PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF

PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF

A process for the preparation of high purity tofacitinib, which reduces formation of N-methyl impurity is provided. Novel intermediates used in the process to prepare tofacitinib is also provided. A process for the preparation of tofacitinib (I), comprising the steps of: adding cyanoacetic acid in m...

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Hauptverfasser: DESAI, Parimal Hasmukhlal, PATRAVALE, Bharatkumar Surendra, SALUNKE, Chetan Liladhar, POLSHETTY, Nitin Janardhan
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Sprache:eng ; fre ; ger
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CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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creator DESAI, Parimal Hasmukhlal
PATRAVALE, Bharatkumar Surendra
SALUNKE, Chetan Liladhar
POLSHETTY, Nitin Janardhan
description A process for the preparation of high purity tofacitinib, which reduces formation of N-methyl impurity is provided. Novel intermediates used in the process to prepare tofacitinib is also provided. A process for the preparation of tofacitinib (I), comprising the steps of: adding cyanoacetic acid in molar equivalent 0.2-1.2 to compound of formula (IIS), followed by addition of carbodiimide coupling agent of formula (III), optionally reacting tofacitinib base with citric acid is further provided.
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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
title PROCESS FOR THE PREPARATION OF TOFACITINIB AND INTERMEDIATES THEREOF
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