(S)-2-Acetylamino-3-(3-Hydroxyphenyl)Propionic Acid置于盐酸体系中,用 Aq. Phosphate Buffer 作为反应溶剂,化学反应 2.0H,以11.1 G的收率获得产物l-M-酪氨酸 参考文献:Optimized Synthesis Of L-M-Tyrosine Suitable For Chemical Scale-Up 标题:Optimized Synthesis Of L-M-Tyrosine Suitable For Chemical Scale-Up 摘要:This Paper Demonstrates How L-M-Tyrosine 1 Can Be Synthesized On Larger-Scale Via Enzyme-Catalyzed Kinetic Resolution Of N-Acyl M-Tyrosine Methyl Ester 4. N-Acyl M-Tyrosine Methyl Ester 4 Was Prepared By A Modification Of Erlenmeyer'S Azalactone Synthesis Followed By Hydrogenation Of The Resultant Dehydroamino Acid 12. The Optimized Four-Step Synthesis Utilizes Cheap And Readily Available Starting Materials And Circumvents Difficult Purification Protocols. DOI:10.1021/op700093Y
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:WO-2008098280-A1 优先权日:2007-02-16 标题:Methods for the synthesis of dicarba bridges in growth hormone peptides 发明人:ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 权利人:POLYCHIP PHARMACEUTICALS PTY; UNIV MONASH; ROBINSON ANDREA JANE; VAN LIEROP BIANCA; WHELAN AMANDA 摘要:The invention relates to peptides comprising the carboxy terminal sequence of a growth hormone or an analogue of such a peptide in which the disulfide bridge is replaced by a dicarba bridge. Compositions containing such dicarba bridged peptides and method of treating obesity in an animal such as a human comprising administration of such dicarba bridged peptides are also disclosed.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-11718864-B2 优先权日:2015-09-23 标 题 :Cells and method of cell culture 发明人:HILLER GREGORY WALTER; MITCHELL JEFFREY JOSEPH; MULUKUTLA BHANU CHANDRA; PEGMAN PAMELA MARY 权利人:PFIZER 摘要:The invention relates to a method of cell culture where the cells are modified to reduce the level of synthesis of growth and/or productivity inhibitors by the cell. The invention also relates to a method of cell culture for improving cell growth and productivity, in particular in fed-batch culture of mammalian cells at high cell density. The invention further relates to a method of producing cells with improved cell growth and/or productivity in cell culture and to cells obtained or obtainable by such methods.
专利号:US-2013131343-A1 优先权日:2009-12-07 标 题:Microwave-assisted synthesis of n-heterocyclic carbene transition metal complexes 发明人:NAVARRO OSCAR; WINKELMANN OLE H 权利人:NAVARRO OSCAR; WINKELMANN OLE H; UNIV HAWAII 摘要:Microwave heating is used to synthesize NHC-transition metal complexes. Reaction times for the formation of NHC-transition metal complexes is greatly reduced. The speed of the reactions allows for otherwise problematic air handling of reagents. Apparatus for carrying out the reactions is less complex than conventional apparatus and requires less energy to achieve the desired temperatures. Methods utilize salts of NHC's which overcomes the oftentimes difficult preparation of free carbenes for formation of the corresponding transition metal complexes.
专利号:US-2023364251-A1 优先权日:2020-08-06 标 题:Methods for the synthesis of protein-drug conjugates 发明人:BORCHARDT ALLEN; HUGHES ROBERT MICHAEL 权利人:CIDARA THERAPEUTICS INC 摘要:The present invention relates to intermediates and methods for synthesizing protein-drug conjugates that can be used for the treatment of diseases and related conditions.
1: Leung K. 8-[(123)I]Iodo-L-1,2,3,4-tetrahydro-7-hydroxyisoquinoline-3-carboxylic acid. 2007 Feb 22 [updated 2008 May 12]. Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004-2013. Available from http://www.ncbi.nlm.nih.gov/books/NBK23698/ Available from http://www.ncbi.nlm.nih.gov/books/NBK23533/ Available from http://www.ncbi.nlm.nih.gov/books/NBK23494/
合成参考文献
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