Short enantioselective total synthesis of (+)-tofacitinib

TitleShort enantioselective total synthesis of (+)-tofacitinib
Publication TypeJournal Article
Year of Publication2021
AuthorsMane, KD, Kamble, RB, Suryavanshi, G
JournalTetrahedron Letters
Volume67
Pagination152838
Date PublishedMAR
Type of ArticleArticle
ISSN0040-4039
Keywordsaminohydroxylation, Hydrogenation, L-proline, piperidone
Abstract

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.

DOI10.1016/j.tetlet.2021.152838
Type of Journal (Indian or Foreign)

Foreign

Impact Factor (IF)

2.275

Divison category: 
Chemical Engineering & Process Development

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