Continuous-flow protocol for the synthesis of enantiomerically pure intermediates of anti epilepsy and anti tuberculosis active pharmaceutical ingredients

2019 ◽  
Vol 17 (6) ◽  
pp. 1552-1557 ◽  
Author(s):  
Renata M. Aguiar ◽  
Raquel A. C. Leão ◽  
Alejandro Mata ◽  
David Cantillo ◽  
C. Oliver Kappe ◽  
...  
Keyword(s):  
Amino Acids ◽  
Continuous Flow ◽  
Building Blocks ◽  
Active Pharmaceutical Ingredients ◽  
Enantiomerically Pure ◽  
Pharmaceutical Ingredients ◽  
Chiral Intermediates

Continuous-flow production of chiral intermediates plays an important role in the development of building blocks for Active Pharmaceutical Ingredients (APIs), being α-amino acids and their derivatives widely applied as building blocks.

Towards 4th industrial revolution efficient and sustainable continuous flow manufacturing of active pharmaceutical ingredients

2022 ◽  
Author(s):  
Cloudius Sagandira ◽  
Sinazo Nqeketo ◽  
Kanysile Mhlana ◽  
Thembela Sonti ◽  
Paul Watts ◽  
...  
Keyword(s):  
Pharmaceutical Industry ◽  
Continuous Flow ◽  
Industrial Revolution ◽  
Flow Chemistry ◽  
Active Pharmaceutical Ingredients ◽  
New Paradigm ◽  
Pharmaceutical Ingredients ◽  
Continuous Flow Chemistry

Continuous flow chemistry has opened a new paradigm in both the laboratory and pharmaceutical industry. This review details the recently reported literature on continuous multistep telescoped synthesis of active pharmaceutical...

scholarly journals Continuous one-flow multi-step synthesis of active pharmaceutical ingredients

2020 ◽  
Vol 5 (7) ◽  
pp. 1186-1197 ◽  
Author(s):  
Victor R. L. J. Bloemendal ◽  
Mathilde A. C. H. Janssen ◽  
Jan C. M. van Hest ◽  
Floris P. J. T. Rutjes
Keyword(s):  
Continuous Flow ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Flow Processes ◽  
Selection Of

This review highlights a selection of multistep continuous flow (one-flow) processes leading to the synthesis of active pharmaceutical ingredients (APIs).

Evolution of flow-oriented design strategies in the continuous preparation of pharmaceuticals

2020 ◽  
Vol 5 (9) ◽  
pp. 1527-1555 ◽  
Author(s):  
Zsolt Fülöp ◽  
Péter Szemesi ◽  
Péter Bana ◽  
János Éles ◽  
István Greiner
Keyword(s):  
Continuous Flow ◽  
Active Pharmaceutical Ingredients ◽  
Design Strategies ◽  
Flow Synthesis ◽  
Pharmaceutical Ingredients ◽  
Continuous Preparation

This review focuses on the flow-oriented design (FOD) in the multi-step continuous-flow synthesis of active pharmaceutical ingredients.

scholarly journals Sustainable Electrochemical Decarboxylative Acetoxylation of Aminoacids in Batch and Continuous Flow

2021 ◽  
Author(s):  
Manuel Köckinger ◽  
Paul Hanselmann ◽  
Dominique M. Roberge ◽  
Pierro Geotti-Bianchini ◽  
C. Oliver Kappe ◽  
...  
Keyword(s):  
Amino Acids ◽  
Continuous Flow ◽  
Flow Mode ◽  
Oxidative Decarboxylation ◽  
Pharmaceutical Ingredients ◽  
Synthetic Amino Acids ◽  
Electrochemical Approach ◽  
Synthetic Intermediates ◽  
Space Time Yield ◽  
Aliphatic Carboxylic Acids

Introduction of acetoxy groups to organic molecules is important for the preparation of many active ingredients and synthetic intermediates. A commonly used and attractive strategy is the oxidative decarboxylation of aliphatic carboxylic acids, which entails the generation of a new C(sp3)-O bond. This reaction has been traditionally carried out using excess amounts of harmful lead(IV) acetate. A sustainable alternative to stoichiometric oxidants is the Hofer-Moest reaction, which relies in the 2-electron anodic oxidation of the carboxylic acid. However, examples showing electrochemical acetoxylation of amino acids are scarce. Herein we present a general and scalable procedure for the anodic decarboxylative acetoxylation of amino acids in batch and continuous flow mode. The procedure has been applied to the derivatization of several natural and synthetic amino acids, including key intermediates for the synthesis of active pharmaceutical ingredients. Good to excellent yields were obtained in all cases. Transfer of the process from batch to a continuous flow cell signficantly increased reaction throughput and space-time yield, with excellent product yields obtained even in a single-pass. The sustainability of the electrochemical protocol has been examined by evaluating its green metrics. Comparison with the conventional method demonstrates that an electrochemical approach has a significant positive effect on the greenness of the process

Continuous flow upgrading of glycerol toward oxiranes and active pharmaceutical ingredients thereof

2019 ◽  
Vol 21 (16) ◽  
pp. 4422-4433 ◽  
Author(s):  
Romain Morodo ◽  
Romaric Gérardy ◽  
Guillaume Petit ◽  
Jean-Christophe M. Monbaliu
Keyword(s):  
Amino Alcohol ◽  
Continuous Flow ◽  
Value Added ◽  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients

A robust continuous flow procedure for the transformation of bio-based glycerol into high value-added β-amino alcohol active pharmaceutical ingredients.

scholarly journals Ketone Reductase Biocatalysis in the Synthesis of Chiral Intermediates Toward Generic Active Pharmaceutical Ingredients

2020 ◽  
Vol 24 (6) ◽  
pp. 1131-1140
Author(s):  
Marina Y. Raynbird ◽  
Joanne B. Sampson ◽  
Dan A. Smith ◽  
Siân M. Forsyth ◽  
Jonathan D. Moseley ◽  
...  
Keyword(s):  
Active Pharmaceutical Ingredients ◽  
Pharmaceutical Ingredients ◽  
Chiral Intermediates
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