- Straightforward installation of carbon-halogen, carbon-oxygen and carbon-carbon bonds within metal-organic frameworks (MOF) via palladium-catalysed direct C-H functionalization
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The straightforward C-H functionalization of UiO-67-dcppy materials was realized by a Pd-catalysed PSM. This novel protocol provides an efficient method for the synthesis of various functionalized MOFs, which have shown promising adsorbent ability in removing phenolic contaminates from water. This journal is
- Liu, Tao,Li, Da-Qiang,Wang, Si-Yu,Hu, Yong-Zhou,Dong, Xiao-Wu,Liu, Xin-Yuan,Che, Chi-Ming
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Read Online
- Fast and Tight Boronate Formation for Click Bioorthogonal Conjugation
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A new click bioorthogonal reaction system was devised to enable the fast ligation (kON≈340 m-1 s-1) of conjugatable derivatives of a rigid cyclic diol (nopoldiol) and a carefully optimized boronic acid partner, 2-methyl-5-carboxymethylphenylboronic acid. Using NMR and fluorescence spectroscopy studies, the corresponding boronates were found to form reversibly within minutes at low micromolar concentration in water, providing submicromolar equilibrium constant (Keq≈105-106 m-1). Efficient protein conjugation under physiological conditions was demonstrated with model proteins thioredoxin and albumin, and characterized by mass spectrometry and gel electrophoresis.
- Akgun, Burcin,Hall, Dennis G.
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supporting information
p. 3909 - 3913
(2016/03/19)
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- PROCESS FOR SYNTHESIZING A CETP INHIBITOR
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An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The next to last step of the process is the coupling of an oxazolidinone derivative and a triphenyl compound to provide the methyl ester of a compound which is hydrol
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Page/Page column 6
(2008/12/07)
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- Discovery of a novel series of biphenyl benzoic acid derivatives as potent and selective human β3-adrenergic receptor agonists with good oral bioavailability. Part I
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A novel class of biphenyl analogues containing a benzoic acid moiety based on lead compound 8i have been identified as potent and selective human β3 adrenergic receptor (β3-AR) agonists with good oral bioavailability and long plasma half-life. After further substituent effects were investigated at the terminal phenyl ring of lead compound 8i, we have discovered that more lipophilic substitution at the R position improved potency and selectivity. As a result of these studies, 10a and 10e were identified as the leading candidates with the best balance of potency, selectivity, and pharmacokinetic profiles. In addition, compounds 10a and 10e were evaluated to be efficacious for a carbachol-induced increase of intravesical pressure, such as an overactive bladder model in anesthetized dogs. This represents the first demonstrated result dealing with β3- AR agonists.
- Imanishi, Masashi,Tomishima, Yasuyo,Itou, Shinji,Hamashima, Hitoshi,Nakajima, Yutaka,Washizuka, Kenichi,Sakurai, Minoru,Matsui, Shigeo,Imamura, Emiko,Ueshima, Koji,Yamamoto, Takao,Yamamoto, Nobuhiro,Ishikawa, Hirofumi,Nakano, Keiko,Unami, Naoko,Hamada, Kaori,Matsumura, Yasuhiro,Takamura, Fujiko,Hattori, Kouji
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p. 1925 - 1944
(2008/12/20)
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- CETP INHIBITORS
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Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
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Page/Page column 63; 64
(2008/06/13)
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- Modular Solid-Phase Synthetic Approach to Optimize Structural and Electronic Properties of Oligoboronic Acid Receptors and Sensors for the Aqueous Recognition of Oligosaccharides
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This article describes the design and optimization of the first entirely modular, parallel solid-phase synthetic approach for the generation of well-defined polyamine oligoboronic acid receptors and fluorescence sensors for complex oligosaccharides. The s
- Stones, Duane,Manku, Sukhdev,Lu, Xiaosong,Hall, Dennis G.
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