新型多肽固相合成链接子{4-[叔丁氧羰基氨基-(2',4'-二甲氧基苄基)]苯氧基乙酸}的合成

Synthesis of a Novel Linker 4-[t-Butyloxy carbonylamino)-(2',4'-dimethoxybenzyl)]phenoxyacetic Acid for the Solid-phase Synthesis of Peptide

以4-羟基苯甲酸和间苯二甲醚为原料,经傅-克酰基化反应、苄基保护、还原氨化、Boc保护氨基、脱苄基、亲核取代反应、酯水解等7步反应合成了一个新型的多肽固相合成的链接子4-[叔丁氧羰基氨基-(2',4'-二甲氧基苯基)]苯氧基乙酸,总收率47.2%,纯度>98%,其结构经1H NMR,13C NMR和HR-MS确证。

A novel linker RL1 { 4- [ t-Butyloxy carbonylamino） - （2＇ ,4＇-dimethoxybenzyl） ] phenoxyacetic acid } in total yield of 47.2% with purity of over 98%, a linkage for the solid-phase synthesis of peptide, was synthesized by a seven-step reaction including F -C reaction, group protection, reductive amination, deprotection reactions, ere, using 4-hydroxybenzoic acid and 1,3-dimethoxybenzene as the starting materials. The structure was confirmed by 1H NMR, 13C NMR and HR-MS.