치오포스포티로신을 함유한 펩티드 유도체의 중간체 합성

Synthesis of the Key Intermediate for the Preparation of Thiophosphotyrosine-containing Peptide Derivatives

N-(tert-Butoxycarbonyl)-omicron-(dicyanoethylthiophosphono)-L-tyrosine(7), the key intermediate for the synthesis of thiophosphotyrosine-containing peptide derivatives, was prepared. For the phosphorylation, we used tau-Boc-tyrosine and phosphoramidite in the presence of 1H-tetrazol. For the protection of thiophosphate moiety, cyanoethyl protecting group was used. Thiophosphotyrosine-containing peptides could be used as tools for the elucidation of mechanism of signal transduction pathway and also prepared as PTK inhibitors, PTPase inhibitors and cytosolic protein binding blockers. It may be contributed for the development of potential anticancer agents.