K2S2O8-mediated acylarylation of unactivated alkenes via acyl radical addition/C–H annulation cascade of N-allyl-indoles with silver cocatalysis
TL;DR: A silver-catalyzed, K2S2O8-mediated protocol to access the regioselective acylarylation of unactivated alkenes was reported.
Abstract: A silver-catalyzed, K2S2O8-mediated protocol to access regioselective acylarylation of unactivated alkenes was developed. The reaction between N-allyl-indoles and α-oxocarboxylic acids proceeded smoothly and involved an acyl radical addition/C–H cyclization cascade. The protocol showed a broad substrate scope and good tolerance of functional groups. The reaction proceeded with both internal and terminal alkenes to furnish many functional pyrrolo[1,2-a]indoles bearing the ketone carbonyl group, and this feature also provides the potential to construct structurally complex N-containing heterocycles.
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TL;DR: An efficient and practical visible-light-induced acylation/cyclization of active alkenes with acyl oxime derivatives for constructing acylated indolo/benzimidazo-[2,1,a]isoquinolin-6(5H) ones is developed.
Abstract: Nitrogen heterocycles, especially polycyclic compounds, are significant skeletons in valuable molecules. Herein, we developed an efficient and practical visible-light-induced acylation/cyclization of active alkenes with acyl oxime derivatives for constructing acylated indolo/benzimidazo-[2,1,a]isoquinolin-6(5H) ones. This reaction was compatible with various functional groups and a series of fused indole/imidazole skeletons were prepared in up to 95% yield at room temperature.
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TL;DR: A metal-free polychloromethyl radical-initiated cyclization of unactivated alkenes was developed using CH2Cl2 and CHCl3 as the di-and trichloromethsyl radical sources as discussed by the authors .
Abstract: A metal-free polychloromethyl radical-initiated cyclization of unactivated alkenes was developed using CH2Cl2 and CHCl3 as the di- and trichloromethyl radical sources. Variously substituted N-allyl-indoles were successfully transformed into the corresponding C2-(di- and trichloromethyl) pyrrolo[1,2-a]indoles in moderate to good yields. This reaction has a broad substrate scope and good functional group tolerance. Dibromomethylated products can also be obtained using CH2Br2 under standard conditions.
5 citations
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TL;DR: In this article , a simple metal and additive-free approach for the assembly of 5-trifluoromethyl-1,2,4-triazoles via only heating-induced decarboxylative cyclization of readily available trifluoroacetimidohydrazides and α-oxocarboxylic acids has been developed.
Abstract: A simple metal and additive-free approach for the assembly of 5-trifluoromethyl-1,2,4-triazoles via only heating-induced decarboxylative cyclization of readily available trifluoroacetimidohydrazides and α-oxocarboxylic acids has been developed. In this protocol, the rarely reported tetrahedral carboxylic acids intermediate could be in-situ generated and undergo subsequent decarboxylation to afford the target heterocycle products.
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TL;DR: In this article, a review of the development of utilizing functionalities as directing groups for the construction of C-C and C-hetero bonds via C-H activation using various transition metal catalysts is presented.
Abstract: Transition metal-catalyzed direct functionalization of C–H bonds is one of the key emerging strategies that is currently attracting tremendous attention with the aim to provide alternative environmentally friendly and efficient ways for the construction of C–C and C–hetero bonds. In particular, the strategy involving regioselective C–H activation assisted by various functional groups shows high potential, and significant achievements have been made in both the development of novel reactions and the mechanistic study. In this review, we attempt to give an overview of the development of utilizing the functionalities as directing groups. The discussion is directed towards the use of different functional groups as directing groups for the construction of C–C and C–hetero bonds via C–H activation using various transition metal catalysts. The synthetic applications and mechanistic features of these transformations will be discussed, and the review is organized on the basis of the type of directing groups and the type of bond being formed or the catalyst.
1,238 citations
TL;DR: The present paper focuses on Bleomycin, a single-celled bacterium which has shown the versatility of its ability to Binding Protein and Transport Proteins, and its application in the Response to Enediyness.
Abstract: 1. Introduction 7392. Bleomycin 7392.1. Discovery and Biological Activities 7392.2. Clinical Resistance 7402.2.1. Bleomycin Hydrolase 7412.2.2. Enhanced DNA Repair 7422.2.3. Bleomycin Binding Protein 7422.2.4. Other Mechanisms 7432.3. Resistance by the Producing Organisms 7432.3.1. Bleomycin N-Acetyltranferase (BlmB) 7432.3.2. Bleomycin Binding Protein (BlmA) 7432.3.3. Transport Proteins 7443. EnediynessNine-Membered Enediyne CoreSubfamily7443.1. Discovery and Biological Activities 7453.2. Resistance by the Producing Organisms 7463.2.1. Apo-Protein 7463.2.2. DNA Repair 7473.2.3. Transport 7474. EnediynessTen-Membered Enediyne CoreSubfamily7484.1. Discovery and Biological Activities 7484.2. Clinical Resistance 7504.3. Resistance by the Producing Organisms 7515. Mitomycin 7525.1. Discovery and Biological Activities 7525.2. Clinical Resistance 7545.3. Resistance by the Producing Organisms 7546. Perspective 7547. Abbreviations 7558. Acknowledgment 7559. References 755
472 citations
TL;DR: This paper aims to demonstrate the efforts towards in-situ applicability of EMMARM, as to provide real-time information about concrete mechanical properties such as E-modulus and compressive strength in the response of the immune system to EMTs.
Abstract: the NSFC (Nos. 21272100);Program for Changjiang Scholars and Innovative Research Team in University (PCSIRT: IRT1138);Research Fund for the Doctoral Program of Higher Education of China (Nos. 20100211120014)
376 citations
TL;DR: In this article, the design principles underpinning the development of electrochemical diazidation, dichlorination, and halotrifluoromethylation of alkenes were described.
Abstract: Given its many distinct characteristics, electrochemistry represents an attractive approach to meet the prevailing trends in organic synthesis. In particular, electrocatalysis—a process that integrates electrochemistry and small-molecule catalysis—has the potential to substantially improve the scope of synthetic electrochemistry and provide a wide range of useful transformations. Recently, we have demonstrated new catalytic approaches that combine electrochemistry and redox-metal catalysis for the oxidative difunctionalization of alkenes to access a diverse array of vicinally functionalized structures. This Perspective details our design principles underpinning the development of electrochemical diazidation, dichlorination, and halotrifluoromethylation of alkenes, which were built on foundational work by others in the areas of synthetic electrochemistry, radical chemistry, and transition-metal catalysis. The introduction of redox-active Mn catalysts allows the generation of radical intermediates from read...
364 citations