An Improved Manufacturing Process for Fluvastatin

Fuenfschilling, Peter C.; Hoehn, Pascale; Mutz, Jean-Paul

doi:10.1021/op060191b

Cited by 33 publications

(19 citation statements)

References 9 publications

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“…However, to the best of our knowledge, fluvastatin has been approved as a racemic form. In fact, the Novartis group has reported the manufacturing of racemic fluvastatin 56. As for the chiral version, Prasad and his Novartis group reported a method employing the Wadsworth–Horner–Emmons reaction 57.…”

Section: Enantioselective Addition Of Diketene To Aldehydesmentioning

confidence: 99%

Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions

Hayashi

2016

The Chemical Record

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In this Personal Account, various chiral Schiff base-metal-catalyzed enantioselective organic reactions are reported; the Schiff bases used were O,N,O- as well as N,N,P-tridentate ligands and N,N-bidentate ligands having C symmetry. In particular, the enantioselective addition of trimethylsilyl cyanide, dialkylzinc, and organozinc halides to aldehydes, enantioselective 1,4-addition of dialkylzinc to cyclic and acyclic enones, and asymmetric allylic oxidation are reported. Typically, ketimine-type Schiff base-metal complexes exhibited higher reactivity and enantioselectivity compared with the corresponding aldimine-type Schiff base-metal complexes. Notably, remarkable ligand acceleration was observed for all reactions. The obtained products can be used as key intermediates for optically active natural products and pharmaceuticals.

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Section: Enantioselective Addition Of Diketene To Aldehydesmentioning

confidence: 99%

Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions

Hayashi

2016

The Chemical Record

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“…Therefore, there was a little room left for marginal improvements of the synthesis of fluvastatin and its building blocks. Consequently, studies in this area are scarce [10,112].…”

Section: Fluvastatinmentioning

confidence: 99%

Recent Progress in the Synthesis of Super-Statins

Časar

2015

Topics in Heterocyclic Chemistry

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Super-statins now represent a mature class of marketed drugs that faces the patent cliff, as has already occurred for fluvastatin and atorvastatin and is approaching for rosuvastatin and pitavastatin. However, they continue to trigger huge scientific interest in terms of their efficient preparation. This is not surprising, as easier accessibility of super-statins will promote even bigger demand in the market and consequently the need for higher rates of the production and productivity. Therefore, the stimulus for the development of even more efficient synthetic approaches to the heterocyclic moieties of super-statins and their chiral lateralchain precursors is at a peak, as also for the assembly of the these two parts into super-statins. The present report summarizes recent developments in the field of the synthesis of super-statins published from 2010 to 2015. Emphasis is given to the analysis of novel approaches to the formation of the chiral statin lateral chain, with detailed discussion of the development of new routes to respective heterocyclic cores and the assembly of these key units into the final super-statin structure.

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“…In 2007, the technical know-hows in the manufacturing of artemether and benflumetol were opened [190], including the reduction of QHS with potassium borohydride and replacement of methylene dichloride by methyl acetate in the manufacture of artemether. These effective measures will reduce production cost.…”

Section: Synthesis and Antimalarial Activity Of Qhs Derivatives And Amentioning

confidence: 99%

A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu

Liu

2010

Front. Chem. China

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Qinghaosu (QHS) and its derivatives are a new generation of antimalarial drugs characterized by fast action, high efficacy, and good tolerance. This feature article states the discovery of QHS from traditional Chinese medicine qinghao (Artemisia annua L.) and reviews the progress during the past four decades in the research of phytochemistry of A. annua, chemical reactions and biotransformation of QHS, chemical synthesis and biosynthesis of QHS, synthesis and antimalarial activity of QHS derivatives and analogs, pharmacological studies, clinical application, and the antimalarial mechanism. Undoubtedly, QHS is an example of the value of traditional Chinese medicine in modern medicinal research.

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An Improved Manufacturing Process for Fluvastatin

Cited by 33 publications

References 9 publications

Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions

Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions

Recent Progress in the Synthesis of Super-Statins

A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu

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An Improved Manufacturing Process for Fluvastatin

Cited by 33 publications

References 9 publications

Progress of Chiral Schiff Bases with C1 Symmetry in Metal‐Catalyzed Asymmetric Reactions

Progress of Chiral Schiff Bases with C1 Symmetry in Metal‐Catalyzed Asymmetric Reactions

Recent Progress in the Synthesis of Super-Statins

A golden phoenix arising from the herbal nest — A review and reflection on the study of antimalarial drug Qinghaosu

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Product

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Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions

Progress of Chiral Schiff Bases with C₁ Symmetry in Metal‐Catalyzed Asymmetric Reactions