Linkers for solid-phase synthesis of small molecules: coupling and cleavage techniques

Combinatorial chemistry has an impact on lead discovery as well as on lead optimization. The efficient synthesis of individual compounds, which has re placed the initial goal of synthesizing highly complex mixtures, can be car ried out in solution or on a suitable support material. The role of a linke r in solid-phase chemistry is to connect the starting material reversibly w ith the solid support. The main challenges in choosing an appropriate linke r molecule are that the starting compounds can be easily attached to it, th at it is chemically stable in the envisaged synthesis conditions and that i t should be possible to cleave the final products with high efficiency.