Short enantioselective total synthesis of (+)-tofacitinib

被引:3
|
作者
Mane, Kishor D. [1 ,2 ]
Kamble, Rohit B. [1 ,2 ]
Suryavanshi, Gurunath [1 ,2 ]
机构
[1] Natl Chem Lab, CSIR, Chem Engn & Proc Dev Div, Dr Homi Bhabha Rd, Pune 411008, Maharashtra, India
[2] Acad Sci & Innovat Res, Ghaziabad 201002, India
关键词
L-Proline; Piperidone; Aminohydroxylation; Hydrogenation; FORMAL ASYMMETRIC-SYNTHESIS; ALPHA-AMINOXYLATION; KINASE; INHIBITION; ALDEHYDES;
D O I
10.1016/j.tetlet.2021.152838
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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. (C) 2021 Elsevier Ltd. All rights reserved.
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页数:3
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