Preparation of polymer-bound trityl-hydrazines and their application in the solid phase synthesis of partially protected peptide hydrazides
Preparation of polymer-bound trityl-hydrazines and their application in the solid phase synthesis of partially protected peptide hydrazides
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DOI：
10.1007/bf00142245
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发表时间：
2004
期刊：
影响因子：
--
通讯作者：
G. Stavropoulos;D. Gatos;V. Magafa;K. Barlos
中科院分区：
文献类型：
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作者：
G. Stavropoulos;D. Gatos;V. Magafa;K. Barlos
聚合物结合的 N-三苯甲基肼 4 很容易通过聚合三苯甲基氯化物 3 与肼反应来制备。随后，化合物4已成功应用于使用Fmoc-或Trt-氨基酸的1-羟基苯并三唑基酯固相合成部分受保护的肽酰肼。合成的肽酰肼可以通过温和的酸性处理从树脂上定量地分离出来，而苄基和叔丁基保护基团不受影响。
Polymer-boundN-tritylhydrazines4were easily prepared by reacting polymeric tritylchlorides3with hydrazine. Subsequently, compounds4have been successfully applied to the solid phase synthesis of partially protected peptide hydrazides using 1-hydroxybenzotriazolyl esters of Fmoc- or Trt-amino acids. The synthesized peptide hydrazides can be quantitatively split off from the resins by mild acidic treatment, while the benzyl- andtert-butyl protecting groups remain unaffected.