N-叔丁氧羰基-L-丝氨酸 反应生成单叔丁基琥珀酸酯 参考文献:Radiolabeled Proteins For Diagnostic Or Therapeutic Use 标题:Radiolabeled Proteins For Diagnostic Or Therapeutic Use 摘要:具有特定结构的螯合化合物对于放射性标记靶向分子(如抗体)非常有用.可切割的连接剂将放射性核素金属螯合物连接到抗体上.放射性标记的抗体具有改善的生物分布特性,包括减少在肠道和肾脏内的定位.
专利号:US-2024092821-A1 优先权日:2020-03-31 标题:Synthesis of oligonucleotides and related compounds 发明人:ZHONG MINGHONG; JIN YI; GALA DINESH; PRHAVC MARIJA 权利人:JANSSEN BIOPHARMA INC 摘要:Methods of synthesizing oligonucleotides via new intermediates on a cleavable support having an azidomethyl moiety are disclosed. The method comprises multiple reaction cycles, each of which comprises sequential coupling a nucleoside or oligonucleotide subunit on a cleavable support having an azidomethyl moiety and a nucleoside phosphoramidite or an oligonucleotide phosphoramidite, capping, oxidation/thiolation and deblocking; followed by orthogonal cleavage of the azidomethyl support while keeping all other protecting groups intact. The method can be used in combination with a support moiety for either solid phase or liquid phase oligo synthesis. The soluble support facilitates homogeneous reactions and efficient separations by simple precipitation. The methods also provide novel intermediates useful in the synthesis of oligonucleotide conjugates.
专利号:US-11738092-B2 优先权日:2019-12-04 标题:Methods and compositions for synthesis of therapeutic nanoparticles 发明人:WYENT EMILY A; BLUMENFELD CARL M; LAMM ROBERT J 权利人:DANTARI INC 摘要:Improved methods and reactants for the chemical synthesis of therapeutic nanoparticles are provided. The nanoparticles comprise a polymeric core, to which is attached one or more homing molecules and one or more therapeutic agents. Improvements in speed, yield and purity are attained using the methods disclosed herein.
专利号:US-2013012706-A1 优先权日:2010-03-01 标 题 :Methods and Intermediates for the Synthesis of 4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazines 发明人:HUMMERSONE MARC GEOFFERY; COUSIN DAVID 权利人:PHARMINOX LTD; HUMMERSONE MARC GEOFFERY; COUSIN DAVID 摘要:The present invention provides a compound of general formula (II), or a salt or solvate thereof: n n n n n n n n n n n n wherein n A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein:n -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate;n nand its use in the synthesis of temozolomide and analogues thereof.
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-2021087191-A1 优先权日:2020-12-04 标 题 :SUBSTITUTED 3-ISOBUTYL-9,10-DIMETHOXY-1,3,4,6,7,11B-HEXAHYDRO-2H-PYRIDO[2,1-a]ISOQUINOLIN-2-OL COMPOUNDS, THEIR SYNTHESIS, AND USE THEREOF 发明人:MILLER DAVE ALAN; ELLENBERGER DANIEL J; GUNIC ESMIR; GIRARDET JEAN-LUC; SPANGENBERG ANGELA 权利人:DISPERSOL TECHNOLOGIES LLC 摘要:The invention relates to substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds, their synthesis, pharmaceutical compositions containing them, and methods of using them in the treatment of disorders benefiting from inhibition of vesicular monoamine transporter 2 (VMAT2).
专利号:US-2023355800-A1 优先权日:2019-12-04 标 题 :Methods and compositions for synthesis of therapeutic nanoparticles
[参考文献]: Ying Li, Et Al. One-Step And One-Pot-Two-Step Radiosynthesis Of Cyclo-Rgd-(18)F-Aryltrifluoroborate Conjugates For Functional Imaging. Am J Nucl Med Mol Imaging. 2013;3(1):44-56.
合成参考文献
参考文献:10.1055/s-0041-1737041 摘要:Hydrocarboxylation of Activated Olefins by Photoinduced Thiol Catalysis. Synfacts. 2021 Oct 19;17(11):1261. doi: 10.1055/s-0041-1737041.