1374516-13-8Relevant academic research and scientific papers
Making Dimethylamino a Transformable Directing Group by Nickel-Catalyzed C-N Borylation
Zhang, Hua,Hagihara, Shinya,Itami, Kenichiro
, p. 16796 - 16800 (2015/11/16)
The dimethylamino (Me2N) group is arguably the most versatile functional group capable of highly efficient and site-selective directed aromatic functionalizations at the ortho-, meta-, and para-positions depending on reaction conditions. While the repertoire of Me2N-directed reactions is growing at a rapid pace, the lack of a general method to transform this group to other functionalities hampers its wider application in organic synthesis. Here we report nickel-catalyzed C-N borylations of aryl- and benzyl-dimethylamines that permit the conversion of a huge library of largely underutilized Me2N-containing organic molecules into various functional molecules by taking advantage of the wealth of existing C-B functionalization methods.
Discovery of a potent and selective GPR120 agonist
Shimpukade, Bharat,Hudson, Brian D.,Hovgaard, Christine Kiel,Milligan, Graeme,Ulven, Trond
, p. 4511 - 4515 (2012/08/13)
GPR120 is a receptor of unsaturated long-chain fatty acids reported to mediate GLP-1 secretion, insulin sensitization, anti-inflammatory, and anti-obesity effects and is therefore emerging as a new potential target for treatment of type 2 diabetes and metabolic diseases. Further investigation is however hindered by the lack of suitable receptor modulators. Screening of FFA1 ligands provided a lead with moderate activity on GPR120 and moderate selectivity over FFA1. Optimization led to the discovery of the first potent and selective GPR120 agonist.
