4.4 Article

An Efficient Enantioselective Total Synthesis of Atorvastatin -Calcium

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SYNLETT
卷 34, 期 3, 页码 283-287

出版社

GEORG THIEME VERLAG KG
DOI: 10.1055/a-1970-8386

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total synthesis; statins; atorvastatin calcium; Paal-Knorr Reaction; enantioselectivity

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A concise and efficient synthesis method for the production of atorvastatin calcium, a key cholesterol-lowering drug, has been presented.
A concise and efficient asymmetric synthesis of tert-butyl [(4R,6R)-6-(2-aminoethyl)-2,2-dimethyl-1,3-dioxan-4-yl]acetate is presented. This key chiral-chain precursor of atorvastatin was synthesized from a commercially available inexpensive starting material, and was converted into atorvastatin calcium. The synthesis has the potential for scale up, and could be used to produce atorvastatin calcium on an industrial scale.

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