939050-19-8Relevant articles and documents
Gold(I)-catalyzed Benzylation of (Hetero)aryl Boronic Acids with (Hetero)benzyl Bromides by the Strategy of a SN2-type Reaction
Zang, Wenqing,Wei, Yin,Shi, Min
, p. 2791 - 2795 (2018)
Herein, the first example of gold-catalyzed benzylation of (hetero)aryl boronic acids with (hetero)benzyl bromides to give the corresponding cross-coupling products in moderate to good yields is reported. The reaction proceeds through a possible intermolecular SN2-type reaction pathway to give a wide variety of di(hetero)arylmethanes as the desired products. An intriguing reaction mechanism has been proposed on the basis of control experiments, 31P-NMR spectroscopic detection and DFT calculations.
Feedstocks to Pharmacophores: Cu-Catalyzed Oxidative Arylation of Inexpensive Alkylarenes Enabling Direct Access to Diarylalkanes
Vasilopoulos, Aristidis,Zultanski, Susan L.,Stahl, Shannon S.
, p. 7705 - 7708 (2017/06/20)
A Cu-catalyzed method has been identified for selective oxidative arylation of benzylic C-H bonds with arylboronic esters. The resulting 1,1-diarylalkanes are accessed directly from inexpensive alkylarenes containing primary and secondary benzylic C-H bonds, such as toluene or ethylbenzene. All catalyst components are commercially available at low cost, and the arylboronic esters are either commercially available or easily accessible from the commercially available boronic acids. The potential utility of these methods in medicinal chemistry applications is highlighted.
Benzofuran derivatives as potent, orally active S1P1 receptor agonists: A preclinical lead molecule for MS
Saha, Ashis K.,Yu, Xiang,Lin, Jian,Lobera, Mercedes,Sharadendu, Anurag,Chereku, Srinivas,Schutz, Nili,Segal, Dalia,Marantz, Yael,McCauley, Dilara,Middleton, Scot,Siu, Jerry,Burli, Roland W.,Buys, Janet,Horner, Michelle,Salyers, Kevin,Schrag, Michael,Vargas, Hugo M.,Xu, Yang,McElvain, Michele,Xu, Han
scheme or table, p. 97 - 101 (2011/03/23)
We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3- fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P 1 agonist with >1000× s