Metal-free halogenating agent-mediated removal of Alloc protecting groups from amino acids in solid-phase peptide synthesis, enabling sustainable manufacture of complex therapeutic peptides including GLP-1 analogs.

Patentradars sammanfattning

This invention discloses a metal-free method for removing allyloxycarbonyl (Alloc) protecting groups from amino groups of peptides bound to insoluble polymer supports using halogenating agents (e.g., iodine) and water in suitable solvent compositions. A second aspect combines Alloc removal with peptide bond formation in a single step without solvent displacement, enabling one-pot metal-free Alloc-SPPS synthesis. This approach addresses critical sustainability challenges in solid-phase peptide synthesis (SPPS) by eliminating toxic palladium catalysts while maintaining compatibility with complex peptide architectures, particularly lysine-branched GLP-1 analogs used therapeutically.

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