Six new photolabile linkers for solid phase synthesis. 2. Coupling of various building blocks and photolytic cleavage

Eva B. Åkerblom
Medicinal Chemistry, Pharmacia & Upjohn AB, SE-751 82 Uppsala, Sweden
and Department of Organic Pharmaceutical Chemistry, Uppsala Biomedical Centre, Uppsala University, Box 574, SE-751 23 Uppsala, Sweden

Abstract
Photolabile linkers are very useful in the generation of combinatorial libraries as they offer compound cleavage under mild conditions directly into a solvent suitable for biological testing. Six new photolabile linkers have been developed which allow coupling of building blocks with a carboxy, amino, hydroxy and sulfonyl group. Photolytic cleavage of these building blocks will give libraries with carboxy, amido, methylamido, amino, ureido, hydroxy, aminocarbonyloxy and aminosulfonyl terminal groups. Coupling conditions for these reactions were elucidated and the photolytic cleavage reaction was studied.

Keywords
combinatorial chemical library, linkers, photolysis, solid phase synthesis