Patent · US Active

Methods for preparing Nintedanib and intermediates thereof

US10836751B2 · kind B2 · utility

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7Claims

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Inventors

Zeng Li · Pudong New District, CN
Xiaosong Cheng · Shanghai, CN
Xianliang He · Lo Wu, CN
Jicheng Zhang · Shanghai, CN
Luning Huang · Shanghai, CN
Anping Tao · Shanghai, CN
Hong Gu · Dongguan, CN

Key dates

Filing date	Oct 11, 2017
Grant date	Nov 17, 2020
Priority date	—
Expiry date	Oct 11, 2037

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07D209/34
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

Abstract

The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of methyl 4-(1-alkoxy-1,3-dioxo-3-phenyl propan-2-yl)-3-nitrobenzoate (compound IV) and methyl 3-benzoyl-2-oxoindoline-6-formate (compound V). The method for preparing nintedanib (I) provided by the present application has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.