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Synthesis of deuterium-labeled (3R, 5S)-fluvastatin and (3S, 5R)-fluvastatin

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Abstract

In order to comprehensively understanding the metabolism process of fluvastatin, the stable isotope-labeled (3R, 5S)-fluvastatin and (3S, 5R)-fluvastatin were required. Both of (3R, 5S)-fluvastatin and (3S, 5R)-fluvastatin were synthesized via a seven steps procedure starting from aniline and [2H6] 2-bromopropane. Two versions of deuterium labeled compound revealed over 98% deuterium enrichment, using as an internal standard.

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Funding

Funding was provided by National Natural Science Foundation of China (Grant No. 41472124), PetroChina Innovation Foundation (Grant Nos. 2015D-5006-0210 and 2016D-5007-0702) and Nature Science Foundation of Hubei Province (Grant No. 2016CFB178).

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Correspondence to Lei Tian.

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He, M., Li, J. & Tian, L. Synthesis of deuterium-labeled (3R, 5S)-fluvastatin and (3S, 5R)-fluvastatin. J Radioanal Nucl Chem 319, 263–269 (2019). https://doi.org/10.1007/s10967-018-6279-1

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  • DOI: https://doi.org/10.1007/s10967-018-6279-1

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