Liver ‐Targeted Small‐Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis
AngewchemLiver ‐Targeted Small‐Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis: Targeting of the human ribosome is an unprecedented therapeutic modality with a genome ‐wide selectivity challenge. A liver‐targeted drug candidate is described that inhibits ribosomal synthesis of PCSK9,... (Source: Organometallic Current)
Source: Organometallic Current - November 28, 2017 Category: Chemistry Tags: Drug discovery Source Type: blogs
Consecutive Transformations of Tetrafluoropropenes: Hydrogermylation and Catalytic C −F Activation Steps at a Lewis Acidic Aluminum Fluoride
AngewchemConsecutive Transformations of Tetrafluoropropenes: Hydrogermylation and Catalytic C −F Activation Steps at a Lewis Acidic Aluminum Fluoride: Functionalization reactions of the refrigerants HFO ‐1234yf (2,3,3,3‐tetrafluoropropene) and HFO‐1234ze (1,3,3,3‐tetrafluoropropene) were developed. The selectivity and reactivity towards CF3 groups of... (Source: Organometallic Current)
Source: Organometallic Current - November 28, 2017 Category: Chemistry Tags: C-F activation Source Type: blogs
Organocatalytic Atroposelective Arylation of 2 ‐Naphthylamines as a Practical Approach to Axially Chiral Biaryl Amino Alcohols
AngewchemOrganocatalytic Atroposelective Arylation of 2 ‐Naphthylamines as a Practical Approach to Axially Chiral Biaryl Amino Alcohols: The first phosphoric acid catalyzed direct arylation of 2 ‐naphthylamines with iminoquinones for the atroposelective synthesis of axially chiral biaryl amino alcohols has been developed. This reaction constitutes... (Source: Organometallic Current)
Source: Organometallic Current - November 28, 2017 Category: Chemistry Tags: Arylation chiral organocatalysis Source Type: blogs
---
Ligand-accelerated non-directed C –H functionalization of arenes Nature551,489–493 (23 November 2017)doi:10.1038/nature24632 Peng Wang, Pritha Verma, Guoqin Xia, Jun Shi, Jennifer X. Qiao+ et al.Using a ligand as a promoter enhances the reactivity of the palladium catalyst in non-directed C –H functionalization of arenes, enabling the arene to be used as the limiting reagent.The directed activation of carbon –hydrogen bonds (C–H) is important in the development of synthetically useful reactions, owing to the proximity-induced reactivity and selectivity that is enabled by coordinating functional groups. ...
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: C-H Functionalization Pd Catalyzed Source Type: blogs
Preparation of Functionalized Diaryl ‐ and Diheteroaryllanthanum Reagents by Fast Halogen–Lanthanum Exchange
AngewchemPreparation of Functionalized Diaryl ‐ and Diheteroaryllanthanum Reagents by Fast Halogen–Lanthanum Exchange: Aryl and heteroaryl halides (X=Br, I) undergo a fast and convenient halogen –lanthanum exchange with nBu2LaMe, which leads to functionalized diaryl‐ and diheteroaryllanthanum derivatives. Subsequent trapping... (Source: Organometallic Current)
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: Lanthanides Synthetic method Source Type: blogs
Rhodium(II) ‐ or Copper(I)‐Catalyzed Formal Intramolecular Carbene Insertion into Vinylic C(sp2)−H Bonds: Access to Substituted 1H‐Indenes
AngewchemRhodium(II) ‐ or Copper(I)‐Catalyzed Formal Intramolecular Carbene Insertion into Vinylic C(sp2)−H Bonds: Access to Substituted 1H‐Indenes: A rhodium(II) ‐ or copper(I)‐catalyzed formal intramolecular carbene insertion into vinylic C(sp2)−H bonds is reported herein. This method provides straightforward access to 1H‐indenes with high efficiency... (Source: Organometallic Current)
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: Cu catalyzed Rh Catalyzed Source Type: blogs
Bifurcated Nickel ‐Catalyzed Functionalizations: Heteroarene C−H Activation with Allenes
AngewchemBifurcated Nickel ‐Catalyzed Functionalizations: Heteroarene C−H Activation with Allenes: A unified strategy for nickel(0) ‐catalyzed C−H allylations, alkenylations, and dienylations has been realized through versatile hydroarylations of allenes with ample scope. Thus, an inexpensive nickel... (Source: Organometallic Current)
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: Allenes C-H Activation Ni Catalyzed Source Type: blogs
Transition ‐Metal‐Free Catalytic Hydrodefluorination of Polyfluoroarenes by Concerted Nucleophilic Aromatic Substitution with a Hydrosilicate
