81386-86-9Relevant academic research and scientific papers
Photocatalytic Synthesis of Diarylmethyl Silanes via 1,6-Conjugate Addition of Silyl Radicals to p-Quinone Methides
Luo, Cong,Lu, Wen-Hua,Wang, Guo-Qin,Zhang, Zheng-Bing,Li, Hai-Qiong,Han, Pan,Yang, Dan,Jing, Lin-Hai,Wang, Chen
, p. 3567 - 3576 (2022/02/23)
A novel photocatalytic method for the preparation of diarylmethyl silanes was reported through silyl radicals addition strategy to p-QMs (p-quinone methides). This protocol could tolerate a variety of functional groups affording the corresponding silylation products with moderate to excellent yields. The resulting silylation products could be easily converted into a series of bioactive GPR40 agonists and useful p-QMs precursors for the synthesis of compounds possessing both quaternary carbon centers and silicon substituents through simple operation. A plausible mechanism of silyl radicals to p-QMs was proposed on the basis of experimental results and previous literature.
Visible-Light-Triggered Cyanoalkylation of para-Quinone Methides and Its Application to the Synthesis of GPR40 Agonists
Zhang, Wei,Yang, Chen,Zhang, Zhi-Pei,Li, Xin,Cheng, Jin-Pei
, p. 4137 - 4142 (2019/06/04)
Cyanoalkylated diarylmethanes with biological and pharmacological potentials were synthesized from para-quinone methides and cyanoalkylating reagents through a photocatalytic process. This protocol is operationally simple and mild and has high efficiency,
Discovery of the imidazole-derived GPR40 agonist AM-3189
Ma, Zhihua,Lin, Daniel C.-H.,Sharma, Rajiv,Liu, Jinqian,Zhu, Liusheng,Li, An-Rong,Kohn, Todd,Wang, Yingcai,Liu, Jiwen,Bartberger, Michael D.,Medina, Julio C.,Zhuang, Run,Li, Frank,Zhang, Jane,Luo, Jian,Wong, Simon,Tonn, George R.,Houze, Jonathan B.
, p. 15 - 20 (2015/12/18)
As a follow-up to the GPR40 agonist AMG 837, which was evaluated in clinical trials for the treatment of type II diabetes, further optimization led to the discovery of AM-3189 (13k). AM-3189 is representative of a new class of compounds with minimal CNS penetration, superior pharmacokinetic properties and in vivo efficacy comparable to AMG 837.
Lewis acid promoted dual bond formation: Facile synthesis of dihydrocoumarins and spiro-tetracyclic dihydrocoumarins
Niharika, Pedireddi,Ramulu, Bokka Venkat,Satyanarayana, Gedu
, p. 4347 - 4360 (2014/06/23)
Lewis acid (FeCl3) mediated dual bond (C-C and C-O) formation for synthesis of 3,4-dihydrocoumarins is presented. This method has successfully delivered a number of dihydrocoumarins containing dense functionalities on the aromatic ring. Significantly, the present method enabled achieving dihydrocoumarins with tertiary as well as quaternary carbon atoms at the benzylic position. Gratifyingly, the novel spiro-tetracyclic lactones have also been dextrously prepared using this process. the Partner Organisations 2014.
AGONISTS OF GPR40
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Page/Page column 180-181, (2012/02/05)
The present invention relates to compounds that have the ability to modulate the activity of GPR40 and are there-fore useful in the treatment of GPR40 related disorders. In addition the invention relates to the compounds, methods for their preparation, pharmaceutical compositions containing the compounds and the uses of these compounds in the treatment of certain disorders related to GPR40 activity.
Conjugate addition of arylsilanes to unsaturated carbonyl compounds catalyzed by rhodium in air and water
Huang,Li
, p. 2348 - 2349 (2007/10/03)
ArSiCl3 and Ar2SiCl2, believed to be unstable in aqueous media, reacted efficiently with α,β-unsaturated ketones and esters in air and water (in the presence of sodium fluoride and a rhodium catalyst), giving good to excellent yields of the desired conjugate addition products.
