Application of a photolabile backbone amide linker for cleavage of internal amides in the synthesis towards melanocortin subtype-4 agonists

Publikation: Bidrag til tidsskriftTidsskriftartikelForskningfagfællebedømt

A new photolabile backbone amide handle has been developed for the synthesis of a melanocortin subtype-4 receptor (MCR4) agonist library in the solid phase. This traceless linker allows for the solid-supported synthesis of internal amides and their release under very mild, orthogonal conditions from solid support. The chemistry to attach an amide onto the linker is discussed. Structural variations of the linker in order to facilitate the attachment are investigated. The cleavage rate on the solid phase was measured. Finally, a small arylpiperazine library towards the MCR4 receptor was synthesized and its members characterized via HPLC, MS and NMR.

TidsskriftQSAR and Combinatorial Science
Udgave nummer3
Sider (fra-til)343-353
Antal sider11
StatusUdgivet - apr. 2005
Eksternt udgivetJa

ID: 326847434