专利号:US-2004038331-A1 优先权日:2002-08-23 标题:Solid phase synthesis of biomolecule conjugates 发明人:REDDY M PARAMESWARA; FAROOQUI FIRDOUS; BRILLHART KURT L 摘要:Processes for the solid state phase formation synthesis of biomolecule conjugates, particularly protein-oligonucleotide conjugates are shown. One of the protein or oligonucleotide is reversibly bound to a solid substrate phase. At least one portion of each of the protein and the oligonucleotide molecules is activated with complementary activation groups. The activated protein and the activated oligonucleotide are then reacted, in a buffered solution resulting in the formation of the desired conjugate which remains reversibly bound to the substrate. The nature of the buffered solution is then modified causing the conjugate to be released from the substrate solid phase.
专利号:US-2024024489-A1 优先权日:2020-11-20 标 题:Protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof 发明人:MULARD LAURENCE; DHARA DEBASHIS; PFISTER HELENE; PAOLETTI JULIE; PHALIPON ARMELLE; GUERREIRO-INVERNO CATHERINE 权利人:PASTEUR INSTITUT 摘要:The present invention provides zwitterionic oligosaccharides, in particular fragments of the surface polysaccharides from Shigella sonnei and Shigella sonnei conjugates comprising them. The present invention also provides protected disaccharides, their process of preparation and their use in the synthesis of zwitterionic oligosaccharides, and conjugates thereof, the disaccharide repeating unit of Shigella sonnei being: (I)
专利号:US-9126896-B2 优先权日:2012-06-01 标题:Synthesis of diamido gellants by using Dane salts of amino acids 发明人:BINDL MARTIN; HERRMANN ROLAND; KNAUP GUNTER 权利人:EVONIK INDUSTRIES AG 摘要:The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a Dane salt according to formula II and a Dane salt according to formula III with a coupling reagent; b) adding a diamine according to formula IV to the reaction mixture; and c) adding an acid to the reaction mixture to adjust the pH value of the reaction to <7; wherein L represents a C 2 -C 20 alkyl group, a C 6 -C 20 aryl group, or a C 7 -C 20 alkylaryl group; R 1 and R 2 can be identical or different and represent a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 hydroxyalkyl group, a C 1 -C 4 thioether group, a C 6 -C 20 aryl group, a C 7 -C 20 alkylaryl group, a C 7 -C 20 alkylhydroxyaryl group, a C 4 -C 20 alkylheteroaryl group with 1 to 4 heteroatoms; or a C 1 -C 4 alkylcarboxylic moiety, which may be an acid, an amide, or which may be esterified with a C 1 -C 6 alkyl group or a C 7 -C 20 alkylaryl group; R 3 represents a C 1 -C 4 alkyl group; R 4 represents a hydrogen atom, or a C 1 -C 4 alkyl group; R 5 represents a C 1 -C 4 alkyl group; and X represents an alkali metal.
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-9126897-B2 优先权日:2012-06-01 标 题 :Synthesis of diamido gellants by using amino acid N-carboxyanhydrides 发明人:BINDL MARTIN; HERRMANN ROLAND; KNAUP GUNTER 权利人:EVONIK INDUSTRIES AG 摘要:The invention relates to a method for the synthesis of a compound according to formula I comprising the following steps: a) reacting a N-carboxyanhydride according to formula II and a N-carboxy-anhydride according to formula III with a diamine according to formula IV and b) adding an acid to the reaction to adjust the pH value of the reaction to <7; wherein L represents a C 2 -C 20 alkyl group, a C 6 -C 20 aryl group, or a C 7 -C 20 alkylaryl group; and R 1 and R 2 can be identical or different and represent a hydrogen atom, a C 1 -C 4 alkyl group, a C 1 -C 4 hydroxyalkyl group, a C 1 -C 4 thioether group, a C 6 -C 20 aryl group, a C 7 -C 20 alkylaryl group, a C 7 -C 20 alkylhydroxyaryl group, a C 4 -C 20 alkylheteroaryl group with 1 to 4 heteroatoms; or a C 1 -C 4 alkylcarboxylic moiety, which may be an acid, an amide, or which may be esterified with a C 1 -C 6 alkyl group or a C 7 -C 20 alkylaryl group.
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.
[参考文献]: Michal Ejgenberg, Et Al. Conglomerate Crystallization On Self-Assembled Monolayers. Chem Commun (Camb). 2011 Nov 28;47(44):12161-3. [参考文献]: Yuan Jiang, Et Al. The Existence Region And Composition Of A Polymer-Induced Liquid Precursor Phase For Dl-Glutamic Acid Crystals. Phys Chem Chem Phys. 2012 Jan 14;14(2):914-9.
合成参考文献
参考文献:10.1007/s00411-019-00808-y 摘要:Beshir WB, Soliman YS, Abdel-Fattah AA, Fahim RA. A new EPR dosimeter based on glutamic acid for radiation processing application. Radiation and Environmental Biophysics. 2019 Jul 08;58(4):501–11. doi: 10.1007/s00411-019-00808-y.