94061-80-0Relevant academic research and scientific papers
PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF
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, (2012/01/14)
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.
Methods for predicting the response to statins
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, (2011/10/13)
The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
Facile and highly enantioselective synthesis of (+)- and (-)-fluvastatin and their analogues
Zacharia, James T.,Tanaka, Takanori,Hayashi, Masahiko
supporting information; experimental part, p. 7514 - 7518 (2011/02/22)
A highly enantioselective synthesis of (+)- and (-)-fluvastatin and their analogues has been facilitated by the reaction of an aldehyde with diketene in the presence of Ti(O-i-Pr)4 and a chiral Schiff base ligand. Either enantiomer of the Schiff base could be employed to obtain (+)- or (-)-fluvastatin. Diastereoselective reductions of the resultant keto moiety of β-hydroxy ketoesters provided the syn-1,3-diol esters (91% ee), which were subsequently recrystallized and saponified to afford (+)- and (-)-fluvastatin in >99.9% ee.
PROCESS FOR PREPARATING ENANTIOMERICALLY PURE FLUVASTATIN SODIUM AND A NOVEL POLYMORPHIC FORM THEREOF
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Page/Page column 22-23, (2008/06/13)
The present invention provides processes for preparing enantiomerically pure fluvastatin sodium. The present invention also provides pharmaceutical compositions comprising the enantiomerically pure fluvastatin sodium for antagonizing HMG-CoA. In addition
PROCESS AND INTERMEDIATES FOR THE SELECTIVE SYNTHESIS OF FLUVASTATIN
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Page/Page column 11, (2010/10/20)
The invention relates to process for the selective preparation of 3-hydroxy-6-dialkoxyphosphoryl-5-oxo-hexanoic acid esters, comprising a first step, in which a methylphosphonic acid dialkylester is treated with a base, and a second step, in which the pro
PROCESS FOR THE PREPARATION OF AMORPHOUS FLUVASTATIN SODIUM
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Page/Page column 3-4, (2008/06/13)
The present invention relates to a novel process for the preparation of the HMG-CoA reductase inhibitor, fluvastatin, more specifically to a process for the preparation of amorphous form of fluvastatin sodium.
Asymmetric synthesis of 3,5-dihydroxy-6(E)-heptenoate-containing HMG-CoA reductase inhibitors
Tempkin, Orin,Abel, Stephan,Chen, Chung-Pin,Underwood, Russell,Prasad, Kapa,Chen, Kau-Ming,Repic, Oljan,Blacklock, Thomas J.
, p. 10659 - 10670 (2007/10/03)
A 'one-pot' conversion of aldehyde 6 to hydroxyketoester 10 with high enantioselection, culminating in a practical asymmetric synthesis of (3R,5S) isomer of the antihyperlipoproteinemic agent fluvastatin, 1, is described. All four 3,5-dihydroxy-6(E)-heptenoate stereoisomers were prepared in enantiopure form starting from 10, utilizing selective reduction and oxidation methods.
