专利号:US-7435791-B2 优先权日:2001-07-19 标题:Process for rapid solution synthesis of peptides 发明人:EGGEN IVO FRANCI; TEN KORTENAAR PAULUS BERNARDUS; HAASNOOT CORNELIS ALBERT GRUSON 权利人:ORGANON NV 摘要:The present invention relates to a process for rapid solution synthesis of a peptide, the process comprising repetitive cycles of steps (a)-(d):n (a) a coupling step, using an excess of an activated carboxylic component to acylate an amino component, (b) a quenching step in which a scavenger is used to remove residual activated carboxylic functions, wherein the scavenger may also be used for deprotection of the growing peptide, (c) one or more aqueous extractions and optionally, (d) a separate deprotection step, followed by one or more aqueous extractions, characterised in that the process comprises at least one step (b), referred to as step (b′), in which an amine or a thiol comprising a free anion or a latent anion is used as a scavenger of residual activated carboxylic functions. nn During the process of this invention the growing peptide need not be isolated until the final peptide sequence has been obtained. n This highly efficient process is useful for the production of oligo- and polypeptides of high purity.
专利号:EP-1071442-B9 优先权日:1998-03-23 标题:Methods and compositions for peptide synthesis (t-20) 发明人:KANG MYUNG-CHOL; BRAY BRIAN; LICHTY MAYNARD; MADER CATHERINE; MERUTKA GENE 权利人:TRIMERIS INC 摘要:The present invention relates, first, to methods for the synthesis of peptides, in particular T-20 (also referred to as 'DP-178'; SEQ ID NO:1) and T-20-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides of interest (e.g., T-20). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full length T-20 and T-20-like peptides.
专利号:US-6281331-B1 优先权日:1998-03-23 标 题 :Methods and compositions for peptide synthesis 发明人:KANG MYUNG-CHOL; BRAY BRIAN; LICHTY MAYNARD; MADER CATHERINE 权利人:TRIMERIS INC 摘要:The present invention relates, first, to methods for the synthesis of peptides, in particular T-20 (also referred to as 'DP-178'; SEQ ID NO:1) and T-20-like peptides. Such methods utilize solid and liquid phase synthesis procedures to synthesize and combine groups of specific peptide fragments to yield the peptide of interest. The present invention further relates to individual peptide fragments which act as intermediates in the synthesis of the peptides of interest (e.g., T-20). The present invention still further relates to groups of such peptide intermediate fragments which can be utilized together to produce full length T-20 and T-20-like peptides.
专利号:US-7414106-B2 优先权日:2003-06-19 标 题 :Synthesis of peptide α-thioesters 发明人:CAMARERO JULIO A; MITCHELL ALEXANDER R; DE YOREO JAMES J 权利人:L LIVERMORE NAT SECURITY LLC 摘要:Disclosed herein is a new method for the solid phase peptide synthesis (SPPS) of C-terminal peptide α thioesters using Fmoc/t-Bu chemistry. This method is based on the use of an aryl hydrazine linker, which is totally stable to conditions required for Fmoc-SPPS. When the peptide synthesis has been completed, activation of the linker is achieved by mild oxidation. The oxidation step converts the acyl-hydrazine group into a highly reactive acyl-diazene intermediate which reacts with an α-amino acid alkylthioester (H-AA-SR) to yield the corresponding peptide α-thioester in good yield. A variety of peptide thioesters, cyclic peptides and a fully functional Src homology 3 (SH3) protein domain have been successfully prepared.
专利号:US-2022098155-A1 优先权日:2018-11-14 标 题 :Novel pathway for the synthesis of diazirines, that may or may not be enriched in nitrogen-15 发明人:REBOUL VINCENT; FRANCK XAVIER; GLACHET THOMAS; MARZAG HAMID 权利人:UNIV ROUEN NORMANDIE; UNIV CAEN; INSTITUT NAT DES SCIENCES APPLIQUEES DE ROUEN INSA; CENTRE NAT RECH SCIENT; ECOLE NAT SUPERIEURE DINGENIEURS DE CAEN 摘要:The present invention concerns a novel method for synthesising diazirines, that may or may not be enriched in nitro-gen-15, from amino acids or imines, via a one-pot synthesis method, comprising the reaction of the starting amino acid or imine with ammonia, which may or may not be enriched in nitrogen-15, and a hypervalent iodine oxidant. The present invention also relates to a method for synthesising ammonia enriched in nitrogen-15. The invention also concerns certain diazirines of formula (I) likely to be obtained by the claimed synthesis method, and also refers to the 15 N 2 -diazirines of formula (I′). The claimed diazirines can be used in photoaffinity labelling. The 15 N 2 -diazirines can also be used in hyperpolarisation, in particular in the medical imaging field.
专利号:US-8178474-B1 优先权日:1999-04-21 标题 :Functionalised solid support for alpha-oxoaldehyde synthesis 发明人:MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE 权利人:MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE; PASTEUR INSTITUT; CENTRE NAT RECH SCIENT 摘要:The invention relates to a functionalised solid support for the synthesis of compounds comprising at least one α-oxoaldehyde function, to a process for preparing it and to its applications, in particular for the preparation of a library of organic compounds, of a diagnostic reagent, of a microtitration plate and of a biochip, such as a DNA chip. The present invention also relates to a process for the synthesis of organic compounds comprising at least one α-oxoaldehyde function and to the α-oxoaldehyde peptides obtained using this process.