☆ 4.7 Review

Multistep automated synthesis of pharmaceuticals

TRENDS IN CHEMISTRY (2023)

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Adam D. Clayton et al.

Summary: The optimization of multistep chemical syntheses is crucial for rapid development of new pharmaceuticals. A continuous flow platform was developed to automate the optimization of telescoped reactions. By integrating Bayesian optimization techniques, an 81% overall yield was achieved in just 14 hours, and a favorable competing pathway for the desired product was identified.

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Summary: This study demonstrates the continuous-flow synthesis of (R)-tamsulosin without the need for the isolation or purification of any intermediates or byproducts. The synthesis was achieved through four catalytic transformations in a flow stream, resulting in a high yield and enantiomeric excess.

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Summary: Fully automated synthetic chemistry has the potential to revolutionize the field by providing on-demand access to small molecules. The development of a new class of stable TIDA boronates enables the automated stereospecific assembly of Csp(3)-C bonds, expanding the range of reactions that can be run autonomously. This breakthrough allows for the synthesis of increasingly complex Csp(3)-rich small molecules via automated assembly.

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Simon Rohrbacht et al.

Summary: Despite potential, the automation of synthetic chemistry has only made slow progress in recent decades. In this study, we introduce an automated chemical reaction database with 100 representative molecules. Through robotic experimentation, over 50 reactions from the database were performed, achieving yields and purities comparable to those achieved by experts.

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Summary: Computer-aided synthesis planning (CASP) tools are used to propose synthesis routes for organic compounds, but experimental development is still needed due to limited data availability. This study optimizes a CASP-proposed synthesis route for sonidegib on a robotic flow synthesis platform. Human insights and multi-objective Bayesian optimization improve yield and catalyst activity, while the platform's modularity and flexibility are essential for controlling reaction conditions.

ACS CENTRAL SCIENCE (2022)

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An Adaptive Auto-Synthesizer using Online PAT Feedback to Flexibly Perform a Multistep Reaction

Junliang Liu et al.

Summary: Researchers have developed an adaptive auto-synthesizer that uses online HPLC and FTIR measurements to adapt to the changing reactivities of different substrates, allowing precise control of reaction conditions.

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Jiao Jiao et al.

Summary: Continuous-flow multi-step synthesis utilizes microchannel flow chemistry to transform traditional organic synthesis, requiring innovative methods to address challenges. Recent years have seen significant progress with green reactions, telescoped design, and novel separation techniques, leading to successful preparation of complex APIs.

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Davide Angelone et al.

Summary: The study demonstrates that the Chemputer synthesis robot can be programmed to perform a variety of reactions, including solid-phase peptide synthesis, iterative cross-coupling, and diazirine chemistry. Developing universal and modular hardware that can be automated makes various batch chemistry accessible. The research also showcases a complex convergent robotic synthesis, highlighting the utility of the Chemputer system.

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Summary: In a rapidly changing environment like the current COVID-19 pandemic, continuous flow reactors show potential for increasing the production of urgently needed active pharmaceutical ingredients (APIs) on demand. A flash chemistry approach using organolithium reagents has led to significant improvements in the synthesis of remdesivir, particularly in the C-glycosylation step, allowing for higher yield and faster production in a continuous flow system.

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Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis

Chenguang Liu et al.

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Standardization and Control of Grignard Reactions in a Universal Chemical Synthesis Machine using online NMR

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Summary: The lack of standardization in chemistry literature leads to reproducibility difficulties and dependence on tacit knowledge; online NMR integration with automated chemical synthesis machine enables real-time analysis and adjustment of reactions; validation experiments demonstrate the potential of Chemputer in dynamically controlling synthesis processes.

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CHEMICAL SCIENCE (2021)

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Ready, Set, Flow! Automated Continuous Synthesis and Optimization

Christopher P. Breen et al.

Summary: Synthetic chemistry has opened up new possibilities for innovation in key industries such as medicine, energy, and agriculture. Automation is challenging the traditional process of chemical synthesis, while continuous flow chemistry presents a flexible platform for automation. The merger of synthesis and automation is expected to democratize access to custom complex small molecules and accelerate the development of new synthetic protocols.

TRENDS IN CHEMISTRY (2021)

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Automated self-optimisation of multi-step reaction and separation processes using machine learning

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Enantioselective Sequential-Flow Synthesis of Baclofen Precursor via Asymmetric 1,4-Addition and Chemoselective Hydrogenation on Platinum/Carbon/Calcium Phosphate Composites

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The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology

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

Zsolt Fulop et al.

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Efficient Flow Synthesis of Human Antimicrobial Peptides*

John S. Albin et al.

AUSTRALIAN JOURNAL OF CHEMISTRY (2020)

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Multivariate analysis of inline benchtop NMR data enables rapid optimization of a complex nitration in flow

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A Consolidated and Continuous Synthesis of Ciprofloxacin from a Vinylogous Cyclopropyl Amide

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Seven-Step Continuous Flow Synthesis of Linezolid Without Intermediate Purification

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From p-Xylene to Ibuprofen in Flow: Three-Step Synthesis by a Unified Sequence of Chemoselective C-H Metalations

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Redesign of a Grignard-Based Active Pharmaceutical Ingredient (API) Batch Synthesis to a Flow Process for the Preparation of Melitracen HCl

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Across-the-World Automated Optimization and Continuous-Flow Synthesis of Pharmaceutical Agents Operating Through a Cloud-Based Server

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