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Front Cover: Reductive Carbon–Carbon Bond Forming Reactions with Carbonyls Mediated by Rh–H Complexes (Eur. J. Org. Chem. /2020)

Front Cover: Reductive Carbon–Carbon Bond Forming Reactions with Carbonyls Mediated by Rh–H Complexes (Eur. J. Org. Chem. /2020)

The Front Cover shows an effective synthetic method of a cholesterol absorption inhibitor, ezetimibe, by reductive Mannich reaction using a rhodium‐hydride complex. The back‐ground picture is the Japanese rock garden “karesansui” at Ryōan‐ji Temple in Kyoto (Japan). Karesansui expresses the spirit of “Wabi‐Sabi” that is meaning to discover new radiance (as various C–C bond formations) by reducing any wasteful and useless things. More information can be found in the doi.org/10.1002/ejoc.202001041Minireview by K. Sato, M. Omote et al.

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Kazuyuki Sato, Motoyuki Isoda, Atsushi Tarui, Masaaki Omote
doi.org/10.1002/ejoc.202001287

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Cover Feature: Isomerisation of Vinyl Sulfones for the Stereoselective Synthesis of Vinyl Azides (Eur. J. Org. Chem. /2020)

Cover Feature: Isomerisation of Vinyl Sulfones for the Stereoselective Synthesis of Vinyl Azides (Eur. J. Org. Chem. /2020)

The Cover Feature shows a kinetically controlled process where Green represents “go to Z (cis)” and Red represents “don’t go to E (trans)” for the isomerisation of a series of 3‐azido E‐vinyl sulfones. This process has been studied, and on treatment with the base DBU it has been found that, for most structural variations, these vinyl sulfones selectively generate Z‐vinyl azides. More information can be found in the doi.org/10.1002/ejoc.202001065Full Paper by P. Evans et al.

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Niall Collins, Robert Connon, Goar Sánchez‐Sanz, Paul Evans
doi.org/10.1002/ejoc.202001290

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5-Phenyl-1,3,4-oxadiazol-2(3H)-ones Are Potent Inhibitors of Notum Carboxylesterase Activity Identified by the Optimization of a Crystallographic Fragment Screening Hit

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: William Mahy, Nicky J. Willis, Yuguang Zhao, Hannah L. Woodward, Fredrik Svensson, James Sipthorp, Luca Vecchia, Reinis R. Ruza, James Hillier, Svend Kjær, Sarah Frew, Amy Monaghan, Magda Bictash, Patricia C. Salinas, Paul Whiting, Jean-Paul Vincent, E. Yvonne Jones, and Paul V. Fish
feedproxy.google.com/~r/acs/jmcmar/~3/rMxdt2NCOjI/acs.jmedchem.0c01391

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Completing the β,γ-CXY-dNTP Stereochemical Probe Toolkit: Synthetic Access to the dCTP Diastereomers and 31P and 19F NMR Correlations with Absolute Configurations

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The Journal of Organic Chemistry

The Journal of Organic Chemistry: Latest Articles (ACS Publications)
Authors: Pouya Haratipour, Corinne Minard, Maryam Nakhjiri, Amirsoheil Negahbani, Brian T. Chamberlain, Jorge Osuna, Thomas G. Upton, Michelle Zhao, Boris A. Kashemirov, and Charles E. McKenna
feedproxy.google.com/~r/acs/joceah/~3/Gm0Oc4xERrs/acs.joc.0c01204

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TBAF‐Catalyzed Tandem Synthesis of Triazolo[4,5‐c]quinolines at Ambient Temperature

TBAF‐Catalyzed Tandem Synthesis of Triazolo[4,5‐c]quinolines at Ambient Temperature

An efficient and metal‐free approach for 1H‐[1,2,3]triazolo[4,5‐c]quinolines have been developed based on tandem TBAF‐catalyzed intermolecular azide‐alkyne [3+2] cycloaddition of β‐(2‐aminoaryl)‐α,β‐ynones and TMS‐N3, followed by intramolecular dehydration annulation reaction. This transformation can smoothly proceed at ambient temperature to provide a broad range of functionalized 1H‐[1,2,3]triazolo[4,5‐c]quinolines in up to 95 % yield in 32 examples.

A mild, efficient and metal‐free synthetic method for 1H‐[1,2,3]triazolo[4,5‐c]quinolines has been developed via intermolecular [3+2] cycloaddition of β‐(2‐aminoaryl)‐α,β‐ynones and TMS‐N3, followed by intramolecular dehydration annulation sequential reactions. With 5 mmol‐% of TBAF as catalyst, the reaction can smoothly proceed in DMF at ambient temperature to afford a wide range of functionalized 1H‐[1,2,3]triazolo[4,5‐c]quinolines in good to excellent yields.

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Nan Sun, Han Yang, Kai Zheng, Liqun Jin, Baoxiang Hu, Zhenlu Shen, Xinquan Hu
doi.org/10.1002/ejoc.202001280

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Stereo‐ and Regioselective Construction of Spirooxindoles Having Continuous Spiral Rings via Asymmetric [3+2] Cyclization of 3‐Isothiocyanato Oxindoles with Thioaurone Derivatives

Stereo‐ and Regioselective Construction of Spirooxindoles Having Continuous Spiral Rings via Asymmetric [3+2] Cyclization of 3‐Isothiocyanato Oxindoles with Thioaurone Derivatives

A highly efficient enantioselective [3+2] cyclization of 3‐isothiocyanato oxindoles with thioaurone derivatives was developed for the synthesis of spirooxindoles containing continuous spiral ring structures.

