CAS: 138775-22-1; Fmoc-N-Me-Ile-Oh

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N-Fmoc-N-Methyl-L-Isoleucine Benzhydryl Ester置于三氟乙酸体系中,用 二氯甲烷,甲苯 用作溶剂,化学反应 1.0H,以98%的收率获得fmoc-N-甲基-L-异亮氨酸
参考文献:N-Fmoc-N-甲基-α-氨基酸和n-糖基-N-甲基-α-氨基酸的制备
标题:N-Fmoc-N-甲基-α-氨基酸和n-糖基-N-甲基-α-氨基酸的制备
摘要:亲脂性n-Fmoc-N-甲基-α-氨基酸和n-糖基-N-甲基-α-氨基酸(用于制备n-甲基化肽的有趣结构单元)的合成简便途径是提出了.Nosyl和fmoc保护的单体都是可及的,因此这些化合物可用于溶液以及固相肽合成中.该方法是基于使用苯甲基来暂时保护n-糖基-α-氨基酸的羧基功能以及随后n的甲基化-重氮基的-Nosyl-α-氨基酸二苯甲基酯.苯甲基酯具有几个有益的特征,例如制备简单,对甲基化的稳定性以及在温和条件下的选择性脱保护.整个过程非常有效,因为所采用的条件保持了氨基酸前体的手性完整性,并且该过程不需要对甲基化产物进行色谱纯化.
Doi:10.1007/s00726-008-0221-8

专利信息

专利号:US-2023391818-A1
优先权日:2020-11-05
标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation
发明人：NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.

专利号:US-2024124517-A1
优先权日:2020-12-25
标题:Method for producing peptide compound containing n-substituted-amino acid residue
发明人：MORITA YUYA; NOMURA KENICHI
权利人:CHUGAI PHARMACEUTICAL CO LTD
摘要:An object of the present invention is to provide a method for efficiently producing a high-purity peptide compound with a high yield. It has been found that the object can be achieved by supporting a peptide on a solid phase synthesis resin prior to a first elongation reaction in a solid phase process.