CAS: 35899-43-5; (S)-2-((Tert-Butoxycarbonyl)Amino)-3-(1-Tosyl-1H-Imidazol-4-yl)Propanoic Acid

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69541-68-0 123333-71-1 14997-58-1

上下游产品

CAS号98-59-9 对甲苯磺酰氯(PTSC) | CAS号17791-52-5 B°C-组氨酸 | CAS号71-00-1 L-组氨酸 | CAS号119975-64-3 啡肽 | CAS号103336-05-6 Ditekiren

对甲苯磺酰氯,N-Boc-L-组氨酸置于sodium Carbonate体系中,用 水 作为反应溶剂,化学反应 4.0H,以46%的收率获得产物n-叔丁氧羰基-N(咪唑)-(4-甲基苯磺酰基)-L-组氨酸
参考文献:Activated Ketone Based Inhibitors Of Human Renin
标题:Activated Ketone Based Inhibitors Of Human Renin
摘要:Application Of The Concept Of Activated Ketones To The Design Of Novel And Potent Transition-State Analog Inhibitors Of The Aspartyl Protease Renin Is Described. Three Different Classes Of Peptidic Activated Ketones Were Synthesized: 1,1,1-Trifluoromethyl Ketones,Alpha-Keto Esters,And Alpha-Diketones. The Corresponding Alcohols Were Also Evaluated As Renin Inhibitors In Each Series. While The Trifluoromethyl Alcohol 12 (I50 = 4000 Nm) Was Equipotent To The Simple Methyl Alcohol 7 (I50 = 3200 Nm),The Structurally Similar Alpha-Hydroxy Esters (32 And 30,I50'S = 5.3 And 4.7 Nm,Respectively) And Alpha-Hydroxy Ketones (41 And 42,I50 = 23 And 15 Nm,Respectively) Were 150-300-Fold More Active. The Hydrating Capability Of The Activated Ketone Functionality Was Important For Intrinsic Potency In The Case Of Trifluoromethyl Ketones,As Illustrated By The Significantly Better Activity Of Trifluoromethyl Ketone 13 (I50 = 250 Nm) Compared To Its Alcohol Analog 12 (I50 = 4000 Nm). It Was However Unimportant For The Alpha-Keto Ester (20 And 31,I50 = 15 And 4.1 Nm,Respectively) And Alpha-Diketone (43 And 44,I50 = 52 And 28 Nm,Respectively) Based Inhibitors,Since Their Activity Was Essentially Similar To That Of The Corresponding Alcohols. These Results Collectively Suggest That,Whereas The Trifluoromethyl Ketones Derive Their Renin Inhibitory Potency Primarily From Their Ability To Become Hydrated,This Is Not A Critical Feature For The Activity Of Alpha-Dicarbonyl-Based Inhibitors. The Alpha-Keto Ester And Alpha-Diketone Based Renin Inhibitors Benefit Predominantly From The Hydrophobic And/or H-Bonding Type Binding Interactions Of The Neighboring Ester Or Acyl Group Itself,Rather Than The Ability Of This Group To Deactivate The Adjacent Ketone Group And Thereby Make It Susceptible To Hydration.
DOI:10.1021/jm00069A001

专利信息

专利号:US-2018265547-A1
优先权日:2014-07-18
标 题 :Z-selective olefin metathesis of peptides
发明人：MANGOLD SHANE L; GRUBBS ROBERT H
权利人:CALIFORNIA INST OF TECHN
摘要:The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.

专利号:US-7122628-B2
优先权日:2000-12-22
标 题:Process for the synthesis of a peptide having a Trp residue
发明人：JACKSON STEVEN ALLEN
权利人:IPSEN MFG IRELAND LTD
摘要:A process for the solid phase synthesis of a peptide having at least one thyptophan residue, wherein said method comprises temporarily protecting the indole ring of said tryptophan residue with a side chain protecting group which is labile to a base wherein said protecting group is removed during cleavage of said peptide from the solid support.

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-5175146-A
优先权日:1989-12-05
标题 :Synthetic calcitonin peptides
发明人：BASAVA CHANNA; HOSTETLER KARL Y
权利人:VICAL INC
摘要:Synthetic hypocalcemic peptides which are similar in biological properties to native calcitonins as clinically useful agents. The peptides comprise analogues of native calcitonins having amino acid substitutions and deletions which act to improve potency, prolong duration of the hormonal effect, enhance receptor binding, and increase oral or nasal bioavailability. The calcitonin peptide analogues are less expensive and more easily synthesized than native calcitonins, and have improved resistance to inactivation or degradation. Methods are provided for the synthesis of these peptides. Also, disclosed are novel cyclic peptides, including calcitonin, having increased stability with respect to proteolysis. Methods for the synthesis of these peptides are provided, comprising converting disulfide cyclic peptides and proteins to enzymatically and chemically stable cyclic peptide structures by the replacement of cysteine residues with dicarboxylic acids and diamino acids. The method is applicable to various naturally occurring peptides, their synthetic analogues or derivatives, and proteins.

专利号:US-4950418-A
优先权日:1986-10-09
标题 :Reagent for removing protective groups in peptide synthesis
发明人：YAJIMA HARUAKI; FUJII NOBUTAKA; GUTERRES GILBERTO M A; HONGUU TATSUHIKO
权利人:SHINETSU CHEMICAL CO
摘要:Reagent for removing protective groups employed in peptide synthesis comprises a combination of hard acid and soft base. The hard acid is trialkylsilyltrifluoromethanesulphonate R3SiO3SCF3 and the soft base is ether. The reagent provides high efficiency of deprotection and has a low tendency to cause side reaction.

专利号:AU-2005202990-A1
优先权日:2000-12-22
标 题 :Process for the synthesis of a peptide having a tryptophan residue