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Issue 5, 2014
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Concise synthesis of atorvastatin lactone under high-speed vibration milling conditions

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Abstract

The Hantzsch-type sequential three-component reaction under high-speed vibration milling conditions between 4-methyl-3-oxo-N-phenylpentanamide, tert-butyl 2-[(4R,6R)-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxan-4-yl]acetate and 1-(4-fluorophenyl)-2-iodo-2-phenylethanone in the presence of ytterbium triflate and silver nitrate, followed by hydrolytic deprotection/lactonization, afforded atorvastatin lactone in 38% overall yield, thus providing ready access to the top-selling antihyperlipidemic drug atorvastatin calcium.

Graphical abstract: Concise synthesis of atorvastatin lactone under high-speed vibration milling conditions

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Publication details

The article was received on 24 Feb 2014, accepted on 15 Apr 2014 and first published on 16 Apr 2014


Article type: Research Article
DOI: 10.1039/C4QO00052H
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Org. Chem. Front., 2014,1, 458-463

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    Concise synthesis of atorvastatin lactone under high-speed vibration milling conditions

    V. Estévez, M. Villacampa and J. C. Menéndez, Org. Chem. Front., 2014, 1, 458
    DOI: 10.1039/C4QO00052H

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