CAS: 37535-49-2; H-4-Pal-Oh

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CAS号674309-79-6 2-oxo-3-(1H-pyr... | CAS号102913-23-5 (4Z)-2-methyl-4... | CAS号872-85-5 4-吡啶甲醛 | CAS号131905-74-3 d-methyl 2-acet... | CAS号37535-57-2 B°C-3-(4-吡啶基)-L-丙氨酸 | CAS号169555-95-7 Fm°C-3-(4-吡啶基)-L-丙氨酸

(S)-4'-(Pyridin-4-Ylmethyl)-9λ4-Boraspiro[bicyclo[3.3.1]Nonane-9,2'-[1,3,2]Oxazaborolidin]-5'-One置于四丁基氟化铵体系中,用 四氢呋喃,水 作为反应溶剂,化学反应 3.0H,以77%的收率获得产物l-3-(4-吡啶基)-丙氨酸
参考文献:四丁基氟化铵作为一种温和且通用的试剂,用于将硼恶唑烷酮裂解为相应的游离 α-氨基酸
标题:四丁基氟化铵作为一种温和且通用的试剂,用于将硼恶唑烷酮裂解为相应的游离 α-氨基酸
摘要:用 9-硼双环 [3.3.1] 壬烷 (9-Bbn) 保护 α-氨基酸以得到相应的硼恶唑烷酮非常有吸引力,因为它同时掩盖了氨基和羧酸官能团.然而,脱保护所需的苛刻方法限制了其使用.在这里,我们报告四丁基氟化铵 (Tbaf) 是一种温和且通用的试剂,可将硼恶唑烷酮裂解为相应的游离 α-氨基酸.研究了反应条件,包括使用各种亲核氟化物源,溶剂和反应温度.包含铵阳离子的亲核氟化物源证明优于其他抗衡阳离子.反应范围扩展到 B,B-二苯基-和 B,B-二乙基硼恶唑烷酮配合物的裂解.此外,
DOI:10.1002/ejoc.201700063

专利信息

专利号:US-9475837-B2
优先权日:2011-12-23
标题 :Process for the synthesis of therapeutic peptides
发明人：HURLEY FIONN; WEGNER KATARZYNA; FOLEY PATRICK
权利人:IPSEN MFG IRELAND LTD
摘要:The present invention relates to a process for the large-scale synthesis of therapeutic peptides using a Sieber Amide resin, which comprises solid-phase Fmoc-chemistry.

专利号:US-2024218014-A1
优先权日:2022-11-21
标 题:Synthesis of a cyclic peptide
发明人：BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL
权利人:JANSSEN PHARMACEUTICA NV
摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.

专利号:US-2023212788-A1
优先权日:2020-03-26
标 题:New method for automated on-demand biomolecular array synthesis
发明人：ZHANG YIXIN; LIN WEILIN
权利人:UNIV DRESDEN TECH
摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.

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-12441760-B2
优先权日:2013-08-29
标 题 :Amino diacids containing peptide modifiers
发明人：BARLOS KLEOMENIS; GATOS DIMITRIOS; BARLOS KOSTAS K; VASILEIOU ZOI
权利人:CHEMICAL & BIOPHARMACEUTICAL LABORATORIES OF PATRAS S A
摘要:The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula (1) in the synthesis of peptide derivatives.

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).