CAS: 137219-37-5; (S)-N-((R)-1-(((3S,6R,7S,10R,11S,15S,17S,20S,25As)-10-((S)-Sec-Butyl)-11-Hydroxy-20-Isobutyl-15-Isopropyl-3-(4-Methoxybenzyl)-2,6,17-Trimethyl-1,4,8,13,16,18,21-Heptaoxodocosahydro-15H-Pyrrolo[2,1-F][1,15]Dioxa[4,7,10,20]Tetraazacyclotricosin-7-yl)Amino)-

上下游产品

1-pyruvyl-L-proline 1-(tert-butoxycarbonyl)-L-proline benzyl (2S)-2-pyrrolidinecarboxylate hydr°Chloride H-Pro-OTce

📜(3S,4R,5S)-Boc-Isostatine Methyl Ester置于palladium On Activated Charcoal 咪唑,盐酸,4-二甲氨基吡啶,Sodium Hydroxide,N-羟基-7-氮杂苯并三氮唑,N-<(1H-Benzotriazol-1-yl)(Dimethylamino)Methylene>-N-Methylmethanaminium Hexafluorophosphate N-Oxide,N-<(Dimethylamino)-1H-1,2,3-Triazolo<4,5-B>Pyridin-1-Ylmethylene>-N-Methylmethanaminium Hexafluorophosphate N-Oxide,Ammonium Acetate,氢气,(Benzotriazo-1-Yloxy)Tris(Dimethylamino)Phosphonium Hexafluorophosphate,1-羟基苯并三唑,4-(Dimethylamino)Pyridinium Trifluoroacetate,N,N-二异丙基乙胺,N,N'-二环己基碳二亚胺,Bromo-Tris(1-Pyrrolidinyl)Phosphonium Hexafluorophosphate,三氟乙酸,N,N'-二异丙基碳二亚胺,锌体系中,用 四氢呋喃,1,4-二氧六环,甲醇,二氯甲烷,氯仿,N,N-二甲基甲酰胺,乙腈 用作溶剂,-5.0~25.0 °C,101.33 Kpa 条件下,反应 223.16H,反应生成去氢代代宁b
参考文献:脱氢肌苷b的全合成.在溶液中肽合成中使用use盐和ph盐偶联剂.
标题:脱氢肌苷b的全合成.在溶液中肽合成中使用use盐和ph盐偶联剂.
摘要:描述了二氢肌动蛋白a和脱氢肌苷b的新的总合成.在该大环二肽家族的所有成员中,后者的双氢精蛋白具有最高的抗增殖活性.它是通过将pyr-Pro-Oh侧链与双精胺a偶联而制得的,而双精胺a本身是通过两种新途径合成的.其中一个是基于线性直链的七肽肽的精制而成,该肽掺入了双氢精蛋白侧链的第一个氨基酸(R)-N(me)-Leu.对该线性前体的氨基和羧基末端进行脱保护,然后进行大环化,得到了双联蛋白a的保护衍生物.第二种方法涉及从缺少(R)-N(me)-Leu的线性六肽中合成boc保护的双联蛋白大环.从大环中除去boc基团,然后将其与boc-(R)-N(me)-Leu-Oh偶联,得到boc-地精a.第二种策略的总收率要高得多(27%比4 (对于第一次合成,%),但是两者都允许制备与天然样品相同的合成二氢肌酐a.大量使用了基于phospho和铀盐的偶联剂,例如bop,Pybrop,Pyaop,Hbtu和h
Doi:10.1021/jo961932H

专利信息

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-12441733-B2
优先权日:2018-03-26
标题:Substituted 2,4-dioxotetrahydropyrimidines as intermediates in the synthesis of bruton's tyrosine kinase inhibitors
发明人：ARISTA LUCA; HEBACH CHRISTINA; HOLLINGWORTH GREGORY JOHN; HOLZER PHILIPP; IMBACH-WEESE PATRICIA; LORBER JULIEN; MACHAUER RAINER; SCHMIEDEBERG NIKO; VULPETTI ANNA; ZOLLER THOMAS
权利人:NOVARTIS AG
摘要:The invention relates to compounds of the formulae (I), (III), (IIIa), (XXIa), (XXIII), and/or (XLVI)or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined in the specification; to intermediates in the preparation of the compounds, to pharmaceutical compositions comprising the compounds and to use of the compounds in the treatment of disease.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2024382626-A1
优先权日:2023-05-16
标题 :Irradiation amenable liposomal dye aggregates and methods of synthesis and use thereof
发明人：PORTER TYRONE; STERN NOAH; TUNNELL JAMES; SHRESTHA BINITA
权利人:UNIV TEXAS
摘要:The present invention provides lipid nanoparticles that are amenable to an irradiation at a wavelength at or above 850 nm, have an absorption peak from about 850 to 1100 nm wavelength, and comprise a high transition temperature lipid and a dye (e.g., a J-aggregate of a dye). In some embodiments, the dye (e.g., J-aggregate of the dye) is encapsulated in the lipid nanoparticle. In various embodiments, the present invention also relates to compositions comprising said lipid nanoparticles and methods of generating said lipid nanoparticles and compositions thereof. The present invention further relates to methods relating to the said lipid nanoparticles for imaging, detection, and treatment of diseases or disorders (e.g., phototherapy) in a subject.