4.7 Article

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

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ORGANIC CHEMISTRY FRONTIERS
卷 1, 期 5, 页码 458-463

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ROYAL SOC CHEMISTRY
DOI: 10.1039/c4qo00052h

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  1. Ministerio de Economia y Competitividad, MINECO [CTQ2012-33272-BQU]
  2. Comunidad Autonoma de Madrid

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The Hantzsch-type sequential three-component reaction under high-speed vibration milling conditions between 4-methyl-3-oxo-N-phenylpentanamide, tert-butyl 2-1(4R,6R)-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxan-4-yll-acetate and 1-14-ffuoropheny0-2-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.

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