Development of a Highly Selective Plasmodium falciparum Proteasome Inhibitor with Anti ‐malaria Activity in Humanized Mice
Development of a Highly SelectivePlasmodium falciparum Proteasome Inhibitor with Anti ‐malaria Activity in Humanized MiceDr. Wenhu Zhan,Dr. Hao Zhang,Dr. John Ginn,Annie Leung,Yi J. Liu,Dr. Mayako Michino,Dr. Akinori Toita,Dr. Rei Okamoto,Tzu ‐Tshin Wong,Dr. Toshihiro Imaeda,Dr. Ryoma Hara,Dr. Takafumi Yukawa,Sevil Chelebieva,Patrick K. Tumwebaze,Dr. Maria Jose Lafuente ‐Monasterio,Dr. Maria Santos Martinez ‐Martinez,Dr. Jeremie Vendome,Dr. Thijs Beumin,Dr. Kenjiro Sato,Dr. Kazuyoshi Aso,Prof. Dr. Philip J. Rosenthal,Prof. Dr. Roland A. Cooper,Dr. Peter T. Meinke,Prof. Dr. Carl F. Nathan,Prof. Dr. Laura...
Source: Organometallic Current - March 11, 2021 Category: Chemistry Tags: Drug discovery Inhibitors malaria Peptide Modification Source Type: blogs
Photoenzymatic enantioselective intermolecular radical hydroalkylation
Xiaoqiang Huang , Binju Wang, Yajie Wang, Guangde Jiang, Jianqiang Feng& Huimin ZhaoA transformation in which an ‘ene’ reductase catalyses the visible-light-induced intermolecular radical hydroalkylation of alkenes gives carbonyl compounds with a remote stereocentre in high yield and enantioselectivity. (Source: Organometallic Current)
Source: Organometallic Current - August 7, 2020 Category: Chemistry Tags: Enantioselective Hydroalkylation Photocatalysis Source Type: blogs
A short de novo synthesis of nucleoside analogs
We present a process for rapidly constructing nucleoside analogs from simple achiral materials. Using only proline catalysis, heteroaryl-substituted acetaldehydes are fluorinated and then directly engaged in enantioselective aldol reactions in a one-pot reaction. A subsequent intramolecular fluoride displacement reaction provides a functionalized nucleoside analog. The versatility of this process is highlighted in multigram syntheses of D- or L-nucleoside analogs, locked nucleic acids, iminonucleosides, and C2 ′- and C4′-modified nucleoside analogs. This de novo synthesis creates opportunities for the prepara...
Source: Organometallic Current - August 7, 2020 Category: Chemistry Tags: Nucleosides Source Type: blogs
A photochemical dehydrogenative strategy for aniline synthesis
Shashikant U. Dighe, Fabio Juli á, Alberto Luridiana, James J. Douglas & Daniele LeonoriA dual cobalt and photocatalysis system provides a way to assemble anilines from cyclohexanones and amines by progressively dehydrating the intermediate imine. (Source: Organometallic Current)
Source: Organometallic Current - August 6, 2020 Category: Chemistry Tags: Dehydrogenative Coupling Photochemical Rxn Source Type: blogs
Chemo ‐ and Enantioselective Oxidative α‐Azidation of Carbonyl Compounds
Prof. Dr. Muhammet Uyanik Dr. Naoto Sahara Mayuko Tsukahara Yuhei Hattori Prof. Dr. Kazuaki IshiharaHigh ‐performance hypoiodite catalysis was developed for the chemoselective oxidative or decarboxylative oxidative α‐azidation of 1,3‐dicarbonyl compounds (see scheme). By this method, the late‐stage azidation of complex molecules with NaN3 and hydrogen peroxide as the azide source and oxidant, respectively, was possible under extremely mild conditions. (Source: Organometallic Current)
Source: Organometallic Current - August 6, 2020 Category: Chemistry Tags: Azidation Hypervalent Iodine Reagents Source Type: blogs
Palladium(II) ‐Catalyzed Enantioselective Azidation of Unactivated Alkenes
Xiaonan Li Dr. Xiaoxu Qi Chuanqi Hou Dr. Pinhong Chen Prof. Dr. Guosheng LiuA Pd ‐catalyzed enantioselective intramolecular aminoazidation of unactivated alkenes using readily accessible 1 ‐azido‐1,2‐benziodoxol‐3(1H ) ‐one (ABX) as an azidating agent was established. This reaction affords a wide variety of structurally diverse 3‐N3‐substituted piperidines in good yields with excellent enantioselectivity, proceeds under mild reaction conditions, and features good functional‐group compatibility. (Source: Organometallic Current)
Source: Organometallic Current - August 5, 2020 Category: Chemistry Tags: Alkenes Azidation Enantioselective Pd Catalyzed Source Type: blogs
Synthesis, Characterization, and Reactivity of a Hypervalent ‐Iodine‐Based Nitrooxylating Reagent
Roxan Calvo Antoine Le Tellier Dr. Thomas Nauser Dr. David Rombach Darryl Nater Dr. Dmitry KatayevOrganic nitrate esters were synthesized through the use of a hypervalent ‐iodine‐based nitrooxylating reagent. Its versatile reactivity under various reaction conditions is demonstrated in the synthesis of nitrooxylated β‐keto esters, 1,3‐diketones, malonates, and oxindoles under mild conditions. (Source: Organometallic Current)
Source: Organometallic Current - August 5, 2020 Category: Chemistry Tags: Hypervalent Iodine Reagents Nitration Source Type: blogs
Cobalt ‐Catalyzed C8‐Dienylation of Quinoline‐N‐Oxides
Rahul K. Shukla Akshay M. Nair Salman Khan Prof. Chandra M. R. VollaCoIII‐catalyzed site ‐selective C8−H activation of quinoline N‐oxides is demonstrated, engaging allenes as dienylation partners under relatively mild reaction conditions. The combination of a carbonate leaving group on the allene and 30 mol % of a NaF additive was found to be crucial for the dienylation reaction with a broad range of quinoline N‐oxides and allenes, including late‐stage functionalizations. Mechanistic studies provide key insights into the reaction mechanism. (Source: Organometallic Current)
Source: Organometallic Current - August 5, 2020 Category: Chemistry Tags: Co catalyzed Site selective Source Type: blogs
