CAS: 16504-57-7; (S)-3-Amino-4-Hydroxybutanoic Acid

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16504-56-6 83345-44-2 1956437-97-0

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CAS号586952-09-2 (E)-benzyl 4-hy... | CAS号777-33-3 (S)-(-)-2-(三氟乙酰...

📜(E)-Benzyl 4-Hydroxybut-2-Enoate置于氨,Lithium,Sodium Hydroxide体系中,用 四氢呋喃,叔丁醇,水 用作溶剂,化学反应 12.25H,以51%的收率获得d-Beta-高丝氨酸
参考文献:Homochiral Oxazolidin-2-Ones And Imidazolidin-2-Ones By Tandem Nucleophilic Addition-conjugate Addition
标题:Homochiral Oxazolidin-2-Ones And Imidazolidin-2-Ones By Tandem Nucleophilic Addition-conjugate Addition
摘要:Treatment Of Both Primary Alcohols 1A,B And Secondary Amines 1C,D,Tethered To A Michael Acceptor With (R)-Phenylethyl Isocyanate In The Presence Of Dbu Gave In Good Yield And High Stereoselection Diastereomeric Mixtures Of Oxazolidin-2-Ones 2A,B And 3A.B And Imidazolidin-2-Ones 2C,D And 3C,D,Respectively. The Cyclisation Reaction Was Studied Computationally By Ab Initio Quantum Mechanical Methods. The Observed Stereoselectivity Was Explained On The Basis Of The Different Stability Of Both Anions And Transition States Leading To 2A And 3A,Respectively. The Usefulness Of The Method Was Proven By Conversion Of 2A Into The Enantiomerically Pure Bioactive Amino Acid 5. (C) 2004 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tetasy.2004.05.006

专利信息

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-2008207523-A1
优先权日:2006-09-08
标题 :Compounds as aptamer-dimers and their uses in diagnosis and therapy
发明人：FRIEBE MATTHIAS; STEPHENS ANDREW; SRINIVASAN ANANTH; HECHT MAREN
权利人:FRIEBE MATTHIAS; STEPHENS ANDREW; SRINIVASAN ANANTH; HECHT MAREN
摘要:The object of the present invention is solved by compositions of peptide linkers and their use for synthesis and annealing of aptamer oligonucleotides in form of dimers. The present invention in particularly provides said compositions for the use as a diagnostic and/or therapeutic agent. n In another preferred embodiment the present invention relates to a kit for preparing a radiopharmaceutical preparation, said kit comprising a vial comprising a quantity of the compound according to the invention. n A further preferred embodiment of the present invention relates to methods of producing said compounds, comprising synthesis of said compound in an automated peptide synthesizer. n In another preferred embodiment the present invention concerns the use of said compounds according to the present invention for the manufacture of a medicament, preferably for diagnosis or therapy of proliferative diseases. n In a further preferred embodiment the present invention concerns methods for treating or diagnosing patients administering or utilizing the compounds according to the present invention.

专利号:US-6660832-B1
优先权日:1999-08-20
标题:Macrocyclic compounds and preparation methods thereof
发明人：JEFFERSON ELIZABETH; SWAYZE ERIC EDWARD
权利人:ISIS PHARMACEUTICALS INC
摘要:The present invention is directed to macrocyclic compounds of the formula (I)wherein Q, X, R1 and R5 are as defined herein. Compounds of the invention are useful for therapeutic and prophylactic treatment of bacterial infection in mammals. Solid phase synthetic procedures are provided effecting synthesis of the macrocyclic rings attached to a solid support.

专利号:US-2003171434-A1
优先权日:2000-05-17
标题 :Branched amino acids
发明人：JACKSON RICHARD FRANCIS WILLIA; GRABOWSKA URSZULA
摘要:The invention relates to novel branched amino acids and novel methods for their production. The amino acids are useful in the preparation of non-natural peptides and peptidomimetics, by efficient synthesis methodology allowing good enantiomeric specificity at the alpha carbon. Typically the stereochemistry at the alpha carbon is at least 85%, preferably at least 95%, such as in excess of 99% enantiomerically pure. L-stereochemistry at this location is convenient as most biological interactions will favour this configuration, but the invention also extends to enantiomerically enriched and preferably at least 85%, preferably at least 95% such as at least 99% enantiomerically pure D stereoconfiguration. Compounds of the invention will find utility in the preparation of non-natural peptides and peptidomimetics, such as those used in the exploration of receptor specificity and activity or in peptidomimetic inhibitors of enzyme function. The compounds of the invention are built into such peptides/peptidomimetics using standard peptide chemistry.