MUMBAI, India, Aug. 12 -- Intellectual Property India has published a patent application (202541009019 A) filed by Neuland Laboratories Limited on February 04, 2025, for An Improved Process For The Preparation Of Ivacaftor.
Inventors include Dr. Narendra Kumar Tripathy; Dr. P. Krishnaiah; Dr. N. Venkata Subba Reddy; Mr. Hanuma Kothamasu; Mr. Narender Maroju; Mr. Nagaiah Bollepally; and Mrs. Kapulapalli Anusha.
The application for the patent was published on August 07, 2026, under issue no. 32/2026.
Abstract: The invention discloses an improved process for the preparation of Ivacaftