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    • 1. 发明授权
    • Solid phase Fmoc chemistry process to prepare peptides
    • 固相Fmoc化学过程制备肽
    • US07897724B2
    • 2011-03-01
    • US11729047
    • 2007-03-27
    • Divya Lal SaksenaShrikant MishraChandrakesan MuralidharanNilesh PatilNikhil Umesh MoheMandar Ravindra Maduskar
    • Divya Lal SaksenaShrikant MishraChandrakesan MuralidharanNilesh PatilNikhil Umesh MoheMandar Ravindra Maduskar
    • C07K1/06
    • C07K14/75C07K14/78Y02P20/582
    • The present invention relates to an improved process for the preparation of N6-(aminoiminomethyl)-N2-(3-mercapto-1-oxopropyl)-L-lysylglycyl-L-α-aspartyl-L-tryptophyl-L-prolyl-L-cysteinamide, cyclic(1→6)-disulfide of formula (1), which involves assembling a peptide chain comprising of six amino acids and a thioalkyl carboxylic acid in a required sequence on a solid support to obtain a peptide bound resin of formula (2), capping the free amino groups after each coupling, cleaving Dde group in the peptide of formula (2) from the solid support to obtain peptide-solid support of formula (3), guanylating the peptide of formula (3) at ε-lysine-NH2 in an organic solvent to obtain peptide-solid support of formula (4), cleaving and deprotecting all groups in the peptide of formula (4) from the solid support to obtain peptide-amide formula (5), oxidizing the SH-peptide of formula (5) with an appropriate oxidizing agent to obtain the crude peptide-amide of formula (1) and purifying the crude peptide-amide of formula (1) by chromatographic technique. The solid support is either resin or a cellulose support like cotton, gauze, fabric, paper and perloza beads. The described process is simple, easy, environment friendly, takes lesser time and more cost effective.
    • 本发明涉及一种制备N6-(氨基亚氨基甲基)-N2-(3-巯基-1-氧代丙基)-L-赖氨酰甘氨酰-L-α-天冬氨酰-L-色氨酰-L-脯氨酰基-L- 半胱氨酰胺,式(1)的环状(1→6) - 二硫化物,其包括在固体支持物上以所需的顺序将包含六个氨基酸的肽链和硫代烷基羧酸组装以获得式(2)的肽结合树脂 ),在每次偶联后封端游离氨基,从固体支持物切割式(2)的肽中的Dde基团以获得式(3)的肽 - 固体支持物,在式(3)的肽上进行脒化, 赖氨酸-NH 2在有机溶剂中得到式(4)的肽固体支持物,从固体支持物中切割和脱保护基团中所有基团的肽,得到肽 - 酰胺式(5),氧化SH- 式(5)的肽与适当的氧化剂反应,得到式(1)的粗肽 - 酰胺并纯化粗蛋白 e通过色谱技术制备式(1)的肽 - 酰胺。 固体支持物是树脂或纤维素载体,如棉,纱布,织物,纸和perloza珠。 描述的过程简单,容易,环保,花费更少的时间和更具成本效益。