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.
Tofacitinib intermediate related substance and application thereof
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, (2021/04/03)
The invention belongs to the field of medicine synthesis, and particularly relates to a preparation method of tofacitinib intermediate related substances. The impurity is prepared by reacting a tofacitinib intermediate with 2-halogenated propane. By contr
Preparation method of tofacitinib or salt thereof (by machine translation)
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Paragraph 0055-0056; 0065-0068; 0077-0080; 0089-0092; 0099, (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)