A Practical Synthesis of Rosuvastatin and Other Statin Intermediates

Tartaggia, Stefano; Ferrari, Clark; Pontini, Marta; Lucchi, Ottorino De

doi:10.1002/ejoc.201500356

Cited by 18 publications

(11 citation statements)

References 52 publications

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“…This will trigger the continuous search for the more efficient, cheaper, and sustainable synthesis of statins [137] and in particular super-statins. This has already been reflected in some reports that have appeared in the literature since this review was written [138][139][140][141][142][143][144].…”

Section: Assembly Of Pitavastatinmentioning

confidence: 59%

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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Section: Assembly Of Pitavastatinmentioning

confidence: 59%

Recent Progress in the Synthesis of Super-Statins

Časar

2015

Topics in Heterocyclic Chemistry

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Section: Assembly Of Pitavastatinmentioning

confidence: 62%

Synthesis of Heterocycles in Contemporary Medicinal Chemistry

Časar¹

2016

Topics in Heterocyclic Chemistry

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The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community.The series consists of topic related volumes edited by renowned editors with contributions of experts in the field.More information about this series at

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“…Isoflavones, natural constituents of the benzopyran heterocycle family, are present in soybeans and many plants of the Leguminosae family . These compounds exhibit a wide range of biological activities such as anti‐cancer, anti‐inflammatory, antifungal, antimicrobial, and estrogenic activities . For example, daidzein is an isoflavone type found in many plants and herbs like Kwao Krua ( Pueraria Mirifica ) and Kudzu ( Pueraria lobata ).…”

Section: Introductionmentioning

confidence: 99%

A Catalyst‐Free Synthetic Route to Modified Isoflavone via Multi‐Component Reaction

Alizadeh

Bagherinejad

2020

ChemistrySelect

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A concise and efficient one-pot sequential approach for the synthesis of modified isoflavone was developed from a reaction of 3-formylchromones, malononitrile, various α,α-dicyanoolefines, using Et 3 N as the base, and EtOH as the solvent, in good yield. The value of this method lies in its short reaction time, convenient purification, no need for a metal catalyst, excellent efficiency, and green solvent. This synthesis involves a Knoevenagel condensation/carbanion formation/ring closure, and finally, an elimination to obtain the respective isoflavonoid derivatives.

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A Practical Synthesis of Rosuvastatin and Other Statin Intermediates

Abstract: The efficient aldol condensation between a derivative of methyl 3-hydroxy-5-oxohexanoate and a pyrimidinecarbaldehyde comprising the core structure of rosuvastatin has been developed as an alternative approach to the classical methods employing ylides for the synthesis of rosuvastatin.

Cited by 18 publications

References 52 publications

Recent Progress in the Synthesis of Super-Statins

Recent Progress in the Synthesis of Super-Statins

Synthesis of Heterocycles in Contemporary Medicinal Chemistry

A Catalyst‐Free Synthetic Route to Modified Isoflavone via Multi‐Component Reaction

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