Organic synthesis in a modular robotic system driven by a chemical programming language

The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an abstraction that maps commonly reported methodological instructions into discrete steps amenable to automation. These unit operations were impl...

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Published in:Science (American Association for the Advancement of Science) Vol. 363; no. 6423
Main Authors: Steiner, Sebastian, Wolf, Jakob, Glatzel, Stefan, Andreou, Anna, Granda, Jarosław M, Keenan, Graham, Hinkley, Trevor, Aragon-Camarasa, Gerardo, Kitson, Philip J, Angelone, Davide, Cronin, Leroy
Format: Journal Article
Language:English
Published: United States 11.01.2019
ISSN:1095-9203, 1095-9203
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Abstract The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an abstraction that maps commonly reported methodological instructions into discrete steps amenable to automation. These unit operations were implemented in a modular robotic platform by using a chemical programming language that formalizes and controls the assembly of the molecules. We validated the concept by directing the automated system to synthesize three pharmaceutical compounds, diphenhydramine hydrochloride, rufinamide, and sildenafil, without any human intervention. Yields and purities of products and intermediates were comparable to or better than those achieved manually. The syntheses are captured as digital code that can be published, versioned, and transferred flexibly between platforms with no modification, thereby greatly enhancing reproducibility and reliable access to complex molecules.
AbstractList The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an abstraction that maps commonly reported methodological instructions into discrete steps amenable to automation. These unit operations were implemented in a modular robotic platform by using a chemical programming language that formalizes and controls the assembly of the molecules. We validated the concept by directing the automated system to synthesize three pharmaceutical compounds, diphenhydramine hydrochloride, rufinamide, and sildenafil, without any human intervention. Yields and purities of products and intermediates were comparable to or better than those achieved manually. The syntheses are captured as digital code that can be published, versioned, and transferred flexibly between platforms with no modification, thereby greatly enhancing reproducibility and reliable access to complex molecules.The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an abstraction that maps commonly reported methodological instructions into discrete steps amenable to automation. These unit operations were implemented in a modular robotic platform by using a chemical programming language that formalizes and controls the assembly of the molecules. We validated the concept by directing the automated system to synthesize three pharmaceutical compounds, diphenhydramine hydrochloride, rufinamide, and sildenafil, without any human intervention. Yields and purities of products and intermediates were comparable to or better than those achieved manually. The syntheses are captured as digital code that can be published, versioned, and transferred flexibly between platforms with no modification, thereby greatly enhancing reproducibility and reliable access to complex molecules.
The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an abstraction that maps commonly reported methodological instructions into discrete steps amenable to automation. These unit operations were implemented in a modular robotic platform by using a chemical programming language that formalizes and controls the assembly of the molecules. We validated the concept by directing the automated system to synthesize three pharmaceutical compounds, diphenhydramine hydrochloride, rufinamide, and sildenafil, without any human intervention. Yields and purities of products and intermediates were comparable to or better than those achieved manually. The syntheses are captured as digital code that can be published, versioned, and transferred flexibly between platforms with no modification, thereby greatly enhancing reproducibility and reliable access to complex molecules.
Author Angelone, Davide
Cronin, Leroy
Andreou, Anna
Wolf, Jakob
Aragon-Camarasa, Gerardo
Hinkley, Trevor
Kitson, Philip J
Glatzel, Stefan
Granda, Jarosław M
Steiner, Sebastian
Keenan, Graham
Author_xml – sequence: 1
  givenname: Sebastian
  orcidid: 0000-0001-9582-427X
  surname: Steiner
  fullname: Steiner, Sebastian
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 2
  givenname: Jakob
  orcidid: 0000-0003-0201-2745
  surname: Wolf
  fullname: Wolf, Jakob
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 3
  givenname: Stefan
  orcidid: 0000-0002-0744-0135
  surname: Glatzel
  fullname: Glatzel, Stefan
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 4
  givenname: Anna
  surname: Andreou
  fullname: Andreou, Anna
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 5
  givenname: Jarosław M
  orcidid: 0000-0002-5058-7669
  surname: Granda
  fullname: Granda, Jarosław M
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 6
  givenname: Graham
  orcidid: 0000-0002-6237-2681
  surname: Keenan
  fullname: Keenan, Graham
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 7
  givenname: Trevor
  orcidid: 0000-0002-4834-7631
  surname: Hinkley
  fullname: Hinkley, Trevor
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 8
  givenname: Gerardo
  surname: Aragon-Camarasa
  fullname: Aragon-Camarasa, Gerardo
  organization: School of Computer Science, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 9
  givenname: Philip J
  orcidid: 0000-0003-1826-1869
  surname: Kitson
  fullname: Kitson, Philip J
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 10
  givenname: Davide
  orcidid: 0000-0001-8879-907X
  surname: Angelone
  fullname: Angelone, Davide
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK
– sequence: 11
  givenname: Leroy
  orcidid: 0000-0001-8035-5757
  surname: Cronin
  fullname: Cronin, Leroy
  email: lee.cronin@glasgow.ac.uk
  organization: School of Chemistry, The University of Glasgow, Glasgow G12 8QQ, UK. lee.cronin@glasgow.ac.uk
BackLink https://www.ncbi.nlm.nih.gov/pubmed/30498165$$D View this record in MEDLINE/PubMed
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Snippet The synthesis of complex organic compounds is largely a manual process that is often incompletely documented. To address these shortcomings, we developed an...
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