1092844-00-2

Upstream product

• 1184-85-6 N-methylmethane sulphonamide 
• 29509-06-6 4-methyl-3-oxopentanonitrile 
• 459-57-4 4-fluorobenzaldehyde 
• 1416158-43-4 4-(4-fluorophenyl)-2-hydroxy-6-isopropylpyrimidine-5-carboxamide 
• 1416158-42-3 4-(4-fluorophenyl)-6-isopropyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxamide 
• 34126-90-4 4-methyl-3-oxopentanamide 
• 42558-54-3 Methyl 4-methyl-3-oxopentanoate 

Downstream Products

• 147118-37-4 N-[4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide 

Relevant academic research and scientific papers

A formyl rosuvastatin salts calcium intermediate preparation method

The invention discloses a preparation method of a formoxyl rosuvastatin calcium intermediate. With 2-methyl-3-carbonyl valeronitrile, 4-fluorobenzaldehyde and urea as raw materials, the formoxyl rosuvastatin calcium intermediate 4-(4-fluorophenyl)-2-hydroxy-6-isopropyl-5-formoxyl-2-(N-methyl-N-methylsulfonyl) pyrimidine is synthesized by reactions such as cyclization, oxidation, N-substitution and reduction. Compared with an existing method, the method has the advantages that reaction conditions are mild, the used reagent is relatively cheap and the yield is high.

Method for preparing rosuvastatin intermediate and intermediate compound (by machine translation)

The invention discloses a preparation method of a rosuvastatin intermediate: 4-(4-fluorobenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonyl amino) pyrimidine-5-formonitrile. The method comprises the following steps: carrying out a reaction on ethyl isobutyrate and acetonitrile to generate isobutyryl acetonitrile; and then carrying out cyclization, methylation, reduction, oxidization and substitution on isobutyryl acetonitrile and p-fluoro benzaldehyde as well as thiourea to prepare the intermediate. The 4-(4-fluorobenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonyl amino) pyrimidine-5-formonitrile prepared by the method is low in cost, simple to react, high in yield and easy to realize industrialized production.

IMPROVED PROCESS FOR PREPARING STATIN PRECURSOR

The present invention relates to a process for preparing a statin precursor, which process comprises a first reaction step, wherein a hydroxy-pyrimidine-carbonitrile is reacted with an organic sulfonyl halide to form the sulfonate-pyrimidine-carbonitrile; a second reaction step, wherein the sulfonate-pyrimidine-carbonitrile is reacted with N-methylmethane sulfonamide to form a pyrimidinyl-sulfonamide; and optionally a third reaction step, wherein the pyrimidinyl-sulfonamide is reacted with a reducing agent. All steps are conducted in toluene as the main solvent.

PROCESS FOR PREPARATION OF ROSUVASTATIN CALCIUM

Disclosed is the process for the preparation of 4-(fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)-5-formyl-pyrimidine of formula (I), which is the intermediate of rosuvastatin calcium. Purification of substantially pure acetonide protected tert-butyl ester of rosuvastatin (II) and its use for the preparation of substantially pure amorphous rosuvastatin calcium are also disclosed.