Synthetic Methods for Simvastatin – an Overview | ||||
Journal of Pharmaceutical and Applied Chemistry | ||||
Volume 5, Issue 1, January 2019, Page 1-21 PDF (494.2 K) | ||||
Document Type: Original Article | ||||
DOI: 10.18576/jpac/050103 | ||||
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Authors | ||||
Chandra Kant Belwal; Jaimin Patel | ||||
Research and Process Development, Sterling Biotech Limited, Jambusar State Highway, Vadodara, Gujarat-391421, India | ||||
Abstract | ||||
There are three basic methodologies for simvastatin production; biosynthesis or the fermentation technology method using fungal stains, biocatalytic method to convert lovastatin into simvastatin and synthetic methods for modification of lovastatin into simvastatin. Out of all three methodologies, synthetic modifications of lovastatin into simvastatin are commercialized and widely used methodologies. There are two possible synthetic routes for simvastatin; direct alkylation route and re-esterification route. Relatively high yield and fewer synthetic steps are the main advantages of adopting direct alkylation route while re-esterification route, wherein the 2-methyl butyrate side chain is completely removed and 2,2-dimethylbutyrate side chain is introduced, gives better quality of simvastatin, as the separation of the hydrolyzed product and the esterified product is much easier to achieve compared to the unreacted starting material and the methylated product. | ||||
Keywords | ||||
Simvastatin; Lovastatin; HMG Co-A reductase; Re-esterification; Direct methylation | ||||
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