193204-58-9Relevant academic research and scientific papers
A tri-aromatic amide hemicryptophane host: synthesis and acetylcholine binding
Makita, Yoshimasa,Katayama, Natsuki,Lee, Hsien-Han,Abe, Taro,Sogawa, Kento,Nomoto, Akihiro,Fujiwara, Shin-ichi,Ogawa, Akiya
, p. 5112 - 5115 (2016)
Hemicryptophanes have been designed to include endohedral functionalities in the cavity, giving molecular receptors and catalysts. In this study, a tri-aromatic amide hemicryptophane was synthesized. The host–guest interactions with various types of tetraalkylammonium salts were investigated. The structure of the partial inclusion complex in which an acetylcholine molecule was encapsulated within the hemicryptophane was characterized by NMR, X-ray crystal structure, and ESI-MS analysis.
Coordination chemistry of [Y(pypa)]-and comparison immuno-PET imaging of [44Sc]Sc- And [86Y]Y-pypa-phenyl-TRC105
Li, Lily,de Guadalupe Jaraquemada-Peláez, María,Aluicio-Sarduy, Eduardo,Wang, Xiaozhu,Barnhart, Todd E.,Cai, Weibo,Radchenko, Valery,Schaffer, Paul,Engle, Jonathan W.,Orvig, Chris
, p. 5547 - 5562 (2020/05/13)
Both scandium-44 and yttrium-86 are popular PET isotopes with appropriate half-lives for immuno-positron emission tomography (immuno-PET) imaging. Herein, a new bifunctional H4pypa ligand, H4pypa-phenyl-NCS, is synthesized, conjugate
CHELATORS AND METHODS OF MAKING AND USING SAME
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Paragraph 0087; 0115, (2020/10/09)
A chelating agent having the general formula (I) is provided (I) Metal chelates and constructs for carrying out targeted radionuclide therapy incorporating such chelating agents are provided. Methods of making and using the chelating agent, metal chelates and constructs for carrying out targeted radionuclide therapy, as well as diagnostic and therapeutic methods using such constructs, are provided.
Importance of the proximity and orientation of ligand-linkage to the design of cinnamate-GW9662 hybrid compounds as covalent PPAR agonists
Utsugi, Yuki,Kobuchi, Hirona,Kawamura, Yukio,Atito, Ahmed Salahelden Aboelhamd,Nagao, Masaya,Isoda, Hiroko,Miyamae, Yusaku
, (2019/06/05)
Covalent agonists of PPAR cause unique receptor conformational changes and behave as selective PPAR modulators, whereas there are few covalent agonists other than endogenous unsaturated fatty acids metabolites. Previously, we established a cell-based stra
Dissipative Catalysis with a Molecular Machine
Biagini, Chiara,Fielden, Stephen D. P.,Leigh, David A.,Schaufelberger, Fredrik,Di Stefano, Stefano,Thomas, Dean
supporting information, p. 9876 - 9880 (2019/07/04)
We report on catalysis by a fuel-induced transient state of a synthetic molecular machine. A [2]rotaxane molecular shuttle containing secondary ammonium/amine and thiourea stations is converted between catalytically inactive and active states by pulses of a chemical fuel (trichloroacetic acid), which is itself decomposed by the machine and/or the presence of additional base. The ON-state of the rotaxane catalyzes the reduction of a nitrostyrene by transfer hydrogenation. By varying the amount of fuel added, the lifetime of the rotaxane ON-state can be regulated and temporal control of catalysis achieved. The system can be pulsed with chemical fuel several times in succession, with each pulse activating catalysis for a time period determined by the amount of fuel added. Dissipative catalysis by synthetic molecular machines has implications for the future design of networks that feature communication and signaling between the components.
Improved synthesis of the bifunctional chelator p-SCN-Bn-HOPO
Bhupathiraju, N.V.S. Dinesh K.,Younes, Ali,Cao, Minhua,Ali, Jafar,Cicek, Huseyin T.,Tully, Kathryn M.,Ponnala, Shashikanth,Babich, John W.,Deri, Melissa A.,Lewis, Jason S.,Francesconi, Lynn C.,Drain, Charles Michael
supporting information, p. 6866 - 6871 (2019/07/22)
The bifunctional ligand p-SCN-Bn-HOPO, which has four 1,2-hydroxypyridinone groups on a spermine backbone with an isothiocyanate linker, has been shown to be an efficient and stable chelator for Zr(iv) and, more importantly, the radioisotope 89Zr for use in radiolabeling antibodies for positron emission tomography (PET) imaging. Previous studies of 89Zr-HOPO-trastuzumab in mice showed low background, good tumor to organ contrast, and very low bone uptake which show p-SCN-Bn-HOPO to be an important next-generation bifunctional chelator for radioimmunoPET imaging with 89Zr. However, the reported synthesis of p-SCN-Bn-HOPO involves nine steps and multiple HPLC purifications with an overall yield of about 1.4%. Herein we report an improved and efficient synthesis of p-SCN-Bn-HOPO in four steps with 14.3% overall yield which will improve its availability for further biological studies and wider application in PET imaging. The new synthetic route also allows variation in linker length and chemistries which may be helpful in modifying in vivo clearance behaviors of future agents.
A method of preparing P ethylamine
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, (2017/04/14)
The invention discloses a preparation method of p-aminophenylethylamine, belonging to the technical field of organic synthesis. The technical scheme is as follows: the preparation method comprises the following steps: by using p-nitrophenylethanol as a raw material, carrying out catalytic hydrogenation to reduce the para-position nitro groups of the p-nitrophenylethanol into amino groups, carrying out Boc acid anhydride protection on the para-position nitro groups, carrying out substitution reaction on hydroxy groups with sulfonyl chloride compounds to obtain sulfonic acid compounds, aminating, and finally, removing Boc groups to obtain the p-aminophenylethylamine. The preparation process is simple and easy to implement, and has the advantages of cheap and accessible raw materials, higher reaction efficiency and favorable repetitiveness.
In situ deprotection and dynamic covalent assembly using a dual role catalyst
Wei,Furgal,Scott
supporting information, p. 3874 - 3877 (2017/04/06)
Utilization of constituent molecular precursors bearing covalently coreactive functional groups for self-assembly risks premature reaction, impeding synthetic and purification efforts. To prevent premature amine-aldehyde condensation for oligomers bearing both groups, we employ a dual-role Lewis acid catalyst for both in situ acetal deprotection and subsequent imine exchange, effecting oligomer assembly.
