YAKHAK HOEJI (약학회지)

The Pharmaceutical Society of Korea (대한약학회)
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Synthesis of the Key Intermediate for the Preparation of Thiophosphotyrosine-containing Peptide Derivatives

치오포스포티로신을 함유한 펩티드 유도체의 중간체 합성

  • Published : 1997.10.01
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Abstract

N-(tert-Butoxycarbonyl)-O-(dicyanoethylthiophosphono)-L-tyrosine(7), the key intermediate for the synthesis of thiophosphotyrosine-containing peptide derivat ives, was prepared. For the phosphorylation, we used t-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.

Keywords

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