A highly efficient enantioselective [3+2] cyclization of 3‐isothiocyanato oxindoles with thioaurone derivatives was explored for the synthesis of spirooxindoles containing continuous spiral ring structures. Three continuous spiral ring structures and three consecutive chiral centers (including two spiro quaternary stereocenters) were conveniently constructed at a time. In addition, an uncommon sulfur‐containing spirocyclic ring was constructed at the same time. The reaction went smoothly whether the alkenyl moiety of thioaurone derivatives was at 2‐position (up to 99 % yield, up to 99 % ee, up to > 20:1 dr) or at 3‐position (up to 96 % yield, up to 95 % ee, up to 12:1 dr).

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Hou‐Ze Gui, Zhe Meng, Zhan‐Shuai Xiao, Ze‐Ren Yang, Yin Wei, Min Shi
doi.org/10.1002/ejoc.202001146

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Diazanorbornene: A Valuable Synthon towards Carbocycles and Heterocycles

Diazanorbornene: A Valuable Synthon towards Carbocycles and Heterocycles

The present review summarizes the recent progress on desymmetrization of diazanorbornenes towards substituted/fused cyclopentanoids through catalyzed or uncatalyzed pathways.

Desymmetrization of meso compounds is well recognized as a powerful method for delivering biologically relevant molecular skeletons in a few synthetic steps. Heterobicyclic olefins are a class of meso compounds which exhibit exceptional reactivity due to their high ring strain originating from the unfavorable bond angles and eclipsing interactions. Extensive research was carried out towards the synthetic transformations of oxa‐, aza‐, and diazanorbornenes/norbornadienes for the synthesis of a wide variety of carbocycles and heterocycles in a single step, most importantly in a stereo‐ and chemo‐selective manner. This review summarizes the relevant aspects of diazanorbornene reactivity which will inspire the synthetic community for exploiting these highly strained bicyclic systems for the creation of extensive libraries of novel structurally and biologically interesting molecules. The review is divided into several sections based on the type of reactions that diazanorbornenes are subjected to.

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Preethanuj Preethalayam, E. Jijy, Praveen Prakash, Sarath Chand Sarngadharan, Ajesh Vijayan, K. V. Radhakrishnan, Jubi John
doi.org/10.1002/ejoc.202001131

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Thiourea–Tertiary Amine Promoted Cascade Catalysis: A Tool for Complexity Generation

Thiourea–Tertiary Amine Promoted Cascade Catalysis: A Tool for Complexity Generation

This review discusses the recent developments in the area of the thiourea–tert‐amine promoted, single catalyst‐relay cascade catalysis for the last fifteen years (2005–2020). This would give the readers the current state of the art of this important area in organic synthesis for the generation of chiral polycyclic systems. We assume that the current review would be a handle for the design and development, as well as further growth of this potentially greener approach.

The bifunctional organocatalyst promoted, relay‐cascade catalysis (use of a single catalyst capable of promoting each catalytic cycle in the designed cascade process) has been the hot area of research in recent times, as it enables the green synthesis of complex molecular architectures in an atom, cost, and step‐economic fashion. In this context we summarized the recent developments in the area of the thiourea–tert‐amine based cascade catalysis in the current review article. The discussion was divided into three subsections. double‐, triple‐, and quadruple cascades depending on the number of individual steps involved in the cascade process. In each type there are various combinations of reactions like Michael addition, aldol reaction, Henry reaction, Knoevenagel reaction, cyclization, trans‐esterifications etc. Divergent polycyclic structural frameworks have been achieved employing this cascade catalytic strategy as evidenced in this review. We assume that the current review article would be a handle for the design and development as well as further growth of this potential greener approach.

Wiley: European Journal of Organic Chemistry: Table of Contents
Authors: Soniya Gandhi, Vishnudas Sivadas, Beeraiah Baire
doi.org/10.1002/ejoc.202001114

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Design, Synthesis, and Biological Evaluation of Covalent Inhibitors of Focal Adhesion Kinase (FAK) against Human Malignant Glioblastoma

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Journal of Medicinal Chemistry

Journal of Medicinal Chemistry: Latest Articles (ACS Publications)
Authors: Bo Li, Yongliang Li, Céline Tomkiewicz-Raulet, Pascal Dao, Daniel Lietha, Expédite Yen-Pon, Zhiyun Du, Xavier Coumoul, Christiane Garbay, Mélanie Etheve-Quelquejeu, and Huixiong Chen
feedproxy.google.com/~r/acs/jmcmar/~3/zrv2Rqxnw2M/acs.jmedchem.0c01059

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Synthesis, Characterization, and In Silico Studies of Novel Spirooxindole Derivatives as Ecto-5′-Nucleotidase Inhibitors

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ACS Medicinal Chemistry Letters

ACS Medicinal Chemistry Letters: Latest Articles (ACS Publications)
Authors: Abida Ashraf, Zahid Shafiq, Muhammad Siraj Khan Jadoon, Muhammad Nawaz Tahir, Julie Pelletier, Jean Sevigny, Muhammad Yaqub, and Jamshed Iqbal
feedproxy.google.com/~r/acs/amclct/~3/b9od-P2GdSc/acsmedchemlett.0c00343

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Direct Synthesis of Pyrrolo[1,2-α]quinoxalines via Iron-Catalyzed Transfer Hydrogenation between 1-(2-Nitrophenyl)pyrroles and Alcohols

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The Journal of Organic Chemistry

The Journal of Organic Chemistry: Latest Articles (ACS Publications)
Authors: Simin Chun, Jiwon Ahn, Ramachandra Reddy Putta, Seok Beom Lee, Dong-Chan Oh, and Suckchang Hong
feedproxy.google.com/~r/acs/joceah/~3/-e5kDlxZ1zI/acs.joc.0c02145

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