155906-13-1Relevant articles and documents
P -Toluenesulfonic Acid Induced Conversion of Fluorinated Trimethylsilylethynylanilines into Aminoacetophenones: Versatile Precursors for the Synthesis of Benzoazaheterocycles
Politanskaya, Larisa,Tretyakov, Evgeny
, p. 555 - 564 (2017/11/03)
A simple and efficient approach to the synthesis of fluorinated amino-substituted acetophenones in good to excellent yields is reported. The heart of the proposed method consists of conversion of a Me 3 Si-C≡C- moiety into a MeC(=O)- group in the presence of p -tolu ene sulfonic acid (p -TSA) passing a stage of ethynylaniline formation. The reaction is metal-free, proceeds under mild conditions, and uses readily available starting compounds (trimethylsilylarylacetylene derivatives). The reaction provides access to amino-substituted acetophenones, which may serve as precursors for the synthesis of polyfluorinated azaheterocycles, having potential anticarcinogenic activity.
Identification of new potent GPR119 agonists by combining virtual screening and combinatorial chemistry
Wellenzohn, Bernd,Lessel, Uta,Beller, Andreas,Isambert, Timo,Hoenke, Christoph,Nosse, Bernd
, p. 11031 - 11041 (2013/02/25)
Virtual screening in a huge collection of virtual combinatorial libraries has led to the identification of two new structural classes of GPR119 agonists with submicromolar in vitro potencies. Herein, we describe the virtual screening process involving feature trees fragment space searches followed by a 3D postprocessing step. The in silico findings were then filtered and prioritized, and finally, combinatorial libraries of target molecules were synthesized. Furthermore the so-called activity-anchor principle is introduced as an element to increase the chance to generate true hits. An activity anchor is a structural element expected to provide key contributions to a certain biological activity. Application of this technique has led to the discovery of two new GPR119-agonist hit series, one of which was further optimized to progress as a novel lead class.
Tolane derivatives, liquid crystal compositions containing the derivatives and liquid crystal display devices using the compositions
-
, (2008/06/13)
A tolane derivative, a liquid crystal composition containing the derivative, and a liquid crystal display device including the composition, in which the tolane derivative is represented by the following general formula: STR1 wherein R represents a straigh