CAS: 34994-11-1; Hypusine

📜(2S,9R)-7-Benzyl-2-(Carbobenzoxyamino)-10-Cyano-9-Hydroxy-7-Azadecanoic Acid Benzyl Ester置于platinum(Iv) Oxide 氢气体系中,用 溶剂黄146 用作溶剂,化学反应 3.0H,反应生成(2S)-2-氨基-6-[[(2S)-4-氨基-2-羟基丁基]氨基]己酸
参考文献:Total Syntheses Of (+)-Hypusine And Its (2S,9S)-Diastereomer
标题:Total Syntheses Of (+)-Hypusine And Its (2S,9S)-Diastereomer
摘要:The Total Synthesis Of (2S,9R)-Hypusine Dihydrochloride,An Unusual Amino Acid Constituent Of The Eukaryotic Translation Initiation Factor Eif-4D,And Its (2S,9S) Diastereomer Is Described. The Key Step In The Syntheses Involves The Nepsilon-Alkylation Of Nepsilon-Benzyl-Nalpha-(L)-Lysine Benzyl Ester With (R)-Or (S)-Epichlorohydrin To Give The Respective (2S,9R) And (2S,9S) Chlorohydrins. Subsequent Displacement Of The Respective Chlorides By Cyanide Ion Provides The Protected Hypusine Skeletons. The Final Step,Hydrogenation Over Pto2 In Acoh Followed By Neutralization And Reacidification,Yielded The Respective (2S,9S)-And (2S,9R)-Hypusine Dihydrochlorides In Excess Of 50% Overall Yield.
Doi:10.1021/jo00076A048

专利信息

专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人：FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

专利号:US-11225655-B2
优先权日:2010-04-16
标题:Bi-functional complexes and methods for making and using such complexes
发明人：GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK
权利人:GOULIAEV ALEX HAAHR; FRANCH THOMAS; GODSKESEN MICHAEL ANDERS; JENSEN KIM BIRKEBAEK; NUEVOLUTION AS
摘要:The present invention is directed to a method for the synthesis of a bi-functional complex comprising a molecule part and an identifier oligonucleotide part identifying the molecule part. A part of the synthesis method according to the present invention is preferably conducted in one or more organic solvents when a nascent bi-functional complex comprising an optionally protected tag or oligonucleotide identifier is linked to a solid support, and another part of the synthesis method is preferably conducted under conditions suitable for enzymatic addition of an oligonucleotide tag to a nascent bi-functional complex in solution.

专利号:US-2012095058-A1
优先权日:2003-12-03
标 题 :Method of preventing survival of retrovirally cells and of inhibiting formation of infectious retroviruses
发明人：HANAUSKE-ABEL H M; PALUMBO PAUL; CRACCHIOLO B M; PARK MYUNG-HEE; WOLFF EDITH; HANAUSKE AXEL-RAINER; MATHEWS MICHAEL B; SAXENA DEEPTI; HOQUE MAINUL
权利人:HANAUSKE-ABEL H M; PALUMBO PAUL; CRACCHIOLO B M; PARK MYUNG-HEE; WOLFF EDITH; HANAUSKE AXEL-RAINER; MATHEWS MICHAEL B; SAXENA DEEPTI; HOQUE MAINUL
摘要:The present invention discloses compounds and pharmaceutical compositions which are highly effective at inhibiting the accumulation of spliced and unspliced viral transcripts and their utilization for viral protein synthesis at cellular ribosomes, and at inhibiting the formation of the hypusine residue in cellular eIF-5A precursor proteins, the cellular cofactors that render spliced and unspliced viral transcripts translatable at the ribosomes of infectled cells. The invention further relates to methods of using such compounds and pharmaceutical compositions therefrom for inhibiting or preventing viral protein synthesis. Such inhibition cause a dose-dependent release from the virally induced arrest of the otherwise genetically preprogrammed apoptosis of virally infected cells, and in consequence, triggers their apoptotic ablation and the eradication of the chronic infection-mediating provirus integrated into their genome.

专利号:US-11702652-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries

专利号:US-2009264300-A1
优先权日:2005-12-01
标题 :Enzymatic encoding methods for efficient synthesis of large libraries

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.