Electrochemical Multicomponent Cascade Radical Process Enabling Synthesis of lodomethyl Spiropyrrolidinyl-Oxindoles

A novel electrochemical multicomponent cascade reaction of indole-tethered alkenes with CF_(3)SO_(2)Na and n-BuaNI has been developed,which enables the rapid assembly of spiropyrrolidinyl-oxindoles in good yields.The experimental results and DFT calculations suggest that this reaction proceeds through the oxidation of CF_(3)SO_(2)Na,radical coupling with alkene,spirocyclization,oxidation of sulfinate,iodide substitution,and water coupling.This strategy features mild reaction conditions,easy-to-handle reactants,and good chemical yields.This finding not only enriches the research contents of indole-tethered alkenes but also provides a green strategy for the construction of spiropyrrolidinyl-oxindoles compared with the existing methodologies.

Fluorine-containing drugs approved by the FDA in 2021

Nine new fluorine-containing drugs have been approved by the US Food and Drug Administration(FDA)in 2021,which are presented in this review article.These small molecular drugs feature aromatic fluorine,trifluoromethyl and chlorodifluoro groups.The therapeutic areas of these fluorine-containing drugs include multiple myeloma,lymphoma,HIV,chronic heart failure,chronic myeloid leukemia,(ANCA)-associated vasculitis,migraines,von Hippel-Lindau disease,and non-small cell lung cancer.The brief biological activities and the synthetic methods have been discussed in this review for each of these nine drugs.

Visible-light-irradiated tandem sulfonylation/cyclization of indole tethered alkenes for the synthesis of tetrahydrocarbazoles

A visible-light-mediated reaction of indole derivatives employing arylsulfonyl chlorides as sulfonyl surrogates has been developed,which proceeds via the sequence of reduction of sulfonyl chloride,sulfonylation,and intramolecular cyclization.This mild protocol transforms a diverse array of indole tethered alkenes and simple sulfonyl chlorides into highly valuable functionalized tetrahydrocarbazoles in good yields.This reaction is also suitable for gram-scale synthesis,which provides an efficient and green access to multi-substituted tetrahydrocarbazoles.

iNet:visual analysis of irregular transition in multivariate dynamic networks

Multivariate dynamic networks indicate networks whose topology structure and vertex attributes are evolving along time.They are common in multimedia applications.Anomaly detection is one of the essential tasks in analyzing these networks though it is not well addressed.In this paper,we combine a rare category detection method and visualization techniques to help users to identify and analyze anomalies in multivariate dynamic networks.We conclude features of rare categories and two types of anomalies of rare categories.Then we present a novel rare category detection method,called DIRAD,to detect rare category candidates with anomalies.We develop a prototype system called iNet,which integrates two major visualization components,including a glyph-based rare category identifier,which helps users to identify rare categories among detected substructures,a major view,which assists users to analyze and interpret the anomalies of rare categories in network topology and vertex attributes.Evaluations,including an algorithm performance evaluation,a case study,and a user study,are conducted to test the effectiveness of proposed methods.