Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b01749
James Sanderson
Shared posts
11 Mar 08:38
[ASAP] Allosteric Modulator Discovery: From Serendipity to Structure-Based Design
by Shaoyong Lu, Xinheng He, Duan Ni, Jian Zhang
08 Mar 14:05
[ASAP] Emerging Trends in Flow Chemistry and Applications to the Pharmaceutical Industry
by Andrew R. Bogdan, Amanda W. Dombrowski
Journal of Medicinal Chemistry
DOI: 10.1021/acs.jmedchem.8b01760
pgecheverria, Patricia R. Salamanca likes this
06 Mar 11:07
HIV-1 remission following CCR5Δ32/Δ32 haematopoietic stem-cell transplantation
by Ravindra K Gupta
HIV-1 remission following CCR5Δ32/Δ32 haematopoietic stem-cell transplantation
HIV-1 remission following CCR5Δ32/Δ32 haematopoietic stem-cell transplantation, Published online: 05 March 2019; doi:10.1038/s41586-019-1027-4
HIV-1 remission following CCR5Δ32/Δ32 haematopoietic stem-cell transplantation
25 Feb 07:57
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Med. Chem. Commun., 2018, Accepted Manuscript
DOI: 10.1039/C8MD00327K, Research Article
DOI: 10.1039/C8MD00327K, Research Article
Aaron Keeley, Peter Abranyi-Balogh, George M Keserû
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed...
The content of this RSS Feed (c) The Royal Society of Chemistry
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads. The analysis of theoretical and experimental descriptors revealed...
The content of this RSS Feed (c) The Royal Society of Chemistry
23 Feb 12:21
Open Access
  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.
Design and characterization of a heterocyclic electrophilic fragment library for the discovery of cysteine-targeted covalent inhibitors
Med. Chem. Commun., 2019, 10,263-267
DOI: 10.1039/C8MD00327K, Research Article
DOI: 10.1039/C8MD00327K, Research Article
Open Access  This article is licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported Licence.
A. Keeley, P. Ábrányi-Balogh, G. M. Keserű
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads.
The content of this RSS Feed (c) The Royal Society of Chemistry
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads.
The content of this RSS Feed (c) The Royal Society of Chemistry
22 Feb 09:55
Recent Trends in Iron‐Catalyzed Reactions towards the Synthesis of Nitrogen‐Containing Heterocycles
by Radhakrishnan Sreedevi,
Salim Saranya,
K. R. Rohit,
Gopinathan Anilkumar
Abstract
Heterocycles are generally biologically active compounds and find widespread applications in medicinal chemistry, agricultural science and the fine chemical industry. For the synthesis and functionalization of heterocycles, great efforts have been ascribed over the past decades. The syntheses of heterocyclic compounds are significant due to their diverse biological activity. Recently, iron‐catalyzed reactions have experienced remarkable progress in the synthesis of heterocycles. This review summarizes recent trends in the iron‐catalyzed synthesis of nitrogen‐containing heterocyclic compounds.
22 Feb 09:37
[ASAP] Silver Effect in Regiodivergent Gold-Catalyzed Hydroaminations
by Marcos Veguillas, Georgina M. Rosair, Magnus W. P. Bebbington, Ai-Lan Lee
ACS Catalysis
DOI: 10.1021/acscatal.9b00249
longlenovo zheng, yjdlut likes this
13 Feb 11:59
[ASAP] Structural Simplification of Natural Products
by Shengzheng Wang, Guoqiang Dong, Chunquan Sheng
Chemical Reviews
DOI: 10.1021/acs.chemrev.8b00504
123rliu likes this
29 Mar 18:14
[ASAP] Synthesis of Alkyl Indium Reagents by Using Unactivated Alkyl Chlorides and Their Applications in Palladium-Catalyzed Cross-Coupling Reactions with Aryl Halides
by Bing-Zhi Chen, Man-Ling Zhi, Chuang-Xin Wang, Xue-Qiang Chu, Zhi-Liang Shen and Teck-Peng Loh
Organic Letters
DOI: 10.1021/acs.orglett.8b00441
longzhi zhu, 大河弯不弯 and -1 others like this
