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本文介绍的正交杂化合成策略(HOP)采用以Merrifield树脂为载体,将Fmoc化学与Boc化学结合应用组装多肽,经酸解脱除侧链保护基得到键合在树脂上的裸肽树脂中间体,并进一步经温和、简便的胺解反应,衍生出多肽C末端N-取代酰胺或侧链内酰胺环肽化合物。HOP策略得到的终产物粗制品中不含有常规工艺的酸解试剂等杂质,所以采用该方式合成肽酰胺在收率及粗产物纯度等方面均比较理想。
The orthogonal hybridization strategy (HOP) introduced in this paper adopts Merrifield resin as the carrier, combines the Fmoc chemistry with Boc chemistry to assemble the polypeptide, removes the side chain protecting group by acid solution to obtain the bare peptide resin intermediate , And further derivatizing a C-terminal N-substituted amide or a side-chain lactam cyclic peptide compound by a mild and convenient amineysis reaction. The final products obtained by HOP strategy do not contain the impurities such as the acid hydrolysis reagent of the conventional process. Therefore, the synthesis of peptide amides by this method is ideal in terms of yield and crude product purity.