专利号:US-2025066393-A1 优先权日:2021-12-24 标题 :Amine-protecting group 发明人:XU PENGYU; YONEYAMA SHIN 权利人:SYNCREST INC 摘要:An object of the present invention is to provide novel amine-protecting groups useful for the synthesis of special amino acids. Provided is an amine-protecting group.
专利号:US-12433936-B2 优先权日:2021-04-12 标 题:High-purity adrenocorticotropic hormone analogue and a large-scale preparation method thereof 发明人:MENG JUNDONG; YANG TAO; WU FEIFEI; ZHANG HAONING 权利人:NANJING HANXIN PHARMACEUTICAL TECH CO LTD 摘要:Polypeptide preparation methods of preparing high-purity ACTH (human sequence) or analogue and large-scale preparation method thereof are described. The main steps include: amino acids are coupled from the C-terminal to the N-terminal by Fmoc solid-phase synthesis method to obtain the crude ACTH (human sequence) or analogue peptidyl-resin with protective groups, wherein the reaction temperature of C-15 peptide synthesis is 40-60° C. After cleavage and precipitation, the crude product of ACTH (human sequence) or analogue is obtained, and then the high-purity product is obtained by liquid chromatography. The chromatographic purity of ACTH (human sequence) or analogue prepared by the invention is more than 99%, the stability is good, and the yield of the target peptide is ≥63%.
专利号:US-11419919-B1 优先权日:2021-04-12 标题 :High-purity adrenocorticotropic hormone, analogue and a large-scale preparation method thereof 发明人:MENG JUNDONG; Rui Kangning; LIU BIN; HAN YUANYUAN; CHEN SONG; ZHANG HAONING 权利人:NANJING HANXIN PHARMACEUTICAL TECH CO LTD 摘要:The invention belongs to the technical field of polypeptide preparation methods, and in particular relates to a high-purity ACTH (human sequence) or analogue and large-scale preparation method thereof. The main steps include: amino acids are coupled from the C-terminal to the N-terminal by Fmoc solid-phase synthesis method to obtain the crude ACTH (human sequence) or analogue peptidyl-resin with protective groups, wherein the reaction temperature of C-15 peptide synthesis is 40-60° C. After cleavge and precipitation, the crude product of ACTH (human sequence) or analogue is obtained, and then the high-purity product is obtained by liquid chromatography. The chromatographic purity of ACTH (human sequence) or analogue prepared by the invention is more than 99%, the stability is good, and the yield of the target peptide is ≥63%.
专利号:US-RE49961-E 优先权日:2016-10-21 标 题:Solid phase peptide syntheses 发明人:COLLINS JONATHAN M 权利人:CEM CORP 摘要:An improved method of deprotection in solid phase peptide synthesis is disclosed. In particular the deprotecting composition is added in high concentration and small volume to the mixture of the coupling solution, the growing peptide chain, and any excess activated acid from the preceding coupling cycle, and without any draining step between the coupling step of the previous cycle and the addition of the deprotection composition for the successive cycle. Thereafter, the ambient pressure in the vessel is reduced with a vacuum pull to remove the deprotecting composition without any draining step and without otherwise adversely affecting the remaining materials in the vessel or causing problems in subsequent steps in the SPPS cycle.
专利号:CN-111285921-B 优先权日:2020-02-12 标 题:Liquid-phase total synthesis method of BDK auxiliary group and plecanatide and analogues based on BDK auxiliary group
专利号:US-2024124517-A1 优先权日:2020-12-25 标题:Method for producing peptide compound containing n-substituted-amino acid residue 发明人:MORITA YUYA; NOMURA KENICHI 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:An object of the present invention is to provide a method for efficiently producing a high-purity peptide compound with a high yield. It has been found that the object can be achieved by supporting a peptide on a solid phase synthesis resin prior to a first elongation reaction in a solid phase process.
参考标题:1,1-Dioxonaphtho[1,2-B]Thiophene-2-Methyloxycarbonyl (α-Nsmoc) And 3,3-Dioxonaphtho[2,1-B]Thiophene-2-Methyloxycarbonyl (β-Nsmoc) Amino-Protecting Groups 作者:Louis A. Carpino,Adel Ali Abdel-Maksoud,Dumitru Ionescu,E. M. E. Mansour,Mohamed A. Zewail |发布日期:2007.3.1 摘要:Mechanistically Similar To That Previously Established For The Bsmoc Derivative In That The Reaction Is Initiated By Michael Addition To The β-Carbon Atom Of The α,β-Unsaturated Sulfone System. Application Of α- And β-Nsmoc Amino Acids To The Solid-Phase Synthesis Of Two Model Peptides Was Examined. An Advantage Of The α-Nsmoc System Over The Long-Known Bsmoc System Proved To Be The Milder Conditions Needed For
合成参考文献
摘要:Lubell, W. D.; Blankenship, J. W.; Fridkin, G.; Kaul, R., Science of Synthesis, (2005) 21, 739.