10540-39-3Relevant articles and documents
A highly efficient catalyst of a nitrogen-based ligand for the Suzuki coupling reaction at room temperature under air in neat water
Liu, Shiwen,Lv, Meiyun,Xiao, Daoan,Li, Xiaogang,Zhou, Xiuling,Guo, Mengping
, p. 4511 - 4516 (2014)
Glycine, as a kind of commercially available and inexpensive ligand, is used to prepare an air-stable and water-soluble catalyst for the Suzuki-Miyaura reaction in our study. In the presence of 0.1% [PdCl2(NH 2CH2COOH)2] as the catalyst, extremely excellent catalytic activity towards the Suzuki-Miyaura coupling of aryl halides containing the carboxyl group with various aryl boronic acids is observed at room temperature under air in neat water. the Partner Organisations 2014.
Green synthesis of biphenyl carboxylic acids via Suzuki–Miyaura cross-coupling catalyzed by a water-soluble fullerene-supported PdCl2 nanocatalyst
Liu, Wanyun,Zhou, Xiuming,Huo, Ping,Li, Jingbo,Mei, Guangquan
, p. 50 - 52 (2019)
A green synthesis of variously substituted biphenyl carboxylic acids was achieved through Suzuki–Miyaura cross-coupling of a bromobenzoic acid with an aryl boronic acid using a water-soluble fullerene-supported PdCl2 nanocatalyst (C60-TEGs/ PdCl2). Yields of more than 90% were obtained at room temperature in 4 h using 0.05 mol% catalyst and 2 equiv. K2CO3.
A focused fragment library targeting the antibiotic resistance enzyme - Oxacillinase-48: Synthesis, structural evaluation and inhibitor design
Akhter, Sundus,Lund, Bjarte Aarmo,Ismael, Aya,Langer, Manuel,Isaksson, Johan,Christopeit, Tony,Leiros, Hanna-Kirsti S.,Bayer, Annette
supporting information, p. 634 - 648 (2018/01/19)
β-Lactam antibiotics are of utmost importance when treating bacterial infections in the medical community. However, currently their utility is threatened by the emergence and spread of β-lactam resistance. The most prevalent resistance mechanism to β-lactam antibiotics is expression of β-lactamase enzymes. One way to overcome resistance caused by β-lactamases, is the development of β-lactamase inhibitors and today several β-lactamase inhibitors e.g. avibactam, are approved in the clinic. Our focus is the oxacillinase-48 (OXA-48), an enzyme reported to spread rapidly across the world and commonly identified in Escherichia coli and Klebsiella pneumoniae. To guide inhibitor design, we used diversely substituted 3-aryl and 3-heteroaryl benzoic acids to probe the active site of OXA-48 for useful enzyme-inhibitor interactions. In the presented study, a focused fragment library containing 49 3-substituted benzoic acid derivatives were synthesised and biochemically characterized. Based on crystallographic data from 33 fragment-enzyme complexes, the fragments could be classified into R1 or R2 binders by their overall binding conformation in relation to the binding of the R1 and R2 side groups of imipenem. Moreover, binding interactions attractive for future inhibitor design were found and their usefulness explored by the rational design and evaluation of merged inhibitors from orthogonally binding fragments. The best inhibitors among the resulting 3,5-disubstituted benzoic acids showed inhibitory potential in the low micromolar range (IC50 = 2.9 μM). For these inhibitors, the complex X-ray structures revealed non-covalent binding to Arg250, Arg214 and Tyr211 in the active site and the interactions observed with the mono-substituted fragments were also identified in the merged structures.
NOVEL SELECTIVE 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1
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Page/Page column 22; 24, (2017/02/09)
The present invention relates to novel selective 11-beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors and the use thereof to prevent age-induced skin structure and function defects.
AMIDE DERIVATIVES
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Page 54, (2010/02/06)
The invention concerns amide derivatives of Formula (Ia) wherein X is -NHCO- or -CONH-; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group
Ligandless palladium catalyzed reactions of arylboronic acids and sodium tetraphenylborate with aryl halides in aqueous media
Bumagin, Nikolai A.,Bykov, Victor V.
, p. 14437 - 14450 (2007/10/03)
Polyfunctional biaryls are prepared by a modified Suzuki cross-coupling reaction between arylboronic acids or sodium tetraphenylborate and aryl halides ArX. X = 1. Br. Cl in aqueous solvents or neat water using a phosphine-free palladium catalyst, and in the presence of bases (Na2CO3 or NaOH). All four phenyl groups of Ph4BNa participate ill the reaction. The reaction of Ph4BNa with aryl halides proceeds in water with high catalytic efficiency (250,000 catalytic cycles).
Reaction of Organoboron Compounds with Organic Halides in Aqueous Media, Catalyzed by "Ligand-Free" Palladium
Bumagin,Bykov
, p. 1925 - 1938 (2007/10/03)
The results of investigations of the reactions between aryllboric acids or sodium tetraphenylborate and organic halides in water and DMF- and acetone-water mixtures, catalyzed by palladium salts containing no phosphine ligands [Pd(OAc)2, PdCl2], are considered.
