175353-91-0Relevant articles and documents
Solution-phase combinatorial synthesis via the olefin metathesis reaction
Boger, Dale L.,Chai, Wenying,Ozer, Rachel S.,Andersson, Carl-Magnus
, p. 463 - 468 (1997)
The preparation of C2-symmetric and unsymmetric chemical libraries by solution-phase techniques including the use of the olefin metathesis reaction to join and combinatorially randomize the length of a linking tether is detailed.
Synthesis and evaluation of (4-chlorobenzhydryl) piperazine amides as sodium channel Nav1.7 inhibitors
Back, Seung Keun,Kam, Yoo Lim,Oh, Jung Ae,Na, Heung Sik,Ih, Uhtaek,Park Choo, Hea-Young
, p. 2290 - 2297 (2015/09/22)
Blockage of voltage-gated sodium channels is used to treat neuropathic pain which is chronic and can become debilitating. Sodium channels Nav1.7-1.9 are especially attractive targets for drug discovery because of the broad therapeutic potential of their m
Solution-phase combinatorial synthesis: Convergent multiplication of diversity via the olefin metathesis reaction
Boger, Dale L.,Chai, Wenying
, p. 3955 - 3970 (2007/10/03)
The solution-phase synthesis of iminodiacetic acid diamides functionalized with ω-alkenes and their dimerization via the olefin metathesis reaction in the preparation of mixture libraries are detailed. Libraries containing as many as 113,232 compounds prepared from only N-BOC- iminodiacetic acid anhydride (1), 15 amines, and 4 ω-alkene carboxylic acids illustrate the diversity that may be achieved by a convergent versus divergent combination of a small number of monomer building blocks that provides the multiplication of diversity typically associated with linear library syntheses including peptides, oligonucleotides and sequential template functionalizations. Unlike the divergent synthesis of such libraries which is amenable to solid-phase synthesis techniques, the convergent synthesis is especially well suited for solution-phase synthesis and is precluded by solid-phase techniques since the combining components typically would be on mutually exclusive phases.