1259404-17-5Relevant articles and documents
Short enantioselective total synthesis of (+)-tofacitinib
Mane, Kishor D.,Kamble, Rohit B.,Suryavanshi, Gurunath
, (2021)
An enantioselective total synthesis of Tofacitinib (CP-690,550), a Janus tyrosine kinase (JAK3) specific inhibitor has been achieved from the readily available 4-piperidone. Proline catalysed hydroxylation is the key step for the synthesis of enantiopure 1-benzyl-4-methylpiperidin-3-ol.
Synthesis method of tofacitinib citrate diastereomer impurities
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, (2021/10/27)
The invention discloses a synthesis method of tofacitinib citrate diastereomer impurities, relates to the technical field of drug organic synthesis, and relates to 3 - amino -4 - methylpyridine as a starting material and a quaternary ammonium salt. Raw materials of the whole synthetic route are easily available, the reaction conditions are mild, the post-treatment separation and purification operation is simple and feasible, and the preparation method is good in repeatability.
Preparation method of tofacitinib or salt thereof (by machine translation)
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, (2020/06/20)
The preparation method of the tofacitinib intermediate V compound comprises the following steps: (1) a compound II and a compound III are subjected to a photoreaction reaction to generate an intermediate IV; (2) an intermediate IV and a methylation reagent are subjected to methylation reaction to generate a compound of formula V; wherein R is. 1 And R2 Are each independently an amino protecting group. The preparation method disclosed by the invention does not need to be subjected to isomer resolution purification in the preparation method, avoids using tetrahydroaluminum hydride, is low in synthesis cost, high in yield, simple in reaction condition and post-treatment operation and suitable for industrial production. (by machine translation)