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发明公开
CN107098952A 抗菌环（甘氨酸‑色氨酸‑亮氨酸‑D‑亮氨酸‑缬氨酸‑天冬酰胺）肽的制备方法 审中-实审

抗菌环（甘氨酸‑色氨酸‑亮氨酸‑D‑亮氨酸‑缬氨酸‑天冬酰胺）肽的制备方法
摘要：
本发明公开了一种抗菌环(甘氨酸‑色氨酸‑亮氨酸‑D‑亮氨酸‑缬氨酸‑天冬酰胺)肽的制备方法，包括：1)将基体树脂与Fmoc‑Asn(trt)‑OH在溶剂中进行接触反应以制得一级树脂，接着通过甲醇封头一级树脂，然后通过Fmoc洗脱剂洗脱去除一级树脂的Fmoc，最后经过哌啶脱保护以得到二级树脂；2)将二级树脂依次与多种改性氨基酸进行多次改性反应得到三级树脂；3)将树脂洗脱剂洗脱去除三级树脂中的树脂基团以得到如式(V)所示结构的直链六肽；4)在溶剂、PyAop、HOAt和DIPEA的存在下，直链六肽进行液相环合反应以制得环状物；5)通过基团洗脱剂洗脱去除环状物上的Boc和Trt以制得抗菌环(甘氨酸‑色氨酸‑亮氨酸‑D‑亮氨酸‑缬氨酸‑天冬酰胺)肽。通过该方法能够人工合成抗菌环(甘氨酸‑色氨酸‑亮氨酸‑D‑亮氨酸‑缬氨酸‑天冬酰胺)肽。
摘要（英）：

The invention discloses a method for preparing antibacterial cyclo(glycine-tryptophan-D-leucine-valine-asparaginate) peptide. The method comprises the following steps: 1) performing contact reaction on a substrate resin with Fmoc-Asn (trt)-OH in a solvent so as to obtain a primary resin, performing end capping on the primary resin through methanol, eluting with a Fmoc eluant so as to remove the Fmoc of the primary resin, and performing deprotection with piperidine so as to obtain a secondary resin; 2) performing multiple times of modification reaction on the secondary resin with multiple modified amino acids so as to obtain a third resin; 3) eluting by using a resin eluant so as to obtain resin groups in the third resin and obtain straight-chain hexapeptide of a structure of formula (V) as shown in the specification; 4) in the presence of a solvent, PyAoP, HOAt and DIPEA, performing liquid-phase cyclization reaction on the straight-chain hexapeptide so as to obtain a cyclic product; and 5) eluting with a group eluant so as to remove Boc and Trt on the cyclic product, thereby obtaining the antibacterial cyclo(glycine-tryptophan-D-leucine-valine-asparaginate) peptide. By adopting the method, the antibacterial cyclo(glycine-tryptophan-D-leucine-valine-asparaginate) peptide can be artificially synthesized.

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