专利号:US-2025188118-A1 优先权日:2023-12-06 标题:Liquid phase peptide synthesis methods 发明人:BAUCOM KYLE; GLADFELDER JOSHUA; TURMAN NOLAN 权利人:AMGEN INC 摘要:Disclosed herein are methods of producing peptides, including liquid phase peptide synthesis methods in which one or more cycles of peptide elongation are performed in one pot. In particular, the present disclosure provides liquid phase peptide synthesis methods employing solvent systems comprising 2-methyltetrahydrofuran for condensation reactions, as well as convergent liquid phase peptide assembly methods in which benzyl alcohol anchor groups are selectively removed from an N-protected C-protected peptide by base-catalyzed ester hydrolysis.
专利号:WO-2023287345-A1 优先权日:2021-07-16 标 题 :Aqueous solid phase peptide synthesis 发明人:PAWLAS JAN; LUDEMANN-HOMBOURGER OLIVIER 权利人:POLYPEPTIDE LABORATORIES HOLDING PPL AB 摘要:The present invention relates to a solid phase peptide synthesis (SPPS) where the coupling of amino acids is performed in an aqueous solution comprising at least one organic co-solvent miscible with water. The aqueous solution is capable of sufficiently solubilize the activated Fmoc-α-amine protected amino acid or activated Fmoc-α-amine protected peptide fragment, and where the resin is capable of swelling in the presence of the aqueous solution above about 4 mLg-1. The invention also encompasses a method for regeneration of spent aqueous solution from the SPPS.
专利号:CN-115109118-A 优先权日:2021-03-19 标 题:A kind of method for solid-phase synthesis of DS-8201 intermediate and preparation method of DS-8201
专利号:CN-115073587-A 优先权日:2022-07-08 标 题 :A kind of synthetic process of semi-continuous liquid phase synthesis of bivalirudin
专利号:US-2017029467-A1 优先权日:2015-07-30 标 题:Method of producing bivalirudin 发明人:ZHANG GUOQING; ZHANG RUOPING; BAI JUNCAI 权利人:AMBIOPHARM INC 摘要:The present disclosure provides a method of producing bivalirudin using a peptide fragment or peptide fragments on solid phase peptide synthesis that minimizes, or eliminates, the production of bivalirudin molecules having too few or too many glycine residues.
专利号:US-5202418-A 优先权日:1990-02-02 标题 :Method of performing multiple synthesis of peptides on solid carrier
[参考文献]: Beck A, Et Al. Strategies And Challenges For The Next Generation Of Antibody-Drug Conjugates. Nat Rev Drug Discov. 2017 May;16(5):315-337.
合成参考文献
参考文献:10.1007/s10967-026-10736-z 摘要:Mao Y, Zhou P, Jiang J, Liu Y, Wang H, Han G, Wu J, Zou P, Lu C. Synthesis and preliminary evaluation of a 99mTc-labeled bivalent radiotracer targeting PD-L1. J Radioanal Nucl Chem. 2026 Jan;335(1):385–95. doi: 10.1007/s10967-026-10736-z.