29 Mar 18:01
[ASAP] Copper-Catalyzed Chan–Lam Cyclopropylation of Phenols and Azaheterocycles
by Joseph Derosa, Miriam L. O’Duill, Matthew Holcomb, Mark N. Boulous, Ryan L. Patman, Fen Wang, Michelle Tran-Dubé, Indrawan McAlpine and Keary M. Engle
The Journal of Organic Chemistry
DOI: 10.1021/acs.joc.7b03100
Blake Baker, Yangtianbao93 and 2 others like this
29 Mar 17:50
[ASAP] Breaking the Base Barrier: An Electron-Deficient Palladium Catalyst Enables the Use of a Common Soluble Base in C–N Coupling
by Joseph M. Dennis, Nicholas A. White, Richard Y. Liu, Stephen L. Buchwald
Journal of the American Chemical Society
DOI: 10.1021/jacs.8b01696
29 Mar 17:40
[ASAP] Designing Pd and Ni Catalysts for Cross-Coupling Reactions by Minimizing Off-Cycle Species
by David Balcells, Ainara Nova
ACS Catalysis
DOI: 10.1021/acscatal.8b00230
22 Feb 09:40
Selective [1,4]-Hydrovinylation of 1,3-Dienes with Unactivated Olefins Enabled by Iron Diimine Catalysts
by Valerie A. Schmidt, C. Rose Kennedy, Máté J. Bezdek and Paul J. Chirik
Journal of the American Chemical Society
DOI: 10.1021/jacs.8b00245
zhanglinli, Josep Mas Roselló and one other like this
21 Feb 09:51
Frontispiece: Photoredox Catalysis with Metal Complexes Made from Earth-Abundant Elements
by Christopher B. Larsen, Oliver S. Wenger
This review summarizes recent advances made with photoactive CrIII, FeII, CuI, ZnII, ZrIV, Mo0 and UVI complexes in the context of synthetic organic photoredox chemistry using visible light as an energy input. Mechanistic considerations are combined with discussions of reaction types and scopes. Perspectives for the future of the field are discussed against the background of recent significant developments of new photoactive metal complexes made from earth-abundant elements. More information can be found in the Review article on page 2039 ff.
shirley, Adam Dannenhoffer and -1 others like this
21 Feb 09:46
Train PhD students to be thinkers not just specialists
by Gundula Bosch
Train PhD students to be thinkers not just specialists
Train PhD students to be thinkers not just specialists, Published online: 14 February 2018; doi:10.1038/d41586-018-01853-1
Many doctoral curricula aim to produce narrowly focused researchers rather than critical thinkers. That can and must change, says Gundula Bosch.
Wenzhong Wang, P.Moran and one other like this
21 Feb 09:27
Total Synthesis of Entecavir: A Robust Route for Pilot Production
by Hua Xu, Fang Wang, Weicai Xue, Yunjie Zheng, Qi Wang, Fayang G. Qiu and Yehua Jin
Organic Process Research & Development
DOI: 10.1021/acs.oprd.8b00007
08 Feb 06:53
Iron-Catalyzed Reductive Ethylation of Imines with Ethanol
by Marie Vayer, Sara Patricia Morcillo, Jennifer Dupont, Vincent Gandon, Christophe Bour
Abstract
The borrowing hydrogen strategy has been applied to the ethylation of imines with an air-stable iron complex as precatalyst. This approach opens new perspectives in this area as it enables the synthesis of unsymmetric tertiary amines from readily available substrates and ethanol as a C2 building block. A variety of imines bearing electron-rich aryl or alkyl groups at the nitrogen atom could be efficiently reductively alkylated without the need for molecular hydrogen. The mechanism of this reaction, which shows complete selectivity for ethanol over other alcohols, has been studied experimentally and by means of DFT computations.
The borrowing hydrogen strategy was applied to the ethylation of imines with an air-stable iron complex as precatalyst. This approach enables the synthesis of unsymmetric tertiary amines from readily available substrates and ethanol as a C2 building block. The reductive alkylation of imines bearing electron-rich aryl or alkyl groups at the N atom is thus possible in the absence of molecular hydrogen.
