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Pharmaceutical Regulatory Affairs: Open Access

Pharmaceutical Regulatory Affairs: Open Access

ISSN: 2167-7689

Open Access
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Free Pharmaceutical Chemistry Organic Process Research Journals

A range of generic active pharmaceutical ingredients has been examined for patterns and potential chiral alcohol derivatives within their structures that could be used as key synthetic intermediates. For seven generic active pharmaceutical ingredients (API), eight precursor ketones were acquired and then subjected to a reduction of> 400 ketone reductases commercially available from different suppliers. Positive screening results were obtained for five screened ketones, with several ketone reductases available for each successful ketone. Selectivity was generally> 99.5% ee in most cases, including for the opposite enantiomer. The best three examples were then optimized and quickly scaled to the 1 L scale with high conversion and isolated yield while maintaining selectivity> 99.5% ee for the desired chiral alcohol enantiomer . This work illustrates that where a wide range of enzymes is available, enzymes that are productive to give one or the other enantiomer of alcohol can be easily identified for many ketones and quickly scaled up to produce alcohols. chirals. This approach is particularly applicable to the generation of chiral API intermediaries

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Citations: 533

Pharmaceutical Regulatory Affairs: Open Access received 533 citations as per Google Scholar report

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