Synthesis of the antimalarial API artemether in a flow reactor

Polina Yaseneva; Dorota Plaza; Xiaolei Fan; Konstantin Loponov; Alexei Lapkin

doi:10.1016/j.cattod.2014.04.014

Synthesis of the antimalarial API artemether in a flow reactor

Polina Yaseneva
, Dorota Plaza
, Xiaolei Fan
, Konstantin Loponov
, Alexei Lapkin^*

^*Corresponding author for this work

Research output: Journal Publication › Article › peer-review

18 Citations (Scopus)

Abstract

The earlier developed flow protocol for stoichiometric reduction of an important biologically derivedpharmaceutical precursor, artemisinin, to dihydroartemisinin was extended to a sequential reaction toproduce one of the final APIs, artemether. A highly active heterogeneous catalyst was found for theetherification reaction. The use of QuadraSil catalyst allows to eliminate one step of reaction workup. Acomparative Life Cycle Assessment of both reactions has shown advantages of the flow process over theoptimized literature batch protocols. Results of LCA highlight the significance of solvents in pharmaceut-icals manufacture and the advantage of flow technology, enabling small solvent inventories to be used.

Original language	English
Pages (from-to)	90-96
Number of pages	7
Journal	Catalysis Today
Volume	239
DOIs	https://doi.org/10.1016/j.cattod.2014.04.014
Publication status	Published - 1 Jan 2015
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being
SDG 9 Industry, Innovation, and Infrastructure
SDG 12 Responsible Consumption and Production

Free Keywords

Acid catalysis
Artemisinin
Flow chemistry
Life cycle assessment
Malaria

ASJC Scopus subject areas

Catalysis
General Chemistry

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10.1016/j.cattod.2014.04.014

Cite this

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title = "Synthesis of the antimalarial API artemether in a flow reactor",

abstract = "The earlier developed flow protocol for stoichiometric reduction of an important biologically derivedpharmaceutical precursor, artemisinin, to dihydroartemisinin was extended to a sequential reaction toproduce one of the final APIs, artemether. A highly active heterogeneous catalyst was found for theetherification reaction. The use of QuadraSil catalyst allows to eliminate one step of reaction workup. Acomparative Life Cycle Assessment of both reactions has shown advantages of the flow process over theoptimized literature batch protocols. Results of LCA highlight the significance of solvents in pharmaceut-icals manufacture and the advantage of flow technology, enabling small solvent inventories to be used.",

keywords = "Acid catalysis, Artemisinin, Flow chemistry, Life cycle assessment, Malaria",

author = "Polina Yaseneva and Dorota Plaza and Xiaolei Fan and Konstantin Loponov and Alexei Lapkin",

note = "Publisher Copyright: {\textcopyright} 2014 Elsevier B.V.",

year = "2015",

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doi = "10.1016/j.cattod.2014.04.014",

language = "English",

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journal = "Catalysis Today",

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AU - Yaseneva, Polina

AU - Plaza, Dorota

AU - Fan, Xiaolei

AU - Loponov, Konstantin

AU - Lapkin, Alexei

PY - 2015/1/1

Y1 - 2015/1/1

N2 - The earlier developed flow protocol for stoichiometric reduction of an important biologically derivedpharmaceutical precursor, artemisinin, to dihydroartemisinin was extended to a sequential reaction toproduce one of the final APIs, artemether. A highly active heterogeneous catalyst was found for theetherification reaction. The use of QuadraSil catalyst allows to eliminate one step of reaction workup. Acomparative Life Cycle Assessment of both reactions has shown advantages of the flow process over theoptimized literature batch protocols. Results of LCA highlight the significance of solvents in pharmaceut-icals manufacture and the advantage of flow technology, enabling small solvent inventories to be used.

AB - The earlier developed flow protocol for stoichiometric reduction of an important biologically derivedpharmaceutical precursor, artemisinin, to dihydroartemisinin was extended to a sequential reaction toproduce one of the final APIs, artemether. A highly active heterogeneous catalyst was found for theetherification reaction. The use of QuadraSil catalyst allows to eliminate one step of reaction workup. Acomparative Life Cycle Assessment of both reactions has shown advantages of the flow process over theoptimized literature batch protocols. Results of LCA highlight the significance of solvents in pharmaceut-icals manufacture and the advantage of flow technology, enabling small solvent inventories to be used.

KW - Acid catalysis

KW - Artemisinin

KW - Flow chemistry

KW - Life cycle assessment

KW - Malaria

UR - https://www.scopus.com/pages/publications/84908231875

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DO - 10.1016/j.cattod.2014.04.014

M3 - Article

AN - SCOPUS:84908231875

SN - 0920-5861

VL - 239

SP - 90

EP - 96

JO - Catalysis Today

JF - Catalysis Today

ER -

Synthesis of the antimalarial API artemether in a flow reactor

Abstract

UN SDGs

Free Keywords

ASJC Scopus subject areas

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