专利号:WO-2023030277-A1 优先权日:2021-08-30 标 题:Method for fully liquid-phase synthesis of grnh nonapeptide amide analog 发明人:SUN PENGCHENG; PAN JING; WU JUNYONG; TANG YONGBO; Du Yixiong; GUO LIN 权利人:HUNAN MICRO PEPTIDE BIOMEDICAL CO LTD 摘要:Provided is a method for fully liquid-phase synthesis of a GRnH nonapeptide amide analog, which belongs to the technical field of medicine synthesis. The method comprises respectively synthesizing a 'Trp-Ser-Tyr' fragment, an 'R-Leu' fragment, a 'Pyr-His' fragment and 'Arg-Pro-Hunan T', wherein, R = D-Ala (alarelin), D-Leu (leuprorelin), D-Trp (deslorelin) and D-His (histrelin), and obtaining the GRnH nonapeptide amide analog with high yield and high purity by means of a '3 +2 +2 +2' fragment condensation method. The synthesis method is environmentally friendly, mild, and free of any highly toxic and poisonable reagents. The cost is greatly reduced and the synthesis method is very suitable for large-scale production.
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:WO-9747313-A1 优先权日:1996-06-10 标题:Total synthesis of bacitracin polypetides 发明人:GRIFFIN JOHN H; MCDOUGAL PATRICK G 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Methods for the total synthesis of bacitracin-type polypeptides are described, as well as useful analogs of bacitracin A, and treatment of bacterial infection using such analogs.
专利号:US-2023220001-A1 优先权日:2020-06-09 标 题:Method for synthesis of thioether-containing peptides 发明人:GRUSS HENDRIK; LUTZ CHRISTIAN; SÜSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI 权利人:HEIDELBERG PHARMA RES GMBH 摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.
专利号:US-8828938-B2 优先权日:2009-04-24 标 题:Method for the manufacture of degarelix 发明人:ZHANG HAIXIANG; FOMSGAARD JENS; STAERKAER GUNNAR 权利人:POLYPEPTIDE LABORATORIES AS 摘要:In a step-wise synthesis of degarelix comprising 0.3% by weight or less of 4-([2-(5-hydantoyl)]acetylamino)-phenylalanine analog on (solid support)-NH 2 a step comprises providing a solution of an amino acid or peptide of which the α-amino group is protected by Fmoc; contacting the support with the solution in the presence of reagent for forming a peptide bond between a carboxyl group of the amino acid or peptide and (solid support)-NH 2 ; removing Fmoc by contacting the support with an organic base, in particular piperidine, in an organic solvent. Also disclosed is degarelix of high purity prepared by the method of the invention and the use of Fmoc in the synthesis of degarelix.
专利号:US-2024199685-A1 优先权日:2022-12-15 标 题 :Preparation method of setmelanotide by cyclization of disulfide bond in solid phase 发明人:HSU YAO-LUNG; LEE CHUN-I; LIN CHUN-LING; HUANG YA-LING; LEE JIA-CHUN 权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD 摘要:The present disclosure provides a preparation method of setmelanotide by cyclization of a disulfide bond in a solid phase. By using different solvents or mixed solvents to carry out a cyclization reaction in a solid phase, the reaction concentration can be greatly increased in comparison with a cyclization reaction in a liquid phase, and the production of impurities can also be reduced, so that the effects of reducing the use of the solvents and increasing the production capacity are achieved.