1024024-26-7Relevant articles and documents
A (E)- 3 - [4 - (4 - fluorophenyl) - 6 - isopropyl - 2 - (N - methyl - N - a sulfuryl amidogen) pyrimidine - 5 - yl] acrolein preparation method
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Paragraph 0044; 0045; 0048, (2017/07/04)
The invention discloses a preparation method of (E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methanesulfonylamino) pyrimidine-5-yl] acrolein which can be used as a rosuvastatin intermediate. The preparation method comprises the following steps: reacting 4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methanesulfonylamino) pyrimidine-5-yl-formaldehyde with a sulfur ylide reagent under an alkaline condition to generate an epoxide shown in the formula III; then, reducing in the presence of a metal catalyst to generate a compound shown in the formula II; and finally reacting the compound shown in the formula II to generate the target product. The preparation method is simple in process and low in cost; no expensive catalyst is used; the generation of byproducts is reduced effectively so that the post-treatment becomes simple and easy to operate; in addition, the reaction yield is improved greatly; and therefore, the preparation method is quite suitable for large-scale industrial production.