Mario Barberis

Discovery of potent small-molecule inhibitors of lipoprotein(a) formation

N. Paniagua Díaz, Carlos A. Perez, Ana Escribano, Gema Sanz et autres

Abstract Lipoprotein(a) (Lp(a)), an independent, causal cardiovascular risk factor, is a lipoprotein particle that is formed by the interaction of a low-density lipoprotein (LDL) particle and apolipoprotein(a) (apo(a))1,2. Apo(a) first binds to lysine residues of apolipoprotein B-100 (apoB-100) on LDL through the …

us, au (code pays fourni par la source)

Synthesis of Enantiopure Unnatural Amino Acids by Metallaphotoredox Catalysis

Tomer M. Faraggi, Caroline Rouget-Virbel, Juan A. Rincón, Mario Barberis et autres

We describe herein a two-step process for the conversion of serine to a wide array of optically pure unnatural amino acids. This method utilizes a photocatalytic cross-electrophile coupling between a bromoalkyl intermediate and a diverse set of aryl halides to produce artificial …

us, es (code pays fourni par la source)

Rapid Optimization of Photoredox Reactions for Continuous-Flow Systems Using Microscale Batch Technology

María González‐Esguevillas, David F. Fernández, Juan A. Rincón, Mario Barberis et autres

Photoredox catalysis has emerged as a powerful and versatile platform for the synthesis of complex molecules. While photocatalysis is already broadly used in small-scale batch chemistry across the pharmaceutical sector, recent efforts have focused on performing these transformations in process chemistry due …

us, es (code pays fourni par la source)

Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints

Leonard L. Winneroski, Jon A. Erickson, Steven J. Green, José Enrique López et autres

us (code pays fourni par la source)

The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

Steven M. Mennen, Carolina Alhambra, C. Liana Allen, Mario Barberis et autres

Abstract High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. Today, most major …

us, es, co, gb, au, ch, de (code pays fourni par la source)

Metallaphotoredox-Catalyzed Cross-Electrophile C sp 3 –C sp 3 Coupling of Aliphatic Bromides

Russell T. Smith, Xiaheng Zhang, Juan A. Rincón, Javier Agejas et autres

A strategy for the installation of small alkyl fragments onto pharmaceutically relevant aliphatic structures has been established via metallaphotoredox catalysis. Herein, we report that tris(trimethylsilyl)silanol can be employed as an effective halogen abstraction reagent that, in combination with photoredox and nickel catalysis, …

us, es (code pays fourni par la source)

Practical Asymmetric Fluorination Approach to the Scalable Synthesis of New Fluoroaminothiazine BACE Inhibitors

Pablo García‐Losada, Mario Barberis, Yuan Shi, Erik J. Hembre et autres

Here we report an optimized protocol for the asymmetric introduction of a fluorine atom into a quaternary center facilitated by d -proline, Selectfluor ®, and trifluoroethanol. The synthesis proceeds over four steps starting from a chiral amino alcohol precursor and provides the …

es, us (code pays fourni par la source)

Ewolucja, konstytucja, bezpieczeństwo. Zarys teorii prawdziwie realistycznej

Mario Barberis

(1S,2R,3S,4S,5R,6R)‐2‐アミノ‐3‐[(3,4‐ジフルオロフェニル)スルファニルメチル]‐4‐ヒドロキシ‐ビシクロ[3.1.0]ヘキサン‐2,6‐ジカルボン酸塩酸塩(LY3020371HCl)の発見: 抗鬱様活性を持つ強力な向代謝性グルタミン酸2/3受容体アンタゴニスト

D Chappell Mark, Renhua Li, C Smith Stephon, Alexander Bruce et autres

Safe, Convenient ortho-Claisen Thermal Rearrangement Using a Flow Reactor

Juan A. Rincón, Mario Barberis, María González‐Esguevillas, Martin D. Johnson et autres

The [3,3] Claisen rearrangement is a well-known reaction that has been very useful for the synthesis of o -allyl phenols. The thermally induced rearrangement could present safety and operational issues at large batch scale. Herein, we report a process that utilized a …

es, us (code pays fourni par la source)

Imidazolyl benzimidazoles and imidazo[4,5-b]pyridines as potent p38α MAP kinase inhibitors with excellent in vivo antiinflammatory properties

Mary M. Mader, Alfonso de Dios, Chuan Shih, Rosanne Bonjouklian et autres

us, es (code pays fourni par la source)

Development of a Scalable Process for the Synthesis of trans-2-Methylcyclopropanecarboxylic Acid

Laurent Delhaye, Christophe Stevens, Alain Merschaert, Pieter Delbeke et autres

A scalable process has been developed for the synthesis of trans -2-methylcyclopropanecarboxylic acid via the stereoselective cyclopropanation of ethyl crotonate with dimethylsulfoxonium methylide (Corey’s ylide). This well-known reaction is generally low yielding and very challenging to scale up as it involves highly …

es (code pays fourni par la source)