862994-56-7

Upstream product

• 355806-00-7 rosuvastatin tert-butyl ester 
• 108-18-9 diisopropylamine 
• 925422-06-6 N-[5-chloromethyl-4-(4-fluorophenyl)-6-isopropyl-pyrimidin-2-yl]-N-methyl-methanesulfonamide 
• 1353637-14-5 E-(7-{2-(N-methyl-N-methanesulfonylamino)-4-(4-fluorophenyl)-6-isopropyl-pyrimidin-5-yl}-[(3R,5S)-3,5-dihydroxy-hept-6-enoic acid])-N-methoxy-N-methyl-amide 
• 1353637-13-4 E-(6-{2-[2-(N-methyl-N-methanesulfonylamino)-4-(4-fluorophenyl)-6-isopropyl-pyrimidin-5-yl]vinyl}-[(4R,6S)-2,2-dimethyl-[1,3]dioxan-4-yl])-N-methoxy-N-methyl-acetamide 
• 1353637-12-3 2-[(4R,6S)-2,2-dimethyl-6-(1-phenyl-1H-tetrazole-5-sulfonylmethyl)-[1,3]dioxan-4-yl]-N-methoxy-N-methyl-acetamide 
• 1353637-11-2 2-[(4R,6S)-6-formyl-2,2-dimethyl-[1,3]dioxan-4-yl]-N-methoxy-N-methylacetamide 
• 1353637-09-8 2-[(4R,6S)-6-hydroxymethyl-2,2-dimethyl-[1,3]dioxan-4-yl]-N-methoxy-N-methylacetamide 
• 1353637-28-1 2-[(4R,6S)-6-methanesulfonyloxymethyl-2,2-dimethyl-[1,3]dioxan-4-yl]-N-methoxy-N-methyl-acetamide 
• 1353637-26-9 [(4R,6S)-6-methanesulfonyloxymethyl-2,2-dimethyl-[1,3]dioxan-4-yl]-acetic acid 
• 1234331-53-3 N-{5-[(benzo[d]thiazol-2-ylthio)methyl]-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl}-N-methylmethanesulfonamide 
• 853066-73-6 tributyl[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-ylmethyl]phosphonium bromide 
• 799842-07-2 N-[5-(bromomethyl)-4-(4-fluorophenyl)-6-(propan-2-yl)pyrimidin-2-yl]-N-methylmethanesulfonamide 
• 147118-30-7 ethyl 2-(N-methyl-N-methanesulfonylamino)-4-(4-fluorophenyl)-6-isopropyl-pyrimidin-5-carboxylic acid 

Relevant academic research and scientific papers

PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF

The present invention provides an improved process for preparing HMG-CoA reductase inhibitors such as rosuvasatin calcium, fluvastatin sodium, and pitavastatin calcium under a mild condition, using a novel amide-bond-containing compound having R2-N-O-R1 moiety as a key intermediate. And also, the present invention provides the novel compound, an intermediate useful for the preparation thereof, and a process for the preparation thereof.

PROCESS FOR PREPARING AMORPHOUS ROSUVASTATIN CALCIUM FREE OF IMPURITIES

A pure amorphous form of rosuvastatin calcium having purity of more than 99.5%, preferably a purity of more than 99.8%, more preferably a purity of more than 99.9% as determined by HPLC area percentage, and free from any traces of alkali metal impurities is disclosed. A process of preparing said pure amorphous form of rosuvastatin calcium is disclosed, which comprises hydrolysis of C1-C5 alkyl esters of rosuvastatin, preferably terf-butyl ester of rosuvastatin, with an organic nitrogen base, e.g. guanidines, amidines, amines and quaternary ammonium hydroxides, in the presence of water, optionally containing aprotic solvent, following the conversion of thus obtained rosuvastain salt with a source of calcium to desired rosuvastatin calcium, which is then isolated. An alternative process is disclosed, which comprises the conversion of numerous novel ammonium salts of rosuvastatin, preferably tert-octylammonium salt of rosuvastatin, with the source of calcium to desired commercial rosuvastatin calcium.. Rosuvastatin calcium is HMG CoA reductase, useful in the treatment of hyperlipidemia, hypercholesterolemia and atherosclerosis.