Synthesis of the related substances of tofacitinib citrate
Five related substances of tofacitinib citrate were synthesized to provide references for the quality control of tofacitinib.Using N-methyl-N-[(3R,4R)-4-methylpiperidin-3-yl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine(7)as the starting material,methylation with formaldehyde formed related substance A.Using compound 7 as the starting material,the condensations of the carboxyl group with different amide substrates gave related substances B and C.Using compound 7 as the starting material,the oxidation and reduction reaction formed related substance D.Using tofacitinib(9)as the starting material,the oxidation reaction formed related substance E.The structures of five impurities were confirmed by 1H-NMR and ESI-MS,and the purities of all impurities were higher than 95％(HPLC),which could be used for the quality study of tofacitinib citrate.
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