Click linker: efficient and high-yielding synthesis of a new family of SPOS resins by 1,3-dipolar cycloaddition.
[reaction: see text] Highly efficient methodology for the construction of functionalized resins was presented involving 1,3-dipolar cycloaddition as the key reaction step. On the basis of this concept, the first series of click backbone amide linkers were synthesized and the application of the FIMT resin 3f to the parallel synthesis of putative dopaminergic agents was demonstrated leading to the selective receptor ligands 10i and 10s revealing high affinity to the D4 subtype.
Department of Medicinal Chemistry, Emil Fischer Center, Friedrich-Alexander University, Schuhstrasse 19, D-91052 Erlangen, Germany.
Stefan
S
Löber
Pilar
P
Rodriguez-Loaiza
Peter
P
Gmeiner