87849-22-7Relevant academic research and scientific papers
Biaryl Ketones by Suzuki–Miyaura Cross-Coupling of Organotrifluoroborates and Acyl Chlorides
Forbes, Alaina M.,Meier, G. Patrick,Jones-Mensah, Ebenezer,Magolan, Jakob
, p. 2983 - 2987 (2016/07/11)
A procedure for the synthesis of biaryl ketones by a palladium-catalyzed Suzuki–Miyaura cross-coupling reaction between phenyltrifluoroborates and benzoyl chlorides is described. Organotrifluoroborates are unique to other cross-coupling reagents as they have a high functional-group tolerance and are moisture-stable. Moderate to excellent yields were obtained for all substrates tested.
THERAPEUTIC INHIBITORY COMPOUNDS
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Page/Page column 121, (2015/07/16)
The invention provides compounds of Formula I and Formula II: A-B-C-D-E-F-G-J (I) C-D-E-F-G-J (II) wherein A, B, C, D, E, F, G, and J have any of the values defined in the specification, and salts thereof. The compounds are useful for inhibiting plasma kallikrein, and for treating a disease or condition in an animal where inhibition of plasma kallikrein is indicated.
3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors
Faridoon,Hussein, Waleed M.,Vella, Peter,Islam, Nazar Ul,Ollis, David L.,Schenk, Gerhard,McGeary, Ross P.
, p. 380 - 386 (2012/02/04)
The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.
A phosphine-free carbonylative cross-coupling reaction of aryl iodides with arylboronic acids catalyzed by immobilization of palladium in MCM-41
Cai, Mingzhong,Peng, Jian,Hao, Wenyan,Ding, Guodong
experimental part, p. 190 - 196 (2011/03/20)
The phosphine-free heterogeneous carbonylative cross-coupling of aryl iodides with arylboronic acids under an atmospheric pressure of carbon monoxide was achieved in anisole at 80 °C in the presence of a 3-(2-aminoethylamino) propyl-functionalized MCM-41-immobilized palladium(ii) complex [MCM-41-2N-Pd(ii)], yielding a variety of unsymmetrical biaryl ketones in good to high yield. This heterogeneous palladium catalyst exhibited higher activity and selectivity than PdCl2(PPh3)2, can be recovered and recycled by a simple filtration of the reaction solution, and used for at least 10 consecutive trials without any decrease in activity. Our system not only avoids the use of phosphine ligands, but also solves the basic problem of palladium catalyst recovery and reuse.
Laser Flash Photolysis of tert-Butyl Aroylperbenzoates: Kinetics of the Singlet and Triplet States and the Aroylphenyl Radicals
Shah, Bipin K.,Neckers, Douglas C.
, p. 1830 - 1835 (2007/10/03)
tert-Butyl aroylperbenzoates (1-4) were studied by laser flash photolysis (LFP). LFP (380 nm, pulse width ～350 fs) of 2 and 3 allowed direct observation of their singlet states, which showed broad absorption (λmax ～ 625 nm; τ ～ 20 and ～7.9 ps, respectively). The triplet state of each (λmax ～ 530-560 nm) rapidly dissociates by O-O cleavage as indicated by the short triplet lifetimes (e.g., triplet lifetime of 3 ～0.74 ns). The ～550 nm absorption obtained from the 355 nm LFP (pulse width ～7 ns) of 1, 2, and 4 has been assigned to the corresponding aroylphenyl radicals. Two representative radicals (4-benzoylphenyl 5 and 3-(4′-methylbenzoyl)phenyl 6) investigated in detail showed solvent-dependent lifetimes. Absolute bimolecular rate constants of reactions of these radicals with various quenchers including double-bond-containing monomers have been observed to range from 7.56 × 107 to 1.68 × 109 M-1 s-1 in CCl4 at room temperature. A possible structure of the aroylphenyl radicals and the transition responsible for the 550 nm absorption are discussed.
Synthesis, Crystal Structures, and Laser Flash Photolysis of tert-Butyl Aroylperbenzoates
Shah, Bipin K.,Neckers, Douglas C.
, p. 8368 - 8372 (2007/10/03)
tert-Butyl aroylperbenzoates (1-7) were synthesized. Single-crystal structures for 2 and 5 show that the perester and benzophenone carbonyl groups are almost coplanar in each. Laser flash photolysis (LFP, λex = 355 nm) of 1-5 in CCl4
