One‐Pot Multicomponent Synthesis of β‐Amino Amides

Multicomponent reactions are excellent tools for rapid generation of small molecules with broad chemical diversity and molecular complexity. Herein, a novel one‐pot multicomponent synthesis of β‐amino amides from aldehydes, anilines, carboxylic acids and ynamides has been successfully developed. This process is practical and efficient to unravel synthetic utility and scalability. Moreover, an isotope labeling reaction was conducted to elucidate a plausible reaction mechanism.     

Synthesis of Highly Substituted Pyridines through Copper‐Catalyzed Condensation of Oximes and α,β‐Unsaturated Imines

A copper‐catalyzed condensation reaction of oxime acetates and α,β‐unsaturated ketimines to give pyridine derivatives is reported. The reaction features mild conditions, high functional‐group compatibility, and high regioselectivity with respect to unsymmetrical oxime acetates, thus allowing the preparation of a wide range of polysubstituted pyridines, many of which are not readily accessible by conventional condensation methods.     

Nickel‐Catalyzed Direct Carboxylation of Olefins with CO2: One‐Pot Synthesis of α,β‐Unsaturated Carboxylic Acid Salts

The nickel‐catalyzed direct carboxylation of alkenes with the cheap and abundantly available C₁ building block carbon dioxide (CO₂) in the presence of a base has been achieved. The one‐pot reaction allows for the direct and selective synthesis of a wide range of α,β‐unsaturated carboxylates (TON>100, TOF up to 6 h^?1, TON=turnover number, TOF=turnover frequency). Thus, it is possible, in one step, to synthesize sodium acrylate from ethylene, CO₂, and a sodium salt. Acrylates are industrially important products, the synthesis of which has hitherto required multiple steps.     

A Versatile Methodology for the Synthesis of α,β‐Unsaturated 3‐Iminophosphines

Phorteen phine phosphines : Fourteen new α,β‐unsaturated β‐chloroimines were synthesized from inexpensive ketones by using the Vilsmeier–Haack reagent followed by Schiff‐base condensation. Each imine was subsequently converted to an α,β‐unsaturated 3‐iminophosphine through either late‐metal‐catalyzed phosphorus–carbon cross‐coupling or through an addition–elimination sequence (see scheme). This high‐yield protocol serves as a general means to produce α,β‐unsaturated 3‐iminophosphines.

     

Modular Synthesis of Novel Macrocycles Bearing α,β‐Unsaturated Chemotypes through a Series of One‐Pot,Sequential Protocols

A series of one‐pot, sequential protocols was developed for the synthesis of novel macrocycles bearing α,β‐unsaturated chemotypes. The method highlights a phosphate tether‐mediated approach to establish asymmetry, and consecutive one‐pot, sequential processes to access the macrocycles with minimal purification procedures. This library amenable strategy provided diverse macrocycles containing α,β‐unsaturated carbon‐, sulfur‐, or phosphorus‐based warheads.