- High-Throughput Screening of Reductive Amination Reactions Using Desorption Electrospray Ionization Mass Spectrometry
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This study describes the latest generation of a high-throughput screening system that is capable of screening thousands of organic reactions in a single day. This system combines a liquid handling robot with desorption electrospray ionization (DESI) mass spectrometry (MS) for a rapid reaction mixture preparation, accelerated synthesis, and automated MS analysis. A total of 3840 unique reductive amination reactions were screened to demonstrate the throughputs that are capable with the system. Products, byproducts, and intermediates were all monitored in full-scan mass spectra, generating a complete view of the reaction progress. Tandem mass spectrometry experiments were conducted to verify the identity of the products formed. The amine and electrophile reactivity trends represented in the data match what is expected from theory, indicating that the system accurately models the reaction performance. The DESI results correlated well with those generated using more traditional mass spectrometry techniques like liquid chromatography-mass spectrometry, validating the data generated by the system.
- Cooks, R. Graham,Ferreira, Christina R.,Li, Yangjie,Logsdon, David L.,Paschoal Sobreira, Tiago Jose,Thompson, David H.
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supporting information
p. 1647 - 1657
(2020/10/26)
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- BIS-AMINES, COMPOSITIONS, AND USES RELATED TO CXCR4 INHIBITION
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This disclosure relates bis-amine compounds disclosed herein and uses related to CXCR4 inhibition. In certain embodiments, the compounds have formula (I), salts, derivatives, and prodrugs thereof wherein, A is a bridging aryl or heterocyclyl and R1 and R2 are further disclosed herein. In certain embodiments, the disclosure contemplates pharmaceutical compositions comprising compounds disclosed herein. In certain embodiments, the disclosure relates to methods of treating or preventing CXCR4 related diseases or conditions by administering an effective amount of a compound disclosed herein to a subject in need thereof.
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Page/Page column 65
(2017/02/09)
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- Symmetrical bis-tertiary amines as novel CXCR4 inhibitors
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CXCR4 inhibitors are promising agents for the treatment of cancer metastasis and inflammation. A series of novel tertiary amine derivatives targeting CXCR4 were designed, synthesized, and evaluated. The central benzene ring linker and side chains were mod
- Bai, Renren,Liang, Zhongxing,Yoon, Younghyoun,Liu, Shuangping,Gaines, Theresa,Oum, Yoonhyeun,Shi, Qi,Mooring, Suazette Reid,Shim, Hyunsuk
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p. 340 - 350
(2016/05/24)
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- Highly efficient and eco-friendly synthesis of tertiary amines by reductive alkylation of aldehydes with secondary amines over a Pt nanowires catalyst
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Plentiful tertiary amine derivates are synthesized by direct formation of tertiary amines by the interaction of aldehydes with secondary amines over Pt nanowires under mild conditions. This method offers a green and rapid approach to transform secondary amines into various tertiary amines.
- Wu, Junjie,Lu, Shuanglong,Ge, Danhua,Gu, Hongwei
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p. 81395 - 81398
(2015/10/06)
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- Cesium carbonate-catalyzed reduction of amides with hydrosilanes
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Cesium carbonate has been found to be an effective catalyst for the reduction of tertiary carboxamides with the simple, commercially available PhSiH3 under solvent-free conditions. The catalytic system can effectively reduce a range of amides under relatively mild conditions (from room temperature to 80 C) to yield the corresponding amines in good to excellent yields (71-100%) and thus has the potential for practical applications.
- Xie, Weilong,Zhao, Mengdi,Cui, Chunming
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p. 7440 - 7444
(2014/04/03)
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- Novel bis-piperidinium and bis-pyrrolidinium compounds as versatile phase-transfer catalysts
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Syntheses and applications of new bis-piperidinium and bis-pyrrolidinium compounds as effective two-center phase-transfer catalysts are presented. Applications of these catalysts have been explored in etherification and N-alkylation reactions, and comparisons between these catalysts and traditional phase-transfer catalysts such as cetyltrimethylammonium bromide (CTAB) and 1-ethyl-3-methylimidazolium chloride (emim+Cl-) are presented. ARKAT USA, Inc.
- Saif, Muhammad Jawwad,Anwar, Jamil,Munawar, Munawar Ali,Kashif, Muhammad,Asghar, Muhammad Imran
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experimental part
p. 133 - 145
(2010/12/19)
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- Amines and Ammonium Compounds. CCXXVI. Stevens Rearrangement of Bisammonium Salts Containing a p-Xylylene Moiety
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p-Xylylenebisammonium salts containing phenacyl or acetonyl groups undergo Stevens rather than Sommelet rearrangement, regardless of reaction conditions.
- Karapetyan,Kocharyan,Babayan
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p. 1146 - 1149
(2007/10/03)
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