AngewchemTransition ‐Metal‐Free Catalytic Hydrodefluorination of Polyfluoroarenes by Concerted Nucleophilic Aromatic Substitution with a Hydrosilicate: A transition ‐metal‐free catalytic hydrodefluorination (HDF) reaction of polyfluoroarenes is described. The reaction involves direct hydride transfer from a hydrosilicate as the key intermediate, which... (Source: Organometallic Current)
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: Defunctionalization Metal free Nucleophilic Aromatic Substitution Source Type: blogs
Microwave ‐Assisted Synthesis of Heterocycles by Rhodium(III)‐Catalyzed Annulation of N‐Methoxyamides with α‐Chloroaldehydes
AngewchemMicrowave ‐Assisted Synthesis of Heterocycles by Rhodium(III)‐Catalyzed Annulation of N‐Methoxyamides with α‐Chloroaldehydes: α‐Chloroaldehydes have been used as alkyne equivalents in rhodium‐catalyzed syntheses of isoquinolones and 3,4‐dihydroisoquinolins starting from N‐methoxyamides. Compared to the existing technology, a... (Source: Organometallic Current)
Source: Organometallic Current - November 23, 2017 Category: Chemistry Tags: annulation microwave Rh Catalyzed Source Type: blogs
Gold ‐Catalyzed Asymmetric Intramolecular Cyclization of N‐Allenamides for the Synthesis of Chiral Tetrahydrocarbolines
AngewchemGold ‐Catalyzed Asymmetric Intramolecular Cyclization of N‐Allenamides for the Synthesis of Chiral Tetrahydrocarbolines: Highly enantioselective gold ‐catalyzed intramolecular cyclization of N‐allenamides was implemented by utilizing a designed chiral sulfinamide phosphine ligand (PC‐Phos). This represents the first example... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Gold Catalysis Source Type: blogs
Access to α‐Amino Acid Esters through Palladium‐Catalyzed Oxidative Amination of Vinyl Ethers with Hydrogen Peroxide as the Oxidant and Oxygen Source
AngewchemAccess to α‐Amino Acid Esters through Palladium‐Catalyzed Oxidative Amination of Vinyl Ethers with Hydrogen Peroxide as the Oxidant and Oxygen Source: A novel and convenient palladium catalytic system for the synthesis of α‐amino acid esters from simple starting materials is reported. Hydrogen peroxide not only acts as the green oxidant, but also as... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Amination Pd Catalyzed Source Type: blogs
Access to Chiral Hydropyrimidines through Palladium ‐Catalyzed Asymmetric Allylic C−H Amination
AngewchemAccess to Chiral Hydropyrimidines through Palladium ‐Catalyzed Asymmetric Allylic C−H Amination: A palladium ‐catalyzed asymmetric intramolecular allylic C−H amination controlled by a chiral phosphoramidite ligand was established for the preparation of various substituted chiral hydropyrimidinones,... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Allylic C-H Activation Pd Catalyzed Source Type: blogs
Intermolecular Pummerer Coupling with Carbon Nucleophiles in Non ‐Electrophilic Media
AngewchemIntermolecular Pummerer Coupling with Carbon Nucleophiles in Non ‐Electrophilic Media: A new Pummerer ‐type C−C coupling protocol is introduced based on turbo‐organomagnesium amides, which unlike traditional Pummerer reactions, does not require strong electrophilic activators, engages a broad... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Pummerer reaction Source Type: blogs
Double Catalytic Kinetic Resolution (DoCKR) of Acyclic anti ‐1,3‐Diols: The Additive Horeau Amplification
AngewchemDouble Catalytic Kinetic Resolution (DoCKR) of Acyclic anti ‐1,3‐Diols: The Additive Horeau Amplification: The concept of a synergistic double catalytic kinetic resolution (DoCKR) as described in this article was successfully applied to racemic acyclic anti ‐1,3‐diols, a common motif in natural products. This... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Kinetic resolution Source Type: blogs
Enantioselective Copper ‐Catalyzed Alkylation of Quinoline N‐Oxides with Vinylarenes
AngewchemEnantioselective Copper ‐Catalyzed Alkylation of Quinoline N‐Oxides with Vinylarenes: An asymmetric copper ‐catalyzed alkylation of quinoline N‐oxides with chiral Cu–alkyl species, generated by migratory insertion of a vinylarene into a chiral Cu−H complex, is reported. A variety of quinoline... (Source: Organometallic Current)
Source: Organometallic Current - November 21, 2017 Category: Chemistry Tags: Alkylation Cu catalyzed Enantioselective Source Type: blogs