Anastasiia, QiuJ and 3 others like this
08 Feb 06:52
Aluminum-Catalyzed Hydroboration of Alkenes
by Alessandro Bismuto, Michael J. Cowley and Stephen P. Thomas
ACS Catalysis
DOI: 10.1021/acscatal.7b04279
大河弯弯的, wangruijia and 6 others like this
11 Jan 07:07
Iron-Catalyzed Batch/Continuous Flow C–H Functionalization Module for the Synthesis of Anticancer Peroxides
by Moreshwar B. Chaudhari, Suresh Moorthy, Sohan Patil, Girish Singh Bisht, Haneef Mohamed, Sudipta Basu and Boopathy Gnanaprakasam
The Journal of Organic Chemistry
DOI: 10.1021/acs.joc.7b02854
mj, Naoko Ichiishi likes this
11 Jan 07:07
Metal as Source of Chirality in Octahedral Complexes with Tripodal Tetradentate Ligands
by María Carmona, Ricardo Rodríguez, Vincenzo Passarelli, Fernando J. Lahoz, Pilar García-Orduña and Daniel Carmona
Journal of the American Chemical Society
DOI: 10.1021/jacs.7b12731
liuyufengno1 likes this
11 Jan 07:06
Dehydration of Amides to Nitriles under Conditions of a Catalytic Appel Reaction
by Sergei A. Shipilovskikh, Vladimir Yu. Vaganov, Elena I. Denisova, Aleksandr E. Rubtsov and Andrei V. Malkov
Organic Letters
DOI: 10.1021/acs.orglett.7b03862
09 Jan 07:16
Applications of Flow Chemistry in Drug Development: Highlights of Recent Patent Literature
by David L. Hughes
Organic Process Research & Development
DOI: 10.1021/acs.oprd.7b00363
08 Jan 09:21
Heck Reaction of Electronically Diverse Tertiary Alkyl Halides
by Daria Kurandina, Mónica Rivas, Maxim Radzhabov and Vladimir Gevorgyan
Organic Letters
DOI: 10.1021/acs.orglett.7b03591
longlenovo zheng, 大河弯不弯 likes this
08 Jan 08:56
Nickel-Catalyzed Suzuki–Miyaura Coupling of Aliphatic Amides
by Timothy B. Boit, Nicholas A. Weires, Junyong Kim and Neil K. Garg
ACS Catalysis
DOI: 10.1021/acscatal.7b03688
mj, longzhi zhu and 3 others like this
10 Dec 16:09
Recent Advances in Magnesium Carbenoid Chemistry
by Kimura, Tsutomu
Synthesis
DOI: 10.1055/s-0036-1590894
Magnesium carbenoids are a class of organomagnesium species possessing a halo group at the α-position. The reactions of magnesium carbenoids can be classified into the following three categories: nucleophilic reactions resembling Grignard reagents, electrophilic reactions resembling organic halides, and rearrangements resembling carbenes. This short review summarizes recent studies on magnesium carbenoids reported between 2010 and 2016, and milestone studies reported before 2010 according to the classification of the reactions into the aforementioned three categories.1 Introduction2 Structures of Magnesium Carbenoids3 Reactions of Magnesium Carbenoids as Nucleophiles3.1 Nucleophilic Reactions of Magnesium Carbenoids3.2 Nucleophilic Reactions of Magnesium Alkylidene Carbenoids3.3 Nucleophilic Reactions of Cyclopropylmagnesium Carbenoids4 Electrophilic Reactions of Magnesium Carbenoids4.1 Reactions with Nucleophiles Followed by Electrophiles4.2 Reactions with Nucleophiles Possessing Electrophilic Functional Groups4.3 Nucleophilic Substitution Followed by β-Elimination5 Rearrangements of Magnesium Carbenoids5.1 1,2-Shifts of Magnesium Carbenoids5.2 1,3-C–H Insertions of Magnesium Carbenoids5.3 1,5-C–H Insertions of Magnesium Carbenoids5.4 [2+1] Cycloaddition of a Magnesium Carbenoid6 Conclusion and Outlook
[...]
© Georg Thieme Verlag Stuttgart · New York
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10 Dec 16:05
Computer-Assisted Retrosynthesis Based on Molecular Similarity
by Connor W. Coley, Luke Rogers, William H. Green and Klavs F. Jensen
ACS Central Science
DOI: 10.1021/acscentsci.7b00355
10 Dec 15:44
Chemoselective One-Pot Synthesis of Functionalized Amino-azaheterocycles Enabled by COware
by Thomas A. Clohessy, Alastair Roberts, Eric S. Manas, Vipulkumar K. Patel, Niall A. Anderson and Allan J. B. Watson
Organic Letters
DOI: 10.1021/acs.orglett.7b03214
Brett, zhanglinli and 2 others like this
10 Dec 15:12
Electrochemical Cobalt-Catalyzed C–H Oxygenation at Room Temperature
by Nicolas Sauermann, Tjark H. Meyer, Cong Tian and Lutz Ackermann
Journal of the American Chemical Society
DOI: 10.1021/jacs.7b11025
10 Dec 15:11
Radical Multicomponent Carboamination of [1.1.1]Propellane
by Junichiro Kanazawa, Katsuya Maeda and Masanobu Uchiyama
Journal of the American Chemical Society
DOI: 10.1021/jacs.7b11865
10 Dec 15:09
Selective Single C(sp3)–F Bond Cleavage in Trifluoromethylarenes: Merging Visible-Light Catalysis with Lewis Acid Activation
by Kang Chen, Nele Berg, Ruth Gschwind and Burkhard König
Journal of the American Chemical Society
DOI: 10.1021/jacs.7b10755
longzhi zhu, cxl and 11 others like this