scholarly journals Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis

2021 ◽  
Author(s):  
Eric Voight ◽  
Stephen Greszler ◽  
John Hartung ◽  
Jianguo Ji ◽  
Russell C. Klix ◽  
...  
Keyword(s):  
Adduct Formation ◽  
One Pot ◽  
New Class ◽  
Regioselective Functionalization

A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective <i>N</i>-Boc protection and formaldehyde adduct formation sequence, both enabled by crystallization-induced selectivity. The first step represents the only known application of the Horeau principle of statistical amplification for <i>C</i><sub>2</sub>-symmetric polyheterocycle regioselective functionalization. The resulting versatile intermediate is employed in the high-yielding preparation of several pibrentasvir prodrug candidates.

scholarly journals Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis

2021 ◽  
Author(s):  
Eric Voight ◽  
Stephen Greszler ◽  
John Hartung ◽  
Jianguo Ji ◽  
Russell C. Klix ◽  
...  
Keyword(s):  
Adduct Formation ◽  
One Pot ◽  
New Class ◽  
Regioselective Functionalization

A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective <i>N</i>-Boc protection and formaldehyde adduct formation sequence, both enabled by crystallization-induced selectivity. The first step represents the only known application of the Horeau principle of statistical amplification for <i>C</i><sub>2</sub>-symmetric polyheterocycle regioselective functionalization. The resulting versatile intermediate is employed in the high-yielding preparation of several pibrentasvir prodrug candidates.

Facile and Efficient Synthesis of New Class of Imidazole Derivatives via One-Pot Multicomponent Reactions in Water

2013 ◽  
Vol 16 (10) ◽  
pp. 788-790
Author(s):  
Zinatossadat Hossaini ◽  
Samereh Seyfi ◽  
Faramarz Rostami-Charati ◽  
Mehdi Ghambarian
Keyword(s):  
Multicomponent Reactions ◽  
Efficient Synthesis ◽  
One Pot ◽  
Imidazole Derivatives ◽  
New Class

scholarly journals Stereoselective synthesis of spirocyclic pyrrolidines/pyrrolizidines/pyrrolothiazolidines using l-proline functionalized manganese ferrite nanorods as a novel heterogeneous catalyst

RSC Advances ◽  
2021 ◽  
Vol 11 (24) ◽  
pp. 14755-14768
Author(s):  
Malihe Akhavan ◽  
Ahmadreza Bekhradnia
Keyword(s):  
Heterogeneous Catalyst ◽  
Stereoselective Synthesis ◽  
Manganese Ferrite ◽  
One Pot ◽  
New Class

An efficient, green, one-pot, and three-component protocol has been reported for the stereoselective synthesis of a new class of spiro thiazolidines.

scholarly journals Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis

2021 ◽  
Author(s):  
Eric Voight ◽  
Stephen N Greszler ◽  
John Hartung ◽  
Jianguo Ji ◽  
Russell C Klix ◽  
...  
Keyword(s):  
One Pot ◽  
New Class

A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective N-Boc...

scholarly journals One-pot three-component tandem annulation of 4-hydroxycoumarine with aldehyde and aromatic amines using graphene oxide as an efficient catalyst

2021 ◽  
Vol 11 (1) ◽  
Author(s):  
Rabindranath Singha ◽  
Aminul Islam ◽  
Pranab Ghosh
Keyword(s):  
Graphene Oxide ◽  
Catalytic Activity ◽  
Aromatic Amines ◽  
Significant Loss ◽  
Solvent Free ◽  
One Pot ◽  
Efficient Catalyst ◽  
New Class ◽  
Broad Scope ◽  
Plausible Mechanism

AbstractA convenient and efficient solvent-free, facile, one-pot three-component graphene oxide catalysed approach has been described for the synthesis of chromeno-[4,3-b]quinolin-6-one derivatives from 4-hydroxycoumarin with aldehydes and aromatic amines. Graphene oxide (GO) has proved to be a new class of heterogeneous carbocatalyst which could be easily recovered and reused up to 5th run without significant loss of its catalytic activity. A broad scope of substrate applicability is offered and a plausible mechanism is also suggested for this developed protocol.

‘One-pot’ synthesis and redox evaluations of chiral chalcogenocysteinol and β-bis-chalcogenoamine derivatives from l-serine methyl ester

2017 ◽  
Vol 41 (15) ◽  
pp. 7424-7431 ◽  
Author(s):  
Patrícia Foletto ◽  
Luciano Dornelles ◽  
Bernardo A. Iglesias ◽  
Andressa C. Bevilacqua ◽  
Paulo Piquini ◽  
...  
Keyword(s):  
Methyl Ester ◽  
One Pot ◽  
New Class ◽  
One Pot Synthesis

The synthesis of a new class of potential antioxidant chiral chalcogenocysteinols and bis-chalcogenoamines is described in this study.

Colloidal Silica/Poly(Methacrylsiloxane) Nanocomposite Particles: Synthesis, Characterization, and Application in Toners.

2014 ◽  
Vol 1663 ◽  
Author(s):  
Dmitry Fomitchev ◽  
Russell Lewis ◽  
Hairuo Tu ◽  
Li Cheng ◽  
Hajime Kambara ◽  
...  
Keyword(s):  
Particle Size ◽  
Colloidal Silica ◽  
Silica Particles ◽  
Laser Printer ◽  
Mass Ratio ◽  
One Pot ◽  
New Class ◽  
New Material ◽  
Hydrophobic Treatment ◽  
Hydrophobic Material

ABSTRACTWe report on a new class of materials for laser printer toner applications. These materials were prepared from methacrysilane-in-water emulsions stabilized with colloidal silica particles. In this elegant system, the colloidal silica particles reside at the water/oil interface helping to emulsify the oil droplet, self-organizing into a raspberry-like morphology. The emulsion formation is followed by free-radical polymerization, hydrophobic treatment, and drying steps. This one pot synthesis in water affords a hydrophobic material with a particle size in the range of 80 to 300 nm. The particle size could be fine-tuned by changing the oil-to-silica mass ratio or by using colloidal silica particles of different sizes. Results of material characterization by solid-state NMR, electron microscopy, and particle size measurements methods will be presented. Examples of possible extensions of the synthesis towards materials with methacrylsilane partially substituted with other methacrylates will be provided. Application of the new material in toners will be described as will the comparison of its performance with the incumbent material - hydrophobic colloidal silica.

Alginate–copper microspheres as efficient and reusable heterogeneous catalysts for the one-pot synthesis of 4-organylselanyl-1H-pyrazoles

2020 ◽  
Vol 10 (12) ◽  
pp. 3918-3930 ◽  
Author(s):  
Jaqueline F. Souza ◽  
Thalita F. B. de Aquino ◽  
José E. R. Nascimento ◽  
Raquel G. Jacob ◽  
André R. Fajardo
Keyword(s):  
Heterogeneous Catalysts ◽  
One Pot ◽  
New Class ◽  
One Pot Synthesis ◽  
Facile Preparation ◽  
The One ◽  
Substituted Pyrazoles

This study demonstrates the facile preparation and use of alginate–Cu2+ microspheres in the catalysis of a new class of organoselenium substituted pyrazoles through one-pot reactions.

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