日:2006-08-29
标 题:Heterocyclic fxr binding compounds
发明人：KREMOSER CLAUS; DEUSCHLE ULRICH; ABEL ULRICH; SCHULZ ANDREAS
权利人:PHENEX PHARMACEUTICALS AG
摘要:The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.