Natural products and their derivatives have historically been invaluable as a source of therapeutic agents. However, in the past decade, research into natural products in the pharmaceutical industry has declined, owing to issues such as the lack of compatibility of traditional natural-product extract libraries with high-throughput screening. However, as discussed in this review, recent technological advances that help to address these issues, coupled with unrealized expectations from current lead-generation strategies, have led to a renewed interest in natural products in drug discovery.

The evolving role of natural products in drug discovery

In 2010, Richard Heck, Ei-ichi Negishi, and Akira Suzuki joined the prestigious circle of Nobel Laureate chemists for their roles in discovering and developing highly practical methodologies for C-C bond construction. From their original contributions in the early 1970s the landscape of the strategies and methods of organic synthesis irreversibly changed for the modern chemist, both in academia and in industry. In this Review, we attempt to trace the historical origin of these powerful reactions, and outline the developments from the seminal discoveries leading to their eminent position as appreciated and applied today.

Palladium-Catalyzed Cross-Coupling: A Historical Contextual Perspective to the 2010 Nobel Prize

Large-scale applications of transition metal-catalyzed couplings for the synthesis of pharmaceuticals.

Dialkylbiaryl phosphines are a valuable class of ligand for Pd-catalyzed amination reactions and have been applied in a range of contexts. This perspective attempts to aid the reader in the selection of the best choice of reaction conditions and ligand of this class for the most commonly encountered and practically important substrate combinations.

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Dialkylbiaryl Phosphines in Pd-Catalyzed Amination: A User's Guide.

The potential of palladacycles: more than just precatalysts

A specific combination, linked pro-drug or a compound of an angiotensin receptor antagonist and a NEPi are used in the treatment of hypertension.

Pharmaceutical combinations of an angiotensin receptor antagonist and an nep inhibitor

Reduction of nitroarenes to anilines using activated iron generated by Fe/HCl or Zn/FeSO 4 is described. A variety of functional groups such as alkyne, ketone, enone, nitrile, lactone, and aromatic halide are well tolerated under these conditions.

A Practical and Chemoselective Reduction of Nitroarenes to Anilines Using Activated Iron

LCZ696: a dual-acting sodium supramolecular complex

A new, economical, practical and racemization-free method for the reductive removal of 2-oxazolidinones from N-acyloxazolidinones with sodium borohydride

An efficient palladium-catalyzed amination of aromatic bromides with hindered N-alkyl-substituted anilines is described, either using the combination of Pd(OAc)2 and P(t-Bu)3 or a palladium(I) tri-tert-butylphosphine bromide dimer, [Pd(μ-Br)(t-Bu3P)]2, a new, commercially available, and easily handled catalyst.

Mahavir Prashad

Papers

Pharmaceutical combinations of an angiotensin receptor antagonist and an nep inhibitor

A Practical and Chemoselective Reduction of Nitroarenes to Anilines Using Activated Iron

LCZ696: a dual-acting sodium supramolecular complex

A new, economical, practical and racemization-free method for the reductive removal of 2-oxazolidinones from N-acyloxazolidinones with sodium borohydride

Palladium-catalyzed amination of aryl bromides with hindered N-alkyl-substituted anilines using a palladium(I) tri-tert-butylphosphine bromide dimer.