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The last decade has witnessed great progress on transition metal-catalyzed C-H bond functionalization.These newly developed synthetic methods provide alternative and valuable approaches to assemble protected unnatural amino acids and peptides from simple amino acid derivatives.In this report we wish to describe that 2-methoxyiminoacetyl(MIA)is a conveniently available,removable and convertible auxiliary for promoting Pd-catalyzed functionalization of C-H bond of amino acid derivatives,[1] leading to formation of several types of protected unnatural amino acids and peptides in a convenient manner.