AN IMPROVED HIGHLY EFFICIENT PROCESS FOR THE PREPRATION OF NINTEDANIB AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
The present invention relates to an improved highly efficient and economic process for large-scale production of Nintedanib and pharmaceutically acceptable salt thereof. The present invention also relates to a single step process that form highly pure Nintedanib through novel intermediates. In this...
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creator | DHARMESH MAHENDRABHAI, Shah HARSHAD GHANSHYAMBHAI, Kathrotiya ARPIT KIRITBHAI, Patel SAGAR PREMJIBHAI, Kothadiya RAJENDRAKUMAR GOKALBHAI, Chavda MANISH BHIKHABHAI, Karad TUSHAR BHARATKUMAR, Mehta |
description | The present invention relates to an improved highly efficient and economic process for large-scale production of Nintedanib and pharmaceutically acceptable salt thereof. The present invention also relates to a single step process that form highly pure Nintedanib through novel intermediates. In this process, Nintedanib base [I] is prepared in a single step, in-situ process wherein the process is performed by formation of two novel intermediates namely, methyl-1-(bromoacetyl)-2-oxo-2,3-dihydro-1H-indole-6-carboxylate and methyl-(3Z)-1-(bromoacetyl)-3-[methoxy(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate. This process avoids use of expensive and hazardous reagent and solvent such as methyl cyclohexane. Further, there is no isolation and analysis of any intermediate after every step completion that made the process easy to perform without much hurdles. Along with the ease of performance, present invention process also gives high-purity final product with high yield. This makes the process highly cost-effective and time-efficient. |
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The present invention also relates to a single step process that form highly pure Nintedanib through novel intermediates. In this process, Nintedanib base [I] is prepared in a single step, in-situ process wherein the process is performed by formation of two novel intermediates namely, methyl-1-(bromoacetyl)-2-oxo-2,3-dihydro-1H-indole-6-carboxylate and methyl-(3Z)-1-(bromoacetyl)-3-[methoxy(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate. This process avoids use of expensive and hazardous reagent and solvent such as methyl cyclohexane. Further, there is no isolation and analysis of any intermediate after every step completion that made the process easy to perform without much hurdles. Along with the ease of performance, present invention process also gives high-purity final product with high yield. 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subjects | CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES |
title | AN IMPROVED HIGHLY EFFICIENT PROCESS FOR THE PREPRATION OF NINTEDANIB AND PHARMACEUTICALLY ACCEPTABLE SALT THEREOF |
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