124752-23-4Relevant articles and documents
A new way to tert-Butyl [(4R,6R)-6-aminoethyl-2,2-dimethyl-1,3-dioxan-4-yl]acetate, a key intermediate of atorvastatin synthesis
Radl, Stanislav
, p. 2275 - 2283 (2003)
A new synthesis of tert-butyl [(4R,6R)-6-aminoethyl-2,2-dimethyl-1,3-dioxan-4-yl]acetate, a key intermediate of the synthesis of an effective HMG-CoA reductase inhibitor atorvastatin, is described. The synthesis is based on the Henry reaction of nitromethane and tert-butyl [(4R,6S)-6-formyl-2,2-dimethyl-1,3-dioxan-4-yl] acetate. The formed nitroaldol was then O-acetylated and the sodium borohydride reduction of the intermediate provided tert-butyl [(4R,6R)-2,2-dimethyl-6-nitroethyl-1,3-dioxan-4-yl] acetate. Catalytic hydrogenation of the nitro group led to the title compound.
Method for preparing rosuvastatin side chain through oxidation in continuous flow micro-channel reactor
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Paragraph 0042-0089, (2020/08/12)
The invention relates to a method for preparing a rosuvastatin side chain through oxidation in a continuous flow micro-channel reactor. In the micro-channel reactor, a compound D6 is oxidized by sodium hypochlorite to synthesize a compound D7; the reaction flow is shown in the specification. The method solves the problems that existing preparation methods are long in reaction time, high in requirements on reaction condition, incapable of continuous product, high in cost and the like. The method has the advantages of simplicity and safety in operation, short reaction time, high product conversion rate, high product purity and the like, materials after reaction can be directly subjected to aftertreatment operation, aftertreatment is simple, the product yield is 92% or above, the product purity is 99.8%, and the method is particularly suitable for industrial large-scale production.
Rosuvastatin calcium intermediate, preparation method thereof and application of intermediate
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Paragraph 0083-0085, (2019/04/17)
The invention discloses a rosuvastatin calcium intermediate, a preparation method thereof and an application of the intermediate. The synthesis process of the intermediate is environmentally friendly,simple and convenient to operate and low in EHS (environment health safety) risk, raw materials are easily available, and used chemical reagents are low in toxicity and low in price, so that the synthesis process of the intermediate is a green synthesis process suitable for industrial production. In addition, the intermediate is applied to synthesis of rosuvastatin calcium and key intermediates thereof, has short route and high yield, effectively reduces the industrial production cost of rosuvastatin calcium, and has a higher industrial application prospect.