Invention Grant
- Patent Title: Solid phase Fmoc chemistry process to prepare peptides
- Patent Title (中): 固相Fmoc化学过程制备肽
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Application No.: US11729047Application Date: 2007-03-27
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Publication No.: US07897724B2Publication Date: 2011-03-01
- Inventor: Divya Lal Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Nilesh Patil , Nikhil Umesh Mohe , Mandar Ravindra Maduskar
- Applicant: Divya Lal Saksena , Shrikant Mishra , Chandrakesan Muralidharan , Nilesh Patil , Nikhil Umesh Mohe , Mandar Ravindra Maduskar
- Applicant Address: IN Mumbai
- Assignee: USV, Ltd.
- Current Assignee: USV, Ltd.
- Current Assignee Address: IN Mumbai
- Agency: Pharmaceutical Patent Atty's LLC
- Main IPC: C07K1/06
- IPC: C07K1/06

Abstract:
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.
Public/Granted literature
- US20070249806A1 Solid phase Fmoc chemistry process to prepare peptides Public/Granted day:2007-10-25
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