600168-40-9Relevant academic research and scientific papers
Assembly of organosilver coordination frameworks with polycyclic benzenoid aromatic ethynide ligands
Hau, Sam C.K.,Mak, Thomas C.W.
, p. 123 - 133 (2015/08/18)
Abstract In a series of nine silver(I) complexes synthesized with ethynyl-functionalized condensed-ring benzenoid aromatics, the terminal ethynide group is invariably inserted into an argentophilic Agn (n = 4-5) basket, leading to the generation of coordination chains or multinuclear metallocycles via silver-aromatic interaction and strong face-to-face aromatic π-π stacking interaction. The coordination preferences of the ethynide ligand with respect to the size of the aromatic nucleus proved to be dominant factors in directing the construction of multi-dimensional organosilver(I) networks, which are consolidated by weak intermolecular interactions in supramolecular assembly.
NHC catalysed trimethylsilylation of terminal alkynes and indoles with Ruppert's reagent under solvent free conditions
Arde, Panjab,Reddy, Virsinha,Anand, Ramasamy Vijaya
, p. 49775 - 49779 (2014/12/11)
An organo-catalytic protocol for the trimethylsilylation of terminal alkynes employing Ruppert's reagent (CF3SiMe3) as a trimethylsilyl source has been developed under solvent and fluoride free conditions. This method was found to be very effective as a variety of terminal alkynes bearing aliphatic or aromatic substituents underwent smooth transformation to their corresponding silylated products in excellent yields within a few minutes using N-heterocyclic carbene as an organo-catalyst. This methodology was also applied to the chemospecific N-silylation of indoles. This journal is
Structure-guided design of A3 adenosine receptor-selective nucleosides: Combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions
Tosh, Dilip K.,Deflorian, Francesca,Phan, Khai,Gao, Zhan-Guo,Wan, Tina C.,Gizewski, Elizabeth,Auchampach, John A.,Jacobson, Kenneth A.
supporting information; experimental part, p. 4847 - 4860 (2012/07/27)
(N)-Methanocarba adenosine 5′-methyluronamides containing known A3 AR (adenosine receptor)-enhancing modifications, i.e., 2-(arylethynyl)adenine and N6-methyl or N6-(3-substituted- benzyl), were nanomolar full agonists of human (h) A3AR and highly selective (Ki ~0.6 nM, N6-methyl 2-(halophenylethynyl) analogues 13 and 14). Combined 2-arylethynyl-N6-3-chlorobenzyl substitutions preserved A3AR affinity/selectivity in the (N)-methanocarba series (e.g., 3,4-difluoro full agonist MRS5698 31, K i 3 nM, human and mouse A3) better than that for ribosides. Polyaromatic 2-ethynyl N6-3-chlorobenzyl analogues, such as potent linearly extended 2-p-biphenylethynyl MRS5679 34 (Ki hA3 3.1 nM; A1, A2A, inactive) and fluorescent 1-pyrene adduct MRS5704 35 (Ki hA3 68.3 nM), were conformationally rigid; receptor docking identified a large, mainly hydrophobic binding region. The vicinity of receptor-bound C2 groups was probed by homology modeling based on recent X-ray structure of an agonist-bound A2AAR, with a predicted helical rearrangement requiring an agonist-specific outward displacement of TM2 resembling opsin. Thus, the X-ray structure of related A2AAR is useful in guiding the design of new A3AR agonists.
