CAS: 187618-60-6; Fmoc-D-Arg(Pbf)-Oh

相似化合物

154445-77-9 200124-22-7 200115-86-2

上下游产品

(fluorenylmethoxy)carbonyl chloride N-(9H-fluoren-2-ylmethoxycarbonyloxy)succinimideFm°C-L-Arg-OH

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-2020247841-A1
优先权日:2017-09-27
标 题 :Synthesis of icatibant
发明人：RAMU VASANTHAKUMAR GANGA; PATIL NITIN SOPANRAO; PALLE VENTAKA RAGHAVENDRACHARYUL; Yogesha
权利人:BIOCON LTD
摘要:The present invention relates to the efficient solid-phase synthesis of Icatibant represented by Formula (I). The present invention relates to an efficient process for the preparation of Icatibant by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare Icatibant. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to ensure complete removal of piperidine and reactions are going for completion, and thus avoid addition/deletion sequences and also improve the process yield.

专利号:EP-3875466-A1
优先权日:2020-03-05
标 题 :Process for the synthesis of etelcalcetide
发明人：MARTELLI GIULIA; CABRI WALTER; FERRAZZANO LUCIA; VIOLA ANGELO; TOLOMELLI ALESSANDRA; RICCI ANTONIO
权利人:FRESENIUS KABI IPSUM S R L; ALMA MATER STUDIORUM UNIV OF BOLOGNA
摘要:The present invention provides a manufacturing process for etelcalcetide through direct disulfide bond formation with N-chlorosuccinimide in high yield and high purity.

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:US-11420997-B2
优先权日:2018-04-13
标题:Peptide synthesis method
发明人：SUZUKI HIDEAKI; MUTO SUSUMU; FUJITA SHUJI; KUBO DAISUKE
权利人:JITSUBO CO LTD
摘要:The present invention has an object of shortening the process time and reducing use of a poor solvent for solidifying a carrier (Tag)-peptide component, by removing impurities without conducting solid-liquid separation (condensation, solid-liquid separation and drying operation) of a Tag-peptide component, in an Fmoc method using a Tag for liquid phase peptide synthesis. Provided is the peptide synthesis method that includes the following steps a-d: step a: a carrier-protected amino acid, carrier-protected peptide, or a carrier-protected amino acid amide, and an N-Fmoc-protected amino acid or an N-Fmoc-protected peptide are condensed in an organic solvent or a mixed solution of organic solvents, to obtain an N-Fmoc-carrier-protected peptide, step b: a water-soluble amine is added to the reaction solution after the condensation reaction, step c: the Fmoc group is deprotected from the protected amino group in the presence of a water-soluble amine, and step d: the reaction solution is neutralized by adding an acid, and further, by adding and washing with an acidic aqueous solution, then, by liquid-liquid separation an aqueous layer is removed to obtain an organic layer.

专利号:US-2024209034-A1
优先权日:2021-04-12
标题:Engineering peptides for a a vb6 integrin binding and related methods of use and synthesis
发明人：SELLERS DREW; CARDLE IAN; PUN SUZIE HWANG
权利人:UNIV WASHINGTON; SEATTLE CHILDRENS HOSPITAL D/B/A SEATTLE CHILDRENS RES INSTITUTE
摘要:Embodiments of the claimed invention are directed to synthetic peptides comprising an amino acid sequence of X 1 X 2 VX 3 NLRGDLQVLX 4 QKVCX 5 T (SEQ ID NO:18), wherein at least one of X 1 and X 2 is a cysteine, and wherein one or more of X 3 , X 4 , and X 5 is a non-natural amino acid. Also described are methods of using the claimed embodiments for inhibiting growth of a cancer cell overexpressing integrin αvβ6. Additionally, also described are methods of using the claimed embodiments for detecting a cancer cell overexpressing integrin αvβ6.