Practical and Scalable Synthetic Method for Preparation of Dolutegravir Sodium: Improvement of a Synthetic Route for Large-Scale Synthesis

2019 ◽  
Vol 23 (4) ◽  
pp. 558-564 ◽  
Author(s):  
Yasunori Aoyama ◽  
Toshikazu Hakogi ◽  
Yuki Fukui ◽  
Daisuke Yamada ◽  
Takao Ooyama ◽  
...  
Keyword(s):  
Large Scale ◽  
Synthetic Method ◽  
Synthetic Route ◽  
Large Scale Synthesis

Updating Levothyroxine Synthesis for the Modern Age

2020 ◽  
Vol 17 ◽  
Author(s):  
Shashika Sevvandi Perera ◽  
Dinara Shashanka Gunasekera ◽  
Umayangani Kumari Wanninayake ◽  
Dhanushi Thathsara Welideniya ◽  
Adheesha Saseenda Jayathilaka ◽  
...  
Keyword(s):  
Experimental Data ◽  
Sodium Salt ◽  
Large Scale ◽  
Active Pharmaceutical Ingredient ◽  
Levothyroxine Sodium ◽  
Synthetic Route ◽  
Fine Chemical ◽  
Modern Age ◽  
Alternative Path ◽  
Large Scale Synthesis

: Synthesis of Levothyroxine sodium, the sodium salt of a synthetic levoisomer of thyroxine, revolutionized the management of hypothyroidism and related symptoms. However, the main synthetic route to this active pharmaceutical ingredient (API) is more than 70+ years old with low-yielding steps, obsolete reagents, and lacks experimental data on intermediates, which makes laboratory and large-scale synthesis of this API difficult and time consuming. Here, we describe an improved synthesis of levothyroxine, using commonly available modern reagents. By modifying and replacing low yielding and/or unproductive steps of Chalmers synthesis, we were able to achieve higher overall yields (39-51%) consistently. Key modifications include an alternative path to the selective N-acetylation step that yielded 5 in a pure and consistent fashion. Our improved methodology coupled with detailed experimental data provides a practical alternative to existing methods that can be conveniently implemented to synthesize Levothyroxine sodium in fine chemical settings.

scholarly journals A large-scale synthesis of heteroatom (N and S) co-doped hierarchically porous carbon (HPC) derived from polyquaternium for superior oxygen reduction reactivity

2016 ◽  
Vol 18 (9) ◽  
pp. 2699-2709 ◽  
Author(s):  
Mingjie Wu ◽  
Jinli Qiao ◽  
Kaixi Li ◽  
Xuejun Zhou ◽  
Yuyu Liu ◽  
...  
Keyword(s):  
Oxygen Reduction ◽  
Porous Carbon ◽  
Large Scale ◽  
Synthetic Route ◽  
Hierarchically Porous ◽  
Large Scale Synthesis ◽  
Co Doped

A simple, large-scale and green synthetic route is demonstrated for the preparation of polyquaternium derived heteroatom (N and S) co-doped hierarchically porous carbon (HPC).

Exogenous Directing Group Free, Ligand-Enabled gamma-C(sp3)–H Arylation of Free Primary Aliphatic Amines and α-Amino Esters

2019 ◽  
Author(s):  
Yongzheng Ding ◽  
Shuai Fan ◽  
Xiaoxi Chen ◽  
yuzhen gao ◽  
Gang Li
Keyword(s):  
Amino Acids ◽  
Large Scale ◽  
Free Ligand ◽  
Aliphatic Amines ◽  
Rapid Synthesis ◽  
Amino Esters ◽  
Directing Group ◽  
Large Scale Synthesis ◽  
Primary Aliphatic Amines

A Pdᴵᴵ-catalyzed, ligand-enabled gamma-C(sp3)–H arylation of free primary aliphatic amines and amino esters without using an exogenous directing group is reported. This reaction is compatible with unhindered free aliphatic amines, and it is also be applicable to the rapid synthesis of biologically and synthetically valuable unnatural α-amino acids. Large scale synthesis is also feasible using this method.<br>

A Simplified Protocol for the ortho-Deuteration of Acidic Aromatic Compounds in D2O

2019 ◽  
Author(s):  
Alyssa Garreau ◽  
Hanyang Zhou ◽  
Michael Young
Keyword(s):  
Carboxylic Acid ◽  
Aromatic Compounds ◽  
Large Scale ◽  
Simplified Approach ◽  
Directing Group ◽  
Large Scale Synthesis

