Sodium Palmitate置于氯化亚砜体系中,化学反应生成棕榈酰氯 参考文献:Studies On Selectin Blocker. 9. Sars Of Non-Sugar Selectin Blocker Against E-,P-,L-Selectin Bindings 标题:Studies On Selectin Blocker. 9. Sars Of Non-Sugar Selectin Blocker Against E-,P-,L-Selectin Bindings 摘要:As A Part Of Study Of Selectin Blockers,We Have Already Reported That A Non-Sugar Selectin Antagonist (3) Was Successfully Discovered Using A Computational Screening (Hiramatsu,Y.; Tsukida,T.; Nakai,Y.; Inoue,Y.; Kondo,H. J. Med. Chem. 2000,43 1476). To Investigate The Sars Of Compound 3 Against E-,P-,And L-Selectins,We Synthesized The Derivatives Of Compound 3 And Evaluated Their Inhibitory Activities Toward Selectin Bindings. The Structural Diversity Of Compound 3 Contained The Following. (1) A Modification Of The Spacer Unit (4-7),(2) A Modification Of The Tail Unit (8-11),(3) A Modification Of The Head Unit (12-18). As A Result,It Was Found That A Non-Sugar Based Selectin Blocker (3) Could Be A Potential Lead Compound For E-,P-,And L-Selectin Blockers And Some Of The Derivatives Showed Broad And/or Selective Inhibitory Activities Toward The E-,P-,And L-Selectins. In Addition,It Was Found That The Experimental Evidence Well Supported That The Computational Screening Using 3D-Pharmacophore Model Could Be Useful Methodology To Find Out A New Lead For The Several Type Of Selectin Blockers,Which Included A Broad And/or A Selective Inhibitor. (C) 2001 Published By Elsevier Science Ltd. Doi:10.1016/s0968-0896(01)00023-2
专利号:US-9260474-B2 优先权日:2011-09-14 标题:Method for solid phase synthesis of liraglutide 发明人:PAN JUNFENG; LIU JIAN; MA YAPING; YUAN JIANCHENG 权利人:PAN JUNFENG; LIU JIAN; MA YAPING; YUAN JIANCHENG; HYBIO PHARMACEUTICAL CO LTD 摘要:Provided is a method for solid phase synthesis of liraglutide, comprising the following steps: A), Fmoc-Gly-resin being obtained by coupling resin solid phase carrier with glycine with N-end protected by Fmoc(Fmoc-Gly-OH) in the presence of activator system; B) according to the peptide sequence of the main chain of liraglutide, successively coupling with amino acids with N-ends protected by Fmoc and protected side chains by the method for solid phase synthesis, wherein lysine employs Fmoc-Lys(Alloc)-OH; C) removing the protective group, Alloc, from the side chain of lysine; D) coupling the side chain of lysine with Palmitoyl-Glu-OtBu by the method for solid phase synthesis; E) cleavage, removing protection groups and resin to obtain crude liraglutide; F) purifying and lyophilizing to obtain liraglutide.
专利号:US-11066439-B2 优先权日:2016-12-10 标题 :Synthesis of liraglutide 发明人:GANGA RAMU VASANTHAKUMAR; PATIL NITIN; CHARYULU PALLE VENKATA RAGHAVENDRA; JASMINE CASTELINO ROOPA; MACHANI RAMBABU; SUVARNA DEEPA SHANKAR 权利人:BIOCON LTD 摘要:The present invention relates to the efficient solid-phase synthesis of liraglutide represented by Formula-I. The present invention relates to an efficient process for the preparation of liraglutide by sequential coupling employing solid phase approach. It involves sequential coupling of protected amino acids to prepare backbone of liraglutide and upon completion of linear sequence, synthesis was extended from lysine side chain by adding γ-glutamic acid and palmitic acid, followed by removal of protective groups, cleavage of the peptide from solid support and purification of crude liraglutide obtained. The present invention also involves the usage of inorganic salts during the coupling, wash with HOBt in DMF solution after Fmoc-deprotection step to suppress the aggregation of peptides and ensure reactions are going for completion, and thus avoid deletion sequences and improve the process yield.
