N-乙酰-L-4-羟基脯氨酸置于盐酸,乙酸酐体系中,化学反应 9.0H,反应生成顺式-4-羟基-D-脯氨酸 参考文献:Stereoselective Synthesis Of (1R,4R)-N-Acyl-2-Oxa-5-Aza-Bicyclo[2.2.1]Heptan-3-Ones Via Mesoionic Compounds. An Improved Synthesis Of Cis-4-Hydroxy-D-Proline 标题:Stereoselective Synthesis Of (1R,4R)-N-Acyl-2-Oxa-5-Aza-Bicyclo[2.2.1]Heptan-3-Ones Via Mesoionic Compounds. An Improved Synthesis Of Cis-4-Hydroxy-D-Proline 摘要:We Report An Asymmetric Synthesis Of (1R,4R)-N-Acyl-2-Oxa-5-Aza-Bicyclo[2.2.1]Heptan-3-Ones,Starting From The Inexpensive And Commercially Available Trans-4-Hydroxy-L-Proline And Achieved By Treating N-Acyl-Trans-4-Hydroxy-L-Prolines With Acetic Anhydride. The Formation Of Intermediate Mesoionic Compounds May Explain The Formation Of N-Acyl-2-Oxa-5-Azabicyclo[2.2.1]Heptan-3-Ones With (R)-Absolute Configuration At C(4). Acidic Cleavage Of These Lactones Readily Affords N-Acyl-Cis-4-Hydroxy-D-Prolines Or Cis-4-Hydroxy-D-Proline In Good Yields. (C) 2002 Elsevier Science Ltd. All Rights Reserved. Doi:10.1016/s0957-4166(02)00074-5
专利号:US-9433605-B2 优先权日:2006-03-23 标 题 :Method for promoting synthesis of tissue collagen 发明人:KAMIYA TOSHIKAZU; KAMIMURA AYAKO; KAWADA YOKO 权利人:KYOWA HAKKO BIO CO LTD 摘要:An object of the present invention is to provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which is safe and has an excellent effect. The present invention can provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which comprises hydroxyproline or a salt thereof as an active ingredient.
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-2007232813-A1 优先权日:2006-03-28 标 题:Substituted Cyclohexadienals - Syntheses and Applications 发明人:WATANABE CORAN M H; BENCH BENNIE JOHN 权利人:WATANABE CORAN M H; BENCH BENNIE JOHN 摘要:The present invention is generally directed to the use of L-proline and certain derivatives thereof to catalyze the asymmetric self-condensation of α,β-unsaturated aldehydes to form homodimer and heterodimer cyclohexadienals. Reaction conditions are mild and yet amenable to a variety of different substrates yielding molecules with complex scaffolds from simple precursors. This approach allows for diversification and synthesis of this structural class of compounds in sufficient quantity, purity and enantioselectivity for, e.g., biological investigations and use as fluorescent probes, anti-cancer agents, anti-bacterial agents, and/or anti-fungal agents. The present invention is also generally directed to the cyclohexadienals produced.
专利号:US-5892038-A 优先权日:1997-12-08 标 题 :Hydroxy-amino acid amides 发明人:DOLLE III ROLAND ELLWOOD; PATEL HITESH K 权利人:PHARMACOPEIA INC 摘要:Compounds of Formula I I are disclosed as inhibitors of plasmepsin and cathepsin D. The compounds are therefore useful to treat diseases such as malaria. In preferred compounds of formula I, Y is the residue of an N-acylated amino acid, a substituted 4-aminoproline or a substituted piperazinealkanoic acid. Intermediates in the solid phase synthesis of compounds of formula I, in which the compounds are attached to a solid support, are also disclosed.
专利号:US-2010093612-A1 优先权日:2007-02-21 标 题 :Integrin targeted cyclopeptide ligands, their preparation and use 发明人:CASIRAGHI GIOVANNI; BURREDDU PAOLA; MANZONI LEONARDO PIERPAOLO; SCOLASTICO CARLO; ZANARDI FRANCA; BATTISTINI LUCIA; CURTI CLAUDIO; RASSU GLORIA; AUZZAS LUCIANA 权利人:CASIRAGHI GIOVANNI; BURREDDU PAOLA; MANZONI LEONARDO PIERPAOLO; SCOLASTICO CARLO; ZANARDI FRANCA; BATTISTINI LUCIA; CURTI CLAUDIO; RASSU GLORIA; AUZZAS LUCIANA 摘要:The present invention relates to novel hybrid cyclopeptide compounds embodying pyrrolidine- or piperidine-based amino acid substructures grafted onto a RGD (-Arg-Gly-Asp-) tripeptide sequence and acting as targeting ligands towards integrin receptors, intended, for example, for the treatment of altered angiogenic phenomena or for the preparation of therapeutically and/or diagnostically useful compounds; the invention also concerns a process for the synthesis of said cyclopeptides and biologically active derivatives thereof.
专利号:US-11702652-B2 优先权日:2005-12-01 标题:Enzymatic encoding methods for efficient synthesis of large libraries
[参考文献]: Püschl A, Et, Al. Pyrrolidine Pna: A Novel Conformationally Restricted Pna Analogue. Org Lett. 2000 Dec 28;2(26):4161-3. [参考文献]: Watanabe S, Et, Al. Characterization Of Cis-4-Hydroxy-D-Proline Dehydrogenase From Sinorhizobium Meliloti. Biosci Biotechnol Biochem. 2018 Jan;82(1):110-113. [参考文献]: B C Roy, Et Al. Modification Of Mature Non-Reducible Collagen Cross-Link Concentrations In Bovine M. Gluteus Medius And Semitendinosus With Steer Age At Slaughter, Breed Cross And Growth Promotants. Meat Sci. 2015 Dec:110:109-17. [参考文献]: Charles E Deutch, Et Al. Oxidation Of 3,4-Dehydro-D-Proline And Other D-Amino Acid Analogues By D-Alanine Dehydrogenase From Escherichia Coli. Fems Microbiol Lett. 2004 Sep 15;238(2):383-9. [参考文献]: Grégory Lacraz, Et Al. Increased Stiffness In Aged Skeletal Muscle Impairs Muscle Progenitor Cell Proliferative Activity. Plos One. 2015 Aug 21;10(8):E0136217.
合成参考文献
参考文献:10.1021/jacs.4c01419 摘要:Rothchild KW, Hagar M, Berry D, Ryan KS. Two Iron(II), α-Ketoglutarate-Dependent Enzymes Encoded by the PPZ Gene Cluster of Metarhizium majus Enable Production of 8-Hydroxyperamine. J. Am. Chem. Soc. 2024 Apr 05;146(15):10263–7. doi: 10.1021/jacs.4c01419. 参考文献:10.1002/elps.201000187 摘要:Gavina JM, White CE, Finan TM, Britz-McKibbin P. Determination of 4-hydroxyproline-2-epimerase activity by capillary electrophoresis: A stereoselective platform for inhibitor screening of amino acid isomerases. Electrophoresis. 2010 Aug;31(16):2831–7. doi: 10.1002/elps.201000187.