1354621-59-2Relevant articles and documents
Formal asymmetric synthesis of (+)-tofacitinib
Liao, Hao-Chun,Uang, Biing-Jiun
, p. 105 - 109 (2017)
Tofacitinib is an efficient and selective Janus kinase 3 (JAK3) inhibitor, and is used as an immunosuppressant drug for the treatment of rheumatoid arthritis and transplant patients. Herein we report a concise formal asymmetric synthesis of tofacitinib from homochiral 1,3-dioxolanone 10b, which was elaborated through a highly stereoselective Michael addition followed by solvent-free removal of the chiral auxiliary and ring cyclization to furnish chiral imide 8. The preparation of tofacitinib's precursor 16 could be obtained after reduction of 8 followed by sequential oxidation, reductive amination and SNAr reactions.
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.
Novel method for preparing 3-amino-piperidine
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Paragraph 0054-0058, (2020/10/10)
The present invention relates to a manufacturing method which is capable of mass production of (3R,4R)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine on an industrial scale with high quality optical purity, which is a key intermediate necessary for synthesizing tofacitinib.
Preparation method and application of chiral amine B
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, (2019/06/05)
The invention discloses a preparation method of chiral amine B. The preparation method comprises the following steps: (1) carrying out nucleophilic substitution reaction on N-tert-butoxycarbonyl-3-pyridine and halogenated benzyl to obtain an intermediate