Ethyl (2R)-2-Acetamido-3-Naphthalen-1-Ylpropanoate置于盐酸体系中,化学反应 2.0H,以55%的收率获得产物d-3-(1-萘基)-丙氨酸盐酸盐 参考文献:Synthesis And Biological Activities Of Cholecystokinin Analogues Substituted In Position 30 By 3-(1-Naphthyl)-L-Alanine [nal(1)] Or 3-(2-Naphthyl)-L-Alanine [nal(2)] 标题:Synthesis And Biological Activities Of Cholecystokinin Analogues Substituted In Position 30 By 3-(1-Naphthyl)-L-Alanine [nal(1)] Or 3-(2-Naphthyl)-L-Alanine [nal(2)] 摘要:Acetyl Derivatives Of Ethyl Esters Of 3-(1-Naphthyl)-D,L-Alanine And 3-(2-Naphthyl)-D,L-Alanine Were Synthesized Through A Malonic Condensation. Resolution Of These Derivatives By Subtilisin Carlsberg Followed By Acid Hydrolysis Afforded The 2 Optical Isomers Of 3-(1-Naphthyl)-Alanine [nal(1)] And 3-(2-Naphthyl)-Alanine [nal(2)]. The L Enantiomers Of These Amino Acids Were Incorporated Into The Sequence Of Cholecystokinin In Place Of The Tryptophan In Position 30. The Cholecystokinin Analogues Thus Obtained Behaved As Full Agonists,With Reduced Potencies On Rat Pancreatic Acini And On Guinea Pig Brain Membranes,By About One Order Of Magnitude For The Nal(2) Derivative And By 2 Orders Of Magnitude For The Nal(1) Derivative,As Compared To The Potent Parent Compound Boc-Tyr(So3H)-Nle-Gly-Trp-Nle-Asp-Phe-Nh2. DOI:10.1016/0223-5234(91)90056-S
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
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-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-2018371021-A1 优先权日:2017-05-11 标 题 :Peptidomimetic macrocycles and uses thereof 发明人:AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
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
参考文献:10.1007/s10989-026-10809-3 摘要:Chaturvedi S, Choudhary R, Sharma N. High-Resolution LC–MS Approach for Structural Elucidation and (Q)SAR-Based Toxicity Assessment of Cyclic Peptide Lanreotide Acetate Degradation Products. Int J Pept Res Ther. 2026 Feb 01;32(2). doi: 10.1007/s10989-026-10809-3.