(2S)-[(1'R)-Phenylethylamino]-4-Pentenoic Acid置于palladium On Carbon 氢气体系中,用 水 作为反应溶剂,50.0 °C,2.2 Mpa 条件下,反应 47.0H,以41.5%的收率获得产物l-正缬氨酸 参考文献:Novel Imidazolidinone Derivative,Method Of Producing The Same And Method Of Producing Optically Active Amino Acid 标题:Novel Imidazolidinone Derivative,Method Of Producing The Same And Method Of Producing Optically Active Amino Acid
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-12188072-B2 优先权日:2018-03-19 标题 :Compositions and methods for rapid in vitro synthesis of bioconjugate vaccines in vitro via production and N-glycosylation of protein carriers in detoxified prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated carrier proteins. The glycosylated carrier proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated carrier proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated carrier proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:US-12365930-B2 优先权日:2016-07-14 标题:Method for rapid in vitro synthesis of glycoproteins via recombinant production of N-glycosylated proteins in prokaryotic cell lysates 发明人:JEWETT MICHAEL CHRISTOPHER; STARK JESSICA CAROL; DELISA MATTHEW P; JAROENTOMEECHAI THAPAKORN 权利人:UNIV NORTHWESTERN; UNIV CORNELL 摘要:Disclosed are methods, systems, components, and compositions for cell-free synthesis of glycosylated proteins. The glycosylated proteins may be utilized in vaccines, including anti-bacterial vaccines. The glycosylated proteins may include a bacterial polysaccharide conjugated to a carrier, which may be utilized to generate an immune response in an immunized host against the polysaccharide conjugated to the carrier. The glycosylated proteins may be synthesized in cell-free glycoprotein synthesis (CFGpS) systems using prokaryote cell lysates that are enriched in components for glycoprotein synthesis such as oligosaccharyltransferases (OSTs) and lipid-linked oligosaccharides (LLOs) including OSTs and LLOs associated with synthesis of bacterial O antigens.
专利号:US-2023313255-A1 优先权日:2020-07-15 标题:Massively Parallel Enzymatic Synthesis of Polynucleotides 发明人:HORGAN ADRIAN; LACHAIZE HENRI; VERARDO DOMIANO; GODRON XAVIER 权利人:DNA SCRIPT 摘要:The invention is directed to methods and compositions for inkjet assisted synthesis of a plurality of polynucleotides at reaction sites on a substrate using template-free polymerases, such as, terminal deoxynucleotidyl transferases (TdTs). Compositions of the invention include formulations of synthesis reagents for inkjet delivery including, but not limited to, TdT coupling reaction buffers and 3′-O-protected dNTP monomers.
专利号:US-6774259-B2 优先权日:2000-04-11 标 题 :Method for synthesis of n-[(s)]-1-carboxybutyl-(s)-alanine esters and use in synthesis of perindopril 发明人:SOUVIE JEAN-CLAUDE; RENAUD ALAIN 权利人:SERVIER LAB 摘要:A stereoselective process for the industrial synthesis of compounds of formula (I):wherein R represents linear or branched (C1-C6)alkyl, andapplication in the synthesis of perindopril and pharmaceutically acceptable salts thereof.
专利号:US-4902817-A 优先权日:1987-09-17 标 题 :Process for the synthesis of alpha n alkylated amino acids and esters thereof, application to the synthesis of carboxyalkyl dipeptides 发明人:VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES 权利人:ADIR 摘要:Stereoselective process for the industrial synthesis of compounds of formula (I): ##STR1## where R 1 is linear or branched lower alkyl with 1 to 6 carbon atoms, n R 2 is a linear or branched lower alkyl with 1 to 4 carbon atoms, n employing inexpensive starting materials and obtaining optimum yields. n Application to the synthesis of carboxyalkyl dipeptides.
[参考文献]: E V Sycheva, Et Al. [参考文献]: Mikrobiologiia. 2007 Nov-Dec;76(6):805-12. [参考文献]: Iris Thondorf, Et Al. Three-Dimensional Quantitative Structure-Activity Relationship Analyses Of Substrates Of The Human Proton-Coupled Amino Acid Transporter 1 (Hpat1). Bioorg Med Chem. 2011 Nov 1;19(21):6409-18. [参考文献]: Jaclyn Bailey, Et Al. A Novel Mechanism Of V-Type Zinc Inhibition Of Glutamate Dehydrogenase Results From Disruption Of Subunit Interactions Necessary For Efficient Catalysis. Febs J. 2011 Sep;278(17):3140-51. [参考文献]: Jvalini T Dwarkasing, Et Al. Hypothalamic Food Intake Regulation In A Cancer-Cachectic Mouse Model. J Cachexia Sarcopenia Muscle. 2014 Jun;5(2):159-69. [参考文献]: Kevin M Smith, Et Al. An Evolutionary Strategy For Isobutanol Production Strain Development In Escherichia Coli. Metab Eng. 2011 Nov;13(6):674-81.
合成参考文献
参考文献:10.4061/2011/515047 摘要:Pokrovskiy MV, Korokin MV, Tsepeleva SA, Pokrovskaya TG, Gureev VV, Konovalova EA, Gudyrev OS, Kochkarov VI, Korokina LV, Dudina EN, Babko AV, Terehova EG. Arginase Inhibitor in the Pharmacological Correction of Endothelial Dysfunction. International Journal of Hypertension. 2011;2011():1–4. doi: 10.4061/2011/515047. 参考文献:10.1111/j.1742-4658.2011.08240.x 摘要:Bailey J, Powell L, Sinanan L, Neal J, Li M, Smith T, Bell E. A novel mechanism of V‐type zinc inhibition of glutamate dehydrogenase results from disruption of subunit interactions necessary for efficient catalysis. The FEBS Journal. 2011 Aug 11;278(17):3140–51. doi: 10.1111/j.1742-4658.2011.08240.x.