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The syntheses and in vitro biotransformation studies of [^14^C]apixaban, a highly potent, selective, efficacious and orally bioavailable inhibitor of blood coagulation Factor Xa by Brad D. Maxwell; Scott B. Tran; Shiang-Yuan Chen; Donglu Zhang; Bang-Chi Chen; Huiping Zhang; Samuel J. Bonacorsi Jr is a Medicine article available to read on EtoBox.

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## Abstract Apixaban is a potent inhibitor of blood coagulation Factor Xa in the late stages of development. [^14^C]apixaban was synthesized with the 14C label in the two different lactam ring systems within the molecule for various __in vitro__ and __in vivo__ metabolism studies. A nine‐step synthesis of [^14^C]apixaban, **10**, with the label in the central lactam ring was completed in 14% overall yield. A second synthesis of [^14^C]apixaban, **14**, with the 14C label in the outer lactam ring was completed in three steps in a 14% overall yield. No significant differences were observed between the metabolite profiles of **10** and **14**, [^14^C]apixaban, from both rat and human hepatocyte or microsomal incubations. Copyright © 2011 John Wiley & Sons, Ltd.

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Author

Brad D. Maxwell; Scott B. Tran; Shiang-Yuan Chen; Donglu Zhang; Bang-Chi Chen; Huiping Zhang; Samuel J. Bonacorsi Jr

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0022-2135)

Published

2011

Language

EN

Field

Medicine (Life Sciences)