625-36-5Relevant articles and documents
SYNTHESIS OF 7,7-DIMETHYLBICYCLO-OCTANE BY ACETYLATING A DICOBALTOHEXACARBONYL 4-METHYLPENT-3-EN-1-YNE-1 COMPLEX
Veretenov, A. L.,Gybin, A. S.,Smit, V. A.,Chertkov, V. A.,Shashkov, A. S.
, p. 1725 - 1733 (1989)
Dicobaltohexacarbonyl 4-methyl-pent-3-en-1-yne complexes have been acylated with acryloyl and crotonoyl tetrafluoroborates followed by methanolysis to make acylmethoxy adducts containing hem-dimethyl moieties.Conditions have been defined under which such adducts containing enone systems are selectively reduced to allyl alcohols with retention of the cobaltocarbonyl moieties.The latter can be converted by Quand-Poson reaction to the inaccessible polyfunctional derivatives of 7,7-dimethylbicyclooctane.
Preparation method of 3-chloropropionyl chloride
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Paragraph 0019-0021, (2021/10/27)
The invention provides a preparation method of 3-chloropropionyl chloride, wherein the preparation method comprises the following steps: mixing acrylic acid with a certain amount of catalyst, dropwise adding a certain amount of trichlorotoluene at a certain temperature under the protection of nitrogen, reacting for a period of time, and performing vacuum rectification to respectively obtain 3-chloropropionyl chloride and benzoyl chloride. The preparation method has the following beneficial effects: 1) acrylic acid and trichlorotoluene are adopted as raw materials, 3-chloropropionyl chloride is prepared in the presence of a catalyst, and benzoyl chloride with wide application is produced as a byproduct; the reaction route is environment-friendly, the process is simple, no emission is generated, and the requirement of atom economy is met; and the technical problem that toxic raw materials are used in the prior art is solved, and the technical problem that by-products polluting the environment are possibly generated in the prior art is also solved; and 2) the method is low in production cost, and in addition, the reaction route is combined with the specific reaction conditions, so that the yield of the obtained product is quite high and reaches 95% or above.
Development of Benzenesulfonamide Derivatives as Potent Glutathione Transferase Omega-1 Inhibitors
Xie, Yiyue,Tummala, Padmaja,Oakley, Aaron J.,Deora, Girdhar Singh,Nakano, Yuji,Rooke, Melissa,Cuellar, Matthew E.,Strasser, Jessica M.,Dahlin, Jayme L.,Walters, Michael A.,Casarotto, Marco G.,Board, Philip G.,Baell, Jonathan B.
, p. 2894 - 2914 (2020/04/08)
Glutathione transferase omega-1 (GSTO1-1) is an enzyme whose function supports the activation of interleukin (IL)-1β and IL-18 that are implicated in a variety of inflammatory disease states for which small-molecule inhibitors are sought. The potent reactivity of the active-site cysteine has resulted in reported inhibitors that act by covalent labeling. In this study, structure-activity relationship (SAR) elaboration of the reported GSTO1-1 inhibitor C1-27 was undertaken. Compounds were evaluated for inhibitory activity toward purified recombinant GSTO1-1 and for indicators of target engagement in cell-based assays. As covalent inhibitors, the kinact/KI values of selected compounds were determined, as well as in vivo pharmacokinetics analysis. Cocrystal structures of key novel compounds in complex with GSTO1-1 were also solved. This study represents the first application of a biochemical assay for GSTO1-1 to determine kinact/KI values for tested inhibitors and the most extensive set of cell-based data for a GSTO1-1 inhibitor SAR series reported to date. Our research culminated in the discovery of 25, which we propose as the preferred biochemical tool to interrogate cellular responses to GSTO1-1 inhibition.