专利号:US-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-2022298204-A1 优先权日:2019-07-05 标题 :Synthesis of a-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:EP-3792250-A1 优先权日:2019-09-13 标题:Synthesis of alpha-amanitin and its derivatives 发明人:SIEGERT MARY-ANN; KNITTEL CAROLINE HERTA; SÜSSMUTH RODERICH 权利人:PURE BIOORGANICS SIA 摘要:The present invention relates to the chemical synthesis of α-amanitin and its derivatives. The present invention also relates to intermediate products of the α-amanitin synthesis.
专利号:US-4704450-A 优先权日:1983-02-21 标 题 :Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediate peptides 发明人:DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY 权利人:SANOFI SA 摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group; selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
专利号:US-4515920-A 优先权日:1984-04-30 标题 :Synthesis of peptides and proteins 发明人:ERICKSON BRUCE W 权利人:UNIV ROCKEFELLER 摘要:Solid phase synthesis of peptides and proteins have been improved by the use of a trifunctional segment, one functional group of which is bound to a solid support, the other two functional groups being available as substrates upon which identical proteins are synthesized.
专利号:US-4581168-A 优先权日:1983-02-21 标题:Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides 发明人:DIAZ JOSEPH; DEMARNE HENRI; RONCUCCI ROMEO; SCHMELCK PAUL-HENRY 权利人:SANOFI SA 摘要:The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising:--coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: (a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, (b) the guanidine function of the arginine is protected by protonation, and (c) the N-terminal amino acid is protected on the amine by the Boc group;--selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and--eliminating, at the end of sequence, all the protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.
参考标题:Metagenome‐guided Analogue Synthesis Yields Improved Gram‐negative‐active Albicidin‐ And Cystobactamid‐type Antibiotics 作者:Zongqiang Wang,Amanda Kasper,Rabia Mehmood,Melinda Ternei,Shaogang Li,Joel S. Freundlich,Sean F. Brady |发布日期:2021.10.4 摘要:Products Are A Major Source Of New Antibiotics. Here We Utilize Biosynthetic Instructions Contained Within Metagenome-Derived Congener Biosynthetic Gene Clusters (Bgcs) To Guide The Synthesis Of Improved Antibiotic Analogues. Albicidin And Cystobactamid Are The First Members Of A New Class Of Broad-Spectrum ρ-Aminobenzoic Acid (Paba)-Based Antibiotics. Our Search For Paba-Specific Adenylation Domain Sequences
合成参考文献
参考文献:10.1271/bbb.50621 摘要:HAGINOYA E, HOJO H, NAKAHARA Y, NAKAHARA Y, NABESHIMA K, TOOLE BP, WATANABE Y. Synthesis of a Glycosylated Peptide Thioester by the Boc Strategy and Its Application to Segment Condensation. Bioscience, Biotechnology, and Biochemistry. 2006 Jun 23;70(6):1338–49. doi: 10.1271/bbb.50621. 摘要:Lubell, W. D.; Blankenship, J. W.; Fridkin, G.; Kaul, R., Science of Synthesis, (2005) 21, 748. 摘要:Lubell, W. D.; Blankenship, J. W.; Fridkin, G.; Kaul, R., Science of Synthesis, (2005) 21, 722. 摘要:Zhdankin, V. V., Science of Synthesis, (2007) 31, 225.