已经建立了亚硫酸钠(Na 2 S 2 O 4)还原没有吸电子取代基的吡啶鎓盐1到其相应的1,4-二氢吡啶(1,4-DHPs)2的条件,该反应先前被报道为失败。从获得的结果可以认识到疏水作用对于这种减少发生的重要性。本方法提供了通往许多1,4-DHP 2,特别是一系列手性衍生物如5和9的非常方便的途径。
[EN] COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES<br/>[FR] COMPOSÉS POUR TRAITER DES MALADIES NEURODÉGÉNÉRATIVES
申请人:ARRAY BIOPHARMA INC
公开号:WO2011123674A1
公开(公告)日:2011-10-06
The invention provides novel spirotetrahydronaphthalene compounds of Formula α that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
Methods of synthesizing nicotine analogs and derivatives are described. The methods are particularly useful for the regioselective production of enantiomerically pure nicotine anlogs having substituents at the C4 position. Intermediates useful for the synthesis of such compounds are also described.
[EN] FUSED RING COMPOUNDS<br/>[FR] COMPOSÉS CYCLIQUES CONDENSÉS
申请人:GENENTECH INC
公开号:WO2020035031A1
公开(公告)日:2020-02-20
Provided are fused ring compounds of Formula (I), Formula (II), or Formula (III), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods treatment by their administration.
[EN] ELECTRONIC TUNING OF SITE SELECTIVITY<br/>[FR] AJUSTEMENT ÉLECTRONIQUE DE SÉLECTIVITÉ DE SITE
申请人:UNIV ILLINOIS
公开号:WO2014059436A1
公开(公告)日:2014-04-17
Site-selective functionalization of Amphotericin B has been achieved by simply modifying the electronic nature of the reagents. A Hammett analysis is consistent with linking of this phenomenon to the Hammond postulate: electronic tuning to a more product- like transition state amplifies site-discriminating interactions between a reagent and its substrate. Electronic tuning of both an acylpyridinium donor and its carboxylate counterion further promoted site-divergent functionalization. A range of modifications to one of the many hydroxyl groups appended to the ion channel-forming natural product amphotericin B was achieved.