AUXILIARY FOR AMIDE BOND FORMATION

摘要

This invention relates to novel auxiliaries for the formation of amide bonds, and to the use of these auxiliaries in a variety of synthetic applications, such as the synthesis of peptides and peptidomimetic compounds, and in particular for the synthesis of "small cyclic peptides", so-called "difficult" peptide sequences, and large peptides with a native peptide backbone. The auxiliaries of the invention are also useful in the synthesis of peptides or of C-terminal modified peptides, and in on-resin cyclisation of organic molecules, ligating chemistry, backbone substitution and as backbone linkers. In a particularly preferred embodiment, the invention provides auxiliaries which can be removed by photolysis. Methods of synthesis of a linear or cyclic peptide, a C-terminal modified peptide, or of on-resin cyclisation of a peptide molecule, comprising the step of linking an amine nitrogen atom to an auxiliary compound of the invention, specific auxiliary compounds, which may optionally be linked to a solid support, and kits for synthesis are disclosed and claimed.