📜(Trimethylsilyl)Cyclopropanone 反应生成 3-三甲基硅基丙酸 参考文献:Bogdanova,G.S. Et Al.,Journal Of General Chemistry Of The Ussr,1979,Vol. 49,P. 2468 标题:Bogdanova,G.S. Et Al.,Journal Of General Chemistry Of The Ussr,1979,Vol. 49,P. 2468
专利号:US-8722886-B1 优先权日:2012-11-13 标题:Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin 发明人:CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY 权利人:CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY; BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
专利号:WO-2014052054-A1 优先权日:2012-09-25 标题 :Enzymatic platform for the synthesis of isoprenoid precursors and uses thereof 发明人:LEYH THOMAS S 权利人:EINSTEIN COLL MED 摘要:Provided are method of synthesizing (R)-5-diphosphomevalonate (DPM), isopentenyl 5-pyrophosphase (IPP), dimethylallyl 5 -pyrophosphate (DMAPP) and isoprenoid using a one-pot synthesis.
专利号:US-2009263858-A1 优先权日:2004-09-14 标 题 :Process for synthesis of mucin-type peptides and muc1-related glycopeptides 发明人:NISHIMURA SHINICHIRO; HINOU HIROSHI; FUMOTO MASATAKA 权利人:SHIONOGI & CO 摘要:The invention aims at providing novel compounds useful as primer in producing mucin-type glycopeptides which are useful in a wide field including materials for biochemical research, drugs, and food and the production of which was difficult in the prior art; and a process for the production of glycopeptides by using the primers. The aim is attained by providing novel glycopeptide derivatives (represented by the general formula (I)) which each bear an aldehyde or ketone group at the end and each contain an amino acid residue cleavable with a protease; and an easy and simple process for the production of glycopeptides by using the derivative as the primer.
专利号:US-2005165215-A1 优先权日:2003-12-31 标 题 :Peptide synthesis and deprotection using a cosolvent 发明人:BIGELOW ROGER D; SCHWINDT MARK A; WITHERS GREGORY P 摘要:The invention provides methods for synthesizing peptides, which include taking an organic solvent having non-resin bound protected peptide and performing a deprotection reaction on the non-resin bound protected peptide. In these methods it is not required that the peptide is dried immediately before providing to the deprotection reaction. Also provided are methods of synthesizing peptides, wherein a protected peptide is formed in a solution phase reaction, dissolved into an organic solvent, and then introduced into a deprotection reaction. Also provided are methods of synthesizing peptides, wherein a non-resin bound protected peptide is concentrated in an organic solvent prior to being subject to a deprotection reaction.
专利号:US-6248866-B1 优先权日:1997-10-31 标 题:Hypusine reagent for peptide synthesis 发明人:BERGERON JR RAYMOND J 权利人:UNIV FLORIDA 摘要:A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as an improved method for synthesizing the same, the derivative having the formula:wherein: Q1 and Q2 may be the same or different and are amino protective groups; Q3 is an amino protective group which is orthogonal to Q1 and Q2; and Z is a hydroxy protective group.
专利号:US-11220446-B2 优先权日:2017-03-09 标 题:Process for producing an anionic lignin copolymer under aqueous acid conditions 发明人:FATEHI PEDRAM; KONG FANGONG; WANG SHOUJUAN; PRICE JACQUELYN; PALEOLOGOU MICHAEL 权利人:FPINNOVATIONS; UNIV LAKEHEAD 摘要:An acidic water-based process was developed for the synthesis of anionic lignin copolymers with adjustable MW, thermal stability and solubility in water. The anionic lignin copolymer described herein comprises: a molecular weight of 5,000 to 7.4×10 5 g/mol; and a charge density of −1 to −7.2 meq/g. The anionic lignin copolymers described herein which have a molecular weight range of 000-50,000 g/mol can be used as dispersants of negatively charged molecules or particles in numerous process or wastewater streams (e.g. concrete admixtures, gypsum slurries, textile dye) while such copolymers in a molecular weight range of 90,000-740,000 g/mole can be used as flocculants of positively charged molecules or particles in numerous process and wastewater streams including industrial and municipal systems and sludge dewatering in the textile dye, pulp & paper, mining and oil industries.
摘要:Grimmer, J.; Krieg, S.-C.; Manolikakes, G., Science of Synthesis Knowledge Updates, (2021) 1, 251. 摘要:Clarke, M. L.; Fuentes, J. A., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 1, 235. 参考文献:10.1007/bf01388170 摘要:Calmes M, Daunis J. How to build optically active alpha-amino acids. Amino Acids. 1999;16(3-4):215–50. doi: 10.1007/bf01388170. 参考文献:10.1007/s00216-015-9047-x 摘要:Madji Hounoum B, Blasco H, Nadal-Desbarats L, Diémé B, Montigny F, Andres CR, Emond P, Mavel S. Analytical methodology for metabolomics study of adherent mammalian cells using NMR, GC-MS and LC-HRMS. Analytical and Bioanalytical Chemistry. 2015 Oct 07;407(29):8861–72. doi: 10.1007/s00216-015-9047-x.