175278-37-2Relevant articles and documents
Method for preparing N-sulfonyl tetrahydropyrrole compound by using gold complex
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Paragraph 0054-0059, (2021/07/17)
The invention relates to a method for preparing an N-sulfonyl tetrahydropyrrole compound by using a gold complex, which comprises the following step of: reacting a sulfonamide compound and a tetrahydrofuran compound as raw materials with a gold complex containing an ortho-carborane Schiff base ligand as a catalyst at room temperature to obtain the N-sulfonyl tetrahydropyrrole compound. Compared with the prior art, the method has the advantages that the gold complex containing the ortho-carborane Schiff base ligand is adopted as the catalyst, the sulfonamide compound and the tetrahydrofuran compound can be catalyzed to react under the room temperature condition to prepare the N-sulfonyl tetrahydropyrrole compound, the usage amount of the catalyst is low, the reaction condition is mild, the reaction rate is high, the product yield is high, the substrate is high in universality, the raw materials are cheap and easy to obtain, and the method has a wide application prospect in industry.
Iodine-catalyzed sulfonylation of sulfonyl hydrazides with: Tert -amines: A green and efficient protocol for the synthesis of sulfonamides
Chen, Jinyang,Han, Xiaoran,Mei, Lan,Liu, Jinchuan,Du, Kui,Cao, Tuanwu,Li, Qiang
, p. 31212 - 31216 (2019/10/19)
This study provides a direct, sustainable and eco-friendly method for the synthesis of various sulfonamides via the sulfonylation of sulfonyl hydrazides with tert-amines. The method utilizes sulfonyl hydrazides to oxidize and couple with tertiary amines through selective cleavage of C-N bonds. In this reaction, molecular iodine was used as the catalyst and t-butyl hydroperoxide was used as the oxidant.
High-Throughput Screening and Hit Validation of Extracellular-Related Kinase 5 (ERK5) Inhibitors
Myers, Stephanie M.,Bawn, Ruth H.,Bisset, Louise C.,Blackburn, Timothy J.,Cottyn, Betty,Molyneux, Lauren,Wong, Ai-Ching,Cano, Celine,Clegg, William,Harrington, Ross. W.,Leung, Hing,Rigoreau, Laurent,Vidot, Sandrine,Golding, Bernard T.,Griffin, Roger J.,Hammonds, Tim,Newell, David R.,Hardcastle, Ian R.
supporting information, p. 444 - 455 (2016/08/16)
The extracellular-related kinase 5 (ERK5) is a promising target for cancer therapy. A high-throughput screen was developed for ERK5, based on the IMAP FP progressive binding system, and used to identify hits from a library of 57-617 compounds. Four distinct chemical series were evident within the screening hits. Resynthesis and reassay of the hits demonstrated that one series did not return active compounds, whereas three series returned active hits. Structure-activity studies demonstrated that the 4-benzoylpyrrole-2-carboxamide pharmacophore had excellent potential for further development. The minimum kinase binding pharmacophore was identified, and key examples demonstrated good selectivity for ERK5 over p38α kinase.
