专利号:US-2023331778-A1 优先权日:2020-08-31 标 题 :An improved process for fmoc synthesis of etelcalcetide 发明人:LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN; CHAVRE PRAFUL SHAMRAO 权利人:USV PRIVATE LTD 摘要:The present invention relates to an improved process for the synthesis of Etelcalcetide and its analogs by solid phase synthesis of Fmoc protected amino acids in a sequential manner, followed by acetylation of terminal D-cys and cleavage of peptide from solid support. The crude heptapeptide thus obtained is reduced using Tris(2-carboxyethyl) phosphine hydrochloride, purified and oxidized with L-cysteine. The oxidized Etelcalcetide is purified and salt exchanged using a one-step reverse phase chromatography process. The purified Etelcalcetide hydrochloride is then precipitated using organic solvents, concentrated and lyophilized to purity of greater than 99.0%.
专利号:CN-106928321-B 优先权日:2015-12-31 标题:A method of synthesis Etelcalcetide
专利号:CN-114524860-A 优先权日:2021-12-29 标 题:Synthesis method and application of Etelcalcetide
参考标题:Submonomeric Strategy With Minimal Protection For The Synthesis Of C(2)-Modified Peptide Nucleic Acids 作者:Stefano Volpi,Andrea Rozzi,Nicola Rivi,Martina Neri,Wolfgang Knoll,Roberto Corradini |发布日期:2021.2.5 摘要:A Novel Synthesis Of C(2)-Modified Peptide Nucleic Acids (Pnas) Is Proposed, Using A Submonomeric Strategy With Minimally Protected Building Blocks, Which Allowed A Reduction In The Required Synthetic Steps. N(3)-Unprotected, D-Lys- And D-Arg-Based Backbones Were Used To Obtain Positively Charged Pnas With High Optical Purity, As Inferred From Chiral Gc Measurements. "Chiral-Box" Pnas Targeting The