- PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATES THEREOF
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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.
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- Methods for predicting the response to statins
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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.
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- Facile and highly enantioselective synthesis of (+)- and (-)-fluvastatin and their analogues
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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.
- Zacharia, James T.,Tanaka, Takanori,Hayashi, Masahiko
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supporting information; experimental part
p. 7514 - 7518
(2011/02/22)
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- PROCESS FOR THE PREPARATION OF AMORPHOUS FLUVASTATIN SODIUM
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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.
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Page/Page column 3-4
(2008/06/13)
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- PROCESS FOR PREPARATING ENANTIOMERICALLY PURE FLUVASTATIN SODIUM AND A NOVEL POLYMORPHIC FORM THEREOF
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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
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Page/Page column 22-23
(2008/06/13)
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- PROCESS AND INTERMEDIATES FOR THE SELECTIVE SYNTHESIS OF FLUVASTATIN
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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
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Page/Page column 11
(2010/10/20)
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- Asymmetric synthesis of 3,5-dihydroxy-6(E)-heptenoate-containing HMG-CoA reductase inhibitors
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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.
- Tempkin, Orin,Abel, Stephan,Chen, Chung-Pin,Underwood, Russell,Prasad, Kapa,Chen, Kau-Ming,Repic, Oljan,Blacklock, Thomas J.
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p. 10659 - 10670
(2007/10/03)
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