901765-35-3

Upstream product

• 894787-92-9 N-(5-bromo-4-(4-fluorophenyl)-6-isopropylpyriinidin-2-yl)-N-methylmethanesulfonamide 
• 107-13-1 acrylonitrile 
• 7605-28-9 2-(phenylsulfonyl)acetonitrile 
• 147118-37-4 N-[4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide 

Downstream Products

• 890028-66-7 (E)-N-[4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-en-1-yl)pyrimidin-2-yl]-N-methyl methanesulfoneamide 

Relevant academic research and scientific papers

METHOD FOR PRODUCING ROSUVASTATIN CALCIUM INTERMEDIATE

PROBLEM TO BE SOLVED: To provide an efficient production method for a compound that is a rosuvastatin calcium intermediate. SOLUTION: The production method has a step for the condensation of a compound represented by formula (I) and a compound represented

A (E)- 3 - [4 - (4 - fluorophenyl) - 6 - isopropyl - 2 - (N - methyl - N - a sulfuryl amidogen) pyrimidine - 5 - yl] acrolein preparation method

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.

A (E)- 3 - [4 - (4 - fluorophenyl) - 6 - isopropyl - 2 - (N - methyl - N - a sulfuryl amidogen) pyrimidine - 5 - yl] acrolein synthetic method

The invention discloses a method for synthesizing (E)-3-[4-(4-fluorophenyl)-6-isopropyl-2-(N-methyl-N-methane sulfonamide) pyrimidine-5-yl] acraldehyde used as a rosuvastatin calcium intermediate. The synthesizing method comprises the following steps: reacting a compound in formula III with substituted sulphonate or substituted sulfinic acid ester in the existence of a metal reagent, generating a compound in a formula II under the effect of an eliminating reagent and converting into a product, wherein in the formula II, R is chosen from -CN. The method is simple in process and low in cost, the expensive catalyst is avoided and the byproduct is effectively reduced, so that the after treatment is simple and easy to operate, the reaction yield is greatly increased and the method is suitable for large scale industrial production. The formulae are as shown in the specification.

PROCESS FOR THE PREPARATION OF ROSUVASTATIN

A process for the manufacture of a compound of formula (V), useful for making rosuvastatin, by a stereoselective aldol reaction is described.

PROCESSES FOR THE MANUFACTURE OF ROSUVASTATIN AND INTERMEDIATES

A process for the manufacture of a compound of formula (V), useful for making rosuvastatin, by a stereoselective aldol reaction is described. Novel intermediates and processes to make them are also described.