专利号:US-2024067694-A1 优先权日:2021-01-04 标 题:Synthesis of teduglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
专利号:US-2018265547-A1 优先权日:2014-07-18 标 题 :Z-selective olefin metathesis of peptides 发明人:MANGOLD SHANE L; GRUBBS ROBERT H 权利人:CALIFORNIA INST OF TECHN 摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.
专利号:EP-1960423-B1 优先权日:2004-12-30 标 题:Synthesis of peptide t-20 using peptide intermediate fragments 发明人:HAN YEUN-KWEI; JOHNSTON DAVID A; KHATRI HIRALAL N 权利人:HOFFMANN LA ROCHE 摘要:Methods for the solid phase synthesis of T-20 peptides and peptide intermediates, in particular methods involving synthesizing T-20 peptide intermediates at low loading factors to produce products having excellent purity and yield.
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-11518794-B2 优先权日:2016-08-19 标 题:Synthesis method for liraglutide with low racemate impurity 发明人:FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG 权利人:SHENZHEN JYMED TECH CO LTD 摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.
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.
参考标题:Mild Oxidative Cleavage Of 9-Bbn-Protected Amino Acid Derivatives 作者:Tobias Ankner,Thomas Norberg,Jan Kihlberg |发布日期:2015.6 摘要:Protection Of The Amino Acid Moiety Using 9-Bbn Is An Effective Method To Enable Side Chain Manipulations In Synthesis Of Complex Amino Acids. We Investigated The Standard, Mild Method For Deprotection Of The 9-Bbn Group In Methanolic Chloroform, And Found That It Relies On A Slow Oxidation Mediated By Molecular Oxygen. Building On This Insight, We Have Developed A Method That Allows For A Fast And
合成参考文献
摘要:Meuleman, T. J.; Liskamp, R. M. J., Science of Synthesis, (2021) , 46. 参考文献:10.1007/978-1-4939-2978-8_1 摘要:Fauvet B, Lashuel HA. Semisynthesis and Enzymatic Preparation of Post-translationally Modified α-Synuclein. Methods Mol Biol. 2016;1345():3–20. doi: 10.1007/978-1-4939-2978-8_1.