PYRIDINE DERIVATIVES USEFUL AS CYCLOOXYGENASE INHIBITOR
申请人:FUJISAWA PHARMACEUTICAL CO., LTD.
公开号:EP1355885A1
公开(公告)日:2003-10-29
[EN] PYRIDINE DERIVATIVES USEFUL AS CYCLOOXYGENASE INHIBITOR<br/>[FR] DERIVES DE PYRIDINE UTILES EN TANT QU'INHIBITEURS DE CYCLO-OXYGENASE
申请人:FUJISAWA PHARMACEUTICAL CO
公开号:WO2002055502A1
公开(公告)日:2002-07-18
A compound of the formula (I), wherein R1 is hydrogen, halogen, carbymoyl, cyano, formuly, or lower alkyl optionally substituted with halogen, amino or a protected amino; R2 is hydrogen, halogen, cyano or lower alkoxy; R3 is phenyl or pyridyl, each of which is substituted with lower alkoxy; and R4 is lower alkoxy; provided that either R1 or R2 is hydrogen, then the other is other than hydrogen, or its salts, which are useful as a medicament.
Borane-Catalyzed Reduction of Pyridines via a Hydroboration/Hydrogenation Cascade
作者:Zhao-Ying Yang、Heng Luo、Ming Zhang、Xiao-Chen Wang
DOI:10.1021/acscatal.1c02876
日期:2021.9.3
of pyridines. The method was particularly effective for 2,3-disubstitutedpyridines, which generated piperidines in high yields with high cis selectivity. Mechanistic studies indicated that the pyridine substrates and the piperidine products sequentially acted as bases in cooperation with B(C6F5)3 to split H2. The broad functional group tolerance of the method allowed its use for the synthesis of some
我们已经开发了一种用于 B(C 6 F 5 ) 3催化的吡啶的硼氢化/氢化级联还原的方法。该方法对 2,3-二取代吡啶特别有效,它以高产率和高顺式选择性生成哌啶。机理研究表明,吡啶底物和哌啶产物依次作为碱基与B(C 6 F 5 ) 3合作分裂H 2。该方法的广泛官能团耐受性使其可用于合成一些生物活性分子。
A New One-Pot, Three-Component
Synthesis of 2,3,5-Substituted or Annulated-6-(Methylthio)pyridines
A new one-pot, three-component synthesis of 2,3,5-substituted (or 2,3 -annulated)-6-(methylthio)pyridines by reacting acyclic or cyclic active methylene ketones, ammonium acetate, and bis(methylthio)acrolein (1) or its 2-phenyl analogue 8 (as 3-carbon-1,3-biselectrophilic components) in the presence of either AcOH-TFA (4:1) or ZnBr 2 (or Znl 2 ) catalysts has been reported.