CAS: 1334237-71-6; S-(((S)-2-Acetamido-3-(((R)-1-(((R)-1-(((R)-1-(((R)-1-(((R)-1-(((R)-1-Amino-5-Guanidino-1-Oxopentan-2-yl)Amino)-1-Oxopropan-2-yl)Amino)-5-Guanidino-1-Oxopentan-2-yl)Amino)-5-Guanidino-1-Oxopentan-2-yl)Amino)-5-Guanidino-1-Oxopentan-2-yl)Amino)-1-Oxopropan

维拉卡肽置于盐酸,氯化铵体系中,用 水 用作溶剂,化学反应生成维考西肽盐酸盐
参考文献: An Improved Process For The Preparation Of Etelcalcetide Hydrochloride[fr] Procédé Amélioré Pour La Préparation De Chlorhydrate D'ételcalcétide
标题: An Improved Process For The Preparation Of Etelcalcetide Hydrochloride[fr] Procédé Amélioré Pour La Préparation De Chlorhydrate D'ételcalcétide
摘要:本发明涉及一种改进的制备etelcalcetide盐酸盐的方法,其化学式为(I):本发明还提供了一种制备etelcalcetide乙酸盐的方法,其化学式为(Vi),该方法是etelcalcetide盐酸盐的中间体:化学式(Vi).

专利信息

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:US-10899791-B2
优先权日:2017-10-03
标题 :Method for synthesizing etelcalcetide or salts thereof
发明人：LEE KWANG-CHUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; KAO CHIA-SUI; HUANG YA-LING; WANG WEI-SSU
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present invention provides a method for synthesizing etelcalcetide or salts thereof, comprising the steps of: (a) synthesizing the D-amino acids in the formula (I) sequentially by Fmoc solid-phase synthesis, using a solid support as a starting material in solid phase peptide synthesis and sequentially synthesizing a D-form amino acid of formula (I) by Fmoc chemistry; deprotecting Fmoc group and acetylating the amino group to obtain a sequence A comprising protecting groups (PG) in the side chain of D-Cys and D-Arg; (b) removing the protecting group in the side-chain of D-Cys of the sequence A to form a sequence B; (c) disulfide formation at D-Cys of the sequence B by (PG)-L-Cys-OH to obtain a sequence C; (d) using a cleavage solution to remove the protecting groups of the sequence C to give etelcalcetide as formula (I). The present invention can shorten the steps and time for preparing Etelcalcetide.

专利号:WO-2022044030-A1
优先权日:2020-08-31
标 题 :An improved process for fmoc synthesis of etelcalcetide

专利号:EP-4204434-A1
优先权日:2020-08-31
标题 :An improved process for fmoc synthesis of etelcalcetide