<div>Methods to catalytically introduce deuterium in synthetically useful yields ortho to a carboxylic acid directing group on arenes typically requires D2 or CD3CO2D, which makes using these approaches cost prohibitive for large scale synthesis (equipment and reagent costs respectively). Herein we present a simplified approach using catalytic RhIII and D2O as deuterium source, and show its application to H/D exchange on various acidic substrates.</div>

A Simplified Protocol for the ortho-Deuteration of Acidic Aromatic Compounds in D2O

2019 ◽  
Author(s):  
Alyssa Garreau ◽  
Hanyang Zhou ◽  
Michael Young
Keyword(s):  
Carboxylic Acid ◽  
Aromatic Compounds ◽  
Large Scale ◽  
Simplified Approach ◽  
Directing Group ◽  
Large Scale Synthesis

<div>Methods to catalytically introduce deuterium in synthetically useful yields ortho to a carboxylic acid directing group on arenes typically requires D2 or CD3CO2D, which makes using these approaches cost prohibitive for large scale synthesis (equipment and reagent costs respectively). Herein we present a simplified approach using catalytic RhIII and D2O as deuterium source, and show its application to H/D exchange on various acidic substrates.</div>

Improved and Large-Scale Synthesis of N-methyl-D-aspartic Acid

2015 ◽  
Vol 12 (2) ◽  
pp. 197-201 ◽  
Author(s):  
Liang Xi ◽  
Di Wu ◽  
Hong-You Zhu ◽  
Cong-Hai Zhang ◽  
Yi Jin ◽  
...  
Keyword(s):  
Aspartic Acid ◽  
Large Scale ◽  
Large Scale Synthesis

Large-scale synthesis of copper nanoparticles by chemically controlled reduction for applications of inkjet-printed electronics

2008 ◽  
Vol 19 (41) ◽  
pp. 415604 ◽  
Author(s):  
Youngil Lee ◽  
Jun-rak Choi ◽  
Kwi Jong Lee ◽  
Nathan E Stott ◽  
Donghoon Kim
Keyword(s):  
Copper Nanoparticles ◽  
Large Scale ◽  
Printed Electronics ◽  
Large Scale Synthesis

Large-scale synthesis of ionic liquid [BMIM]Br in a microbore tube

2021 ◽  
Author(s):  
Nirvik Sen ◽  
Sameer Ekhande ◽  
K.K. Singh ◽  
S. Mukhopadhyay ◽  
R.S. Sirsam ◽  
...  
Keyword(s):  
Ionic Liquid ◽  
Large Scale ◽  
Large Scale Synthesis

scholarly journals A Facile Urea-Assisted Thermal Decomposition Process of TiO2 Nanoparticles and Their Photocatalytic Activity

Coatings ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. 165
Author(s):  
Sandip Madhukar Deshmukh ◽  
Mohaseen S. Tamboli ◽  
Hamid Shaikh ◽  
Santosh B. Babar ◽  
Dipak P. Hiwarale ◽  
...  
Keyword(s):  
Thermal Decomposition ◽  
Photocatalytic Activity ◽  
Tio2 Nanoparticles ◽  
Large Scale ◽  
Ultra Violet ◽  
Tio2 Nps ◽  
Transmission Electron ◽  
Structures And Properties ◽  
Ft Ir ◽  
Large Scale Synthesis

In the present work, we have reported a facile and large-scale synthesis of TiO2 nanoparticles (NPs) through urea-assisted thermal decomposition of titanium oxysulphate. We have successfully synthesized TiO2 NPs by using this effective route with different weight ratios of titanium oxysulphate: urea. The structures and properties of TiO2 NPs were confirmed by scanning electron microscope) (SEM), transmission electron microscopy (TEM), thermogravimetric analysis (TGA), fourier transform infrared spectroscopy (FT-IR), ultra violet–visible spectroscopy (UV-vis), and photoluminescence (Pl) techniques. XRD demonstrated that TiO2 NPs holds of anatase crystal phase with crystallizing size 14–19 nm even after heating at 600 °C. TGA, SEM, and TEM images reveal urea’s role, which controls the size, morphology, and aggregation of TiO2 NPs during the thermal decomposition. These TiO2 NPs were employed for photodegradation of Methyl Orange (MO) in the presence of ultraviolet (UV) radiation. An interesting find was that the TiO2 NPs exhibited better photocatalytic activity and excellent recycling stability over several photodegradation cycles. Furthermore, the present method has a great perspective to be used as an efficient method for large-scale synthesis of TiO2 NPs.

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