专利号:US-4704450-A 优先权日:1983-02-21 标 题 :Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides 发明人:DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY 权利人:SANOFI SA 摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
专利号:US-4581168-A 优先权日:1983-02-21 标题:Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides 发明人:DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY 权利人:SANOFI SA 摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-4871670-A 优先权日:1982-08-12 标题 :Molecular cloning and characterization of a gene sequence coding for human relaxin 发明人:HUDSON PETER J; SHINE JOHN; NIALL HUGH D; TREGEAR GEOFFREY W 权利人:FLOREY HOWARD INST 摘要:Genes and DNA transfer vectors for the expression of human preprorelaxin; sub-units thereof, including genes and transfer vectors for expression of human prorelaxin and the individual A, B and C peptide chains thereof; and equivalents of all such genes. Methods for synthesis of the peptides involving recombinant DNA techniques.
专利号:US-3725380-A 优先权日:1969-04-05 标 题:Method of synthesizing peptides in the presence of a carbodiimide and a 1-hydroxy-benzotriazole 发明人:KONIG W; GEIGER R 权利人:HOECHST AG 摘要:Improved synthesis of peptides by the carbodiimide method in which an amino-protected amino acid or peptide having a reactive carboxy group is condensed with a carboxy-protected amino acid or peptide having a reactive amino group in the presence of a 1hydroxy-benzotriazole or a substituted 1-hydroxy-benzotriazole of the formula AS WELL AS IN THE PRESENCE OF A CARBODIIMIDE SUCH AS DICYCLOHEXYL CARBODIIMIDE.
专利号:US-4801721-A 优先权日:1984-08-16 标题 :Stereospecific synthesis of carboxyalkyl peptides 发明人:RYAN JAMES W; CHUNG ALFRED 权利人:RYAN JAMES W; CHUNG ALFRED 摘要:Methods for the alkylation of substituted amines with trifluorate esters is disclosed.
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合成参考文献
参考文献:10.1007/978-1-60327-299-5_24 摘要:Fields GB. Using fluorogenic peptide substrates to assay matrix metalloproteinases. Methods Mol Biol. 2010;622():393–433. doi: 10.1007/978-1-60327-299-5_24.