16156-59-5Relevant articles and documents
THE MECHANISM OF THE REACTION OF ARYLOXYTRIMETHYLSTANNANE WITH METHANESULFONYL CHLORIDE
Kozuka, Seizi,Yamaguchi, Shigeru,Tagaki, Waichiro
, p. 1299 - 1300 (1981)
A kinetic study has been conducted for the reaction of aryloxytrimethylstannane with methanesulfonyl chloride.Substituent effect was found to be dependent on the solvent and obscure solvent effect was observed.A mechanism has been suggested involving nearly concerted four-center transition state.
New preparative method of aryl tosylates by using organobismuth reagents
Sakurai, Naoto,Mukaiyama, Teruaki
, p. 928 - 929 (2007)
A new method for the preparation of aryl tosylates by using pentavalent bismuth is described. Treatment of 10-arylphenothiabismine 5,5-dioxides, m-chloroperoxybenzoic acid (MCPBA) and p-toluenesulfonic acid monohydrate in dichloromethane affords aryl tosy
Fluorovinylsulfones and -Sulfonates as Potent Covalent Reversible Inhibitors of the Trypanosomal Cysteine Protease Rhodesain: Structure-Activity Relationship, Inhibition Mechanism, Metabolism, and in Vivo Studies
Jung, Sascha,Fuchs, Natalie,Johe, Patrick,Wagner, Annika,Diehl, Erika,Yuliani, Tri,Zimmer, Collin,Barthels, Fabian,Zimmermann, Robert A.,Klein, Philipp,Waigel, Waldemar,Meyr, Jessica,Opatz, Till,Tenzer, Stefan,Distler, Ute,R?der, Hans-Joachim,Kersten, Christian,Engels, Bernd,Hellmich, Ute A.,Klein, Jochen,Schirmeister, Tanja
, p. 12322 - 12358 (2021/09/02)
Rhodesain is a major cysteine protease of Trypanosoma brucei rhodesiense, a pathogen causing Human African Trypanosomiasis, and a validated drug target. Recently, we reported the development of α-halovinylsulfones as a new class of covalent reversible cysteine protease inhibitors. Here, α-fluorovinylsulfones/-sulfonates were optimized for rhodesain based on molecular modeling approaches. 2d, the most potent and selective inhibitor in the series, shows a single-digit nanomolar affinity and high selectivity toward mammalian cathepsins B and L. Enzymatic dilution assays and MS experiments indicate that 2d is a slow-tight binder (Ki = 3 nM). Furthermore, the nonfluorinated 2d-(H) shows favorable metabolism and biodistribution by accumulation in mice brain tissue after intraperitoneal and oral administration. The highest antitrypanosomal activity was observed for inhibitors with an N-terminal 2,3-dihydrobenzo[b][1,4]dioxine group and a 4-Me-Phe residue in P2 (2e/4e) with nanomolar EC50 values (0.14/0.80 μM). The different mechanisms of reversible and irreversible inhibitors were explained using QM/MM calculations and MD simulations.
Sulfonyl Fluoride Synthesis through Electrochemical Oxidative Coupling of Thiols and Potassium Fluoride
Laudadio, Gabriele,Bartolomeu, Aloisio De A.,Verwijlen, Lucas M. H. M.,Cao, Yiran,De Oliveira, Kleber T.,No?l, Timothy
supporting information, p. 11832 - 11836 (2019/08/26)
Sulfonyl fluorides are valuable synthetic motifs for a variety of applications, among which sulfur(VI) fluoride exchange-based "click chemistry" is currently the most prominent. Consequently, the development of novel and efficient synthetic methods to access these functional groups is of great interest. Herein, we report a mild and environmentally benign electrochemical approach to prepare sulfonyl fluorides using thiols or disulfides, as widely available starting materials, in combination with KF, as an inexpensive, abundant and safe fluoride source. No additional oxidants nor additional catalysts are required and, due to mild reaction conditions, the reaction displays a broad substrate scope, including a variety of alkyl, benzyl, aryl and heteroaryl thiols or disulfides.
Alkali antioxidant containing Paichongding aqueous suspending agent
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Paragraph 0058-0061, (2018/03/23)
The invention relates to an alkali antioxidant containing paichongding aqueous suspending agent which comprises the following components in parts by weight: 40-50 parts of paichongding, 20-25 parts ofa sulfo-phenol antioxidant, 2-4 parts of potassium sorb
