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    • 3. 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。
    • 4. 发明申请
    • Solid phase Fmoc chemistry process to prepare peptides
    • 固相Fmoc化学过程制备肽
    • US20070249806A1
    • 2007-10-25
    • US11729047
    • 2007-03-27
    • Divya SaksenaShrikant MishraChandrakesan MuralidharanNilesh PatilNikhil MoheMandar Maduskar
    • Divya SaksenaShrikant MishraChandrakesan MuralidharanNilesh PatilNikhil MoheMandar Maduskar
    • C07K7/60C07K7/06
    • 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(16)-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N 6 - (氨基亚氨基甲基)-N 2 - (3-巯基-1-氧代丙基)-L-赖氨酰甘氨酰基 - L-α-天冬氨酰基-L-色氨酰-L-脯氨酰基-L-半胱氨酰胺,式(1)的环状(16) - 二硫化物,其包括以所需顺序组装包含六个氨基酸的肽链和硫代烷基羧酸 在固体支持物上获得式(2)的肽结合树脂,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 ),在有机溶剂中在ε-赖氨酸-NH 2上对式(3)的肽进行脒化,得到式(4)的肽固体支持物,将式(4)的肽中的所有基团切割和脱保护 (4)从固体支持物得到肽 - 酰胺配方(5),用合适的氧化剂氧化式(5)的SH-肽,得到粗肽 - 酰胺 通过色谱技术纯化式(1)的粗肽酰胺。 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
    • 7. 发明申请
    • Process for the Preparation of Peptides
    • 肽的制备方法
    • US20080182781A1
    • 2008-07-31
    • US10592118
    • 2004-10-10
    • Divya SaksenaShrikant MishraChandrakesan MuralidharanMilind ThakareNilesh PatilAruna Khare
    • Divya SaksenaShrikant MishraChandrakesan MuralidharanMilind ThakareNilesh PatilAruna Khare
    • A61K38/12C07K7/64C07K7/06
    • C07K7/06Y02P20/55
    • 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 amino acid residues and a thioalkyl carboxylic acid with appropriate protecting groups on a solid phase resin, cleaving the peptide thus obtained from the resin with concomitant removal of side chain protecting groups except Acm protecting group of thiol moiety to obtain peptide amide of formula (3), converting lysine residue of peptide amide of formula (3) having protected thiol group to homoarginine residue by guanylation to obtain peptide of formula (4), preparing silver peptide of formula (5), followed by simultaneous deprotection, obtaining silver peptide of formula (5) and oxidation of silver peptide to obtain crude peptide amide comprising compound of formula (1) and finally subjecting to chromatographic purification. The described process is simple, easy, environment friendly and cost effective.
    • 本发明涉及一种制备N 6 - (氨基亚氨基甲基)-N 2 - (3-巯基-1-氧代丙基-L-赖氨酰甘氨酰-L- -α-天冬氨酰基-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,其包括将氨基酸残基和硫代烷基羧酸与固体上适当的保护基团组装 通过除去除巯基部分的Acm保护基之外的侧链保护基除去由树脂得到的肽,从而得到式(3)的肽酰胺,转化具有被保护的硫醇的式(3)的肽酰胺的赖氨酸残基 通过胍基化得到高精氨酸残基,得到式(4)的肽,制备式(5)的银肽,然后同时去保护,得到式(5)的银肽和银肽的氧化,得到粗肽酰胺, 式(1),最后进行色谱 c净化。 描述的过程简单,容易,环保,成本效益高。