ArticleNature chemistry2021
Automated synthesis of prexasertib and derivatives enabled by continuous-flow solid-phase synthesis.
Article in Nature chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed.
- Secondary-Amine Relay Enables Lysine-Directed Multicomponent Functionalization of Peptides.JACS Au · 2026Article
- Chemical ONature communications · 2026Article
- Review
- Advances in solid handling for continuous flow synthesis of specialty chemicals and pharmaceuticals.Communications chemistry · 2026Review
- Installation of d3-methyl group to drugs by continuous-flow solid-phase synthesis.Nature communications · 2025Article
- Article
- Ultrasound-Assisted Microcontinuous Process Facilitates the Selective Deuteration of Steroid Hormones.Journal of labelled compounds & radiopharmaceuticals · 2025Article
- Diversified Fluoroalkylation of Alkenes Using Quaternary Fluoroalkyl Alcohols as the Fluoroalkylating Reagents.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Artificial intelligence in drug development.Nature medicine · 2025Review
- DigiChemTree enables programmable light-induced carbene generation for on demand chemical synthesis.Communications chemistry · 2024Article
- Advances, opportunities, and challenges in methods for interrogating the structure activity relationships of natural products.Natural product reports · 2024Review
- Printed polymer platform empowering machine-assisted chemical synthesis in stacked droplets.Nature communications · 2024Article
- Synthesis of tertiary alkylphosphonate oligonucleotides through light-driven radical-polar crossover reactions.Nature communications · 2023Article
- Toward the Uniform of Chemical Theory, Simulation, and Experiments in Metaverse Technology.Precision chemistry · 2023Review
- A field guide to flow chemistry for synthetic organic chemists.Chemical science · 2023Review
- Natural and Man-Made Cyclic Peptide-Based Antibiotics.Antibiotics (Basel, Switzerland) · 2022Review
- The way to AI-controlled synthesis: how far do we need to go?Chemical science · 2022Review
- Bayesian Optimization of Computer-Proposed Multistep Synthetic Routes on an Automated Robotic Flow Platform.ACS central science · 2022Article
- Mostly 3D printed chemical synthesis robot.HardwareX · 2022Article
- Semiautomated synthesis of sequence-defined polymers for information storage.Science advances · 2022Article
Corrections and comments
- Commented on bySolid potential.2021
Authors and funding
10 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Recent advances in end-to-end continuous-flow synthesis are rapidly expanding the capabilities of automated customized syntheses of small-molecule pharmacophores, resulting in considerable industrial and societal impacts; however, many hurdles persist that limit the number of sequential steps that can be achieved in such systems, including solvent and reagent incompatibility between individual steps, cumulated by-product formation, risk of clogging and mismatch of timescales between steps in a processing chain. To address these limitations, herein we report a strategy that merges solid-phase synthesis and continuous-flow operation, enabling push-button automated multistep syntheses of active pharmaceutical ingredients. We demonstrate our platform with a six-step synthesis of prexasertib in 65% isolated yield after 32 h of continuous execution. As there are no interactions between individual synthetic steps in the sequence, the established chemical recipe file was directly adopted or slightly modified for the synthesis of twenty-three prexasertib derivatives, enabling both automated early and late-stage diversification.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.