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
来源：
TETRAHEDRON LETTERS | 2021年 / 67卷
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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