专利号:US-7189849-B2 优先权日:1997-02-10 标 题:Synthesis of acyclic nucleoside derivatives 发明人:LEANNA M ROBERT; RASMUSSEN MICHAEL; HANNICK STEVEN M; TIEN JIEN-HEH J; LUKIN KIRILL A; TIAN ZHENPING; CHANG SOU-JEN; CURTY CYNTHIA B; NARAYANAN BIKSHANDARKOIL A; BELLETTINI JOHN; SHELAT BHADRA; SPITZ TIFFANY 权利人:MEDIVIR AB 摘要:Novel processes towards the synthesis of the antiviral valomaciclovir stearate in which an esterified guanine acetal is reduced to the corresponding alcohol, reacted with an activated amino acid and N-deprotected. The esterified guanine acetal is prepared from a 9-guanine derivative bearing an acyclic hydroxymethylbutylacetal. The processes are amendable to one-pot reactions.
专利号:US-11518794-B2 优先权日:2016-08-19 标 题:Synthesis method for liraglutide with low racemate impurity 发明人:FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG 权利人:SHENZHEN JYMED TECH CO LTD 摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.
专利号:US-9546161-B2 优先权日:2001-07-16 标题:Synthesis of UDP-glucose: N-acylsphingosine glucosyl transferase inhibitors 发明人:HIRTH BRADFORD H; SIEGEL CRAIG 权利人:GENZYME CORP 摘要:Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
专利号:US-2018312463-A1 优先权日:2015-10-22 标题:Synthesis of Cyclohexane Carboxamide Derivatives Useful as Sensates in Consumer Products 发明人:YELM KENNETH EDWARD; WOS JOHN AUGUST; BUNKE GREGORY MARK; FREDERICK HEATH; HAUGHT JOHN CHRISTIAN; HOKE STEVEN HAMILTON; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Synthesis methods to produce a series of carboxamides built off of an (S)-2-amino acid backbone or an (R)-2-amino acid backbone, depending upon the desired diastereomer of the end product.
参考标题:Total Synthesis Of Myc-Iv(C16:0, S) Via Automated Electrochemical Assembly 作者:Kumpei Yano,Toshiyuki Itoh,Toshiki Nokami |发布日期:2020.6 摘要:Total Synthesis Of Myc-Iv(C16:0, S) Via Automated Electrochemical Assembly Has Been Accomplished. This Tetrasaccharide Has Been Studied As A Symbiotic Signal Molecule Of Arbuscular Mycorrhiza Fungi. We Have Achieved Stereoselective Synthesis Of A Disaccharide Building Block Using The Mixed-Electrolyte System For Electrochemical Glycosylation; 2 + 1+1 Strategy Enables Us To Access The Tetrasaccharide
合成参考文献
摘要:Toyota, S.; Iwanaga, T., Science of Synthesis, (2010) 45, 816. 摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2014) 2, 455. 摘要:Weast, R.C. and M.J. Astle. CRC Handbook of Data on Organic Compounds. Volumes I and II. Boca Raton, FL: CRC Press Inc. 1985., p. V2 2 参考文献:10.1042/ba20030158 摘要:Le-Tien C, Millette M, Mateescu MA, Lacroix M. Modified alginate and chitosan for lactic acid bacteria immobilization. Biotechnol Appl Biochem. 2004 Jun;39(Pt 3):347–54. doi: 10.1042/ba20030158. 参考文献:10.1186/1752-153x-8-32 摘要:Lahsasni SA, Al Korbi FH, Aljaber NA. Synthesis, characterization and evaluation of antioxidant activities of some novel chalcones analogues. Chemistry Central Journal. 2014 May 07;8(1). doi: 10.1186/1752-153x-8-32.