KR900004761A - Solid phase peptide synthesis - Google Patents

Abstract

No content

Description

Solid phase peptide synthesis

Since this is an open matter, no full text was included.

Claims (6)

Attaching the primary amino acid residue to the polyacrylic resin, coupling the one or more additional amino acid residues to produce the desired peptide, and separating the peptide from the resin, and the water and / or aqueous solution in the coupling scheme. Solid phase peptide synthesis method comprising the step of washing the resin in (s). The method according to claim 1, wherein the polyacrylic resin is a copolymer of three monomers as follows. i) providing a parent of a copolymer, wherein the first monomer 1- (meth) acryloyl-pyrrolidine, 1- (meth) acryloyl-piperidine, 1- (meth) acrylo Mono-perhydroazepine, 1- (meth) acryloyl-4-methyl-piperazine, 4- (meth) acryloyl-morpholine, N, N-dimethyl- (meth) acrylamide and N, A second monomer which crosslinks N-diethyl- (meth) acryloamide ii) copolymer and is any of the following. N, N'-di (meth) acryloyl-diaminomethane and N, N-di (methyl) acryloyl-1,2-diaminoethane and iii) copolymers are activated and any of the following acids Tertiary monomer, which is a methyl ester of any of these acids. 2- (meth) acrylamido-acetic acid, 3- (meth) acrylamido-propionic acid, 4- (meth) acrylamido-butyric acid, 6- (meth) acrylamido-hexanoic acid, N- ( Meth) acryloyl-L-alanine, N- (meth) acryloyl-L-valine, N- (meth) acryloyl-L-leucine, N- (meth) acryloyl-L-phenylalanine, N -(Meth) acryloyl-L-tyrosine, N- (meth) acryloyl-L-methionine, N- (meth) acryloyl-L-lysine and N- (meth) acryloyl-L-proline . The method according to claim 1, wherein the polyacrylic resin is a copolymer according to claim 2 amidated with ethylene diamine. The method according to any preceding claim, wherein the N-protecting group used for amino acid coupling is Boc and the coupling scheme is as follows: 1.-wash: distilled water-2-4 times every 2 minutes, 2.- Deprotection: HCI (6N) in water 1 time 2 minutes again 1 time 30 minutes, 3-wash: distilled water-4-6 times every 2 minutes, 4-neutralization: borate buffer 1 of 2.5 mM PH 8.5-9.0 Equivalent, 1 to 2 minutes once and again 1 to 2 minutes, 5. -Washing: distilled water-4 to 6 times every 1 to 2 minutes, 6-Washing: DMF-2 times every 1 to 2 minutes, 7. -Coupling: symmetric anhydride (2 equiv, twice in DMF), 8.-wash: DMF or NMP- twice every two minutes and 9.- wash: distilled water four times every two minutes. The method according to any one of claims 1 to 3, wherein the N-protecting group used for amino acid coupling is Fmoc, and the coupling scheme is as follows. .1-wash: distilled water-4 to 6 times every 2 minutes, 2.-deprotection: piperidine or diethylamine dissolved in water, 3-wash: isopropanol, 2 times every 2 minutes, distilled water-every 2 minutes 4 to 6 times, 4.-Randomly washed: once for 2 minutes with DMF, 5.-Coupling: symmetric anhydride (3 times in excess in DMF) and 6.-washing: DMF (2 times every 2 minutes), distilled water- 6 times every 2 minutes. A method as substantially described herein with respect to any of the examples. ※ Note: The disclosure is based on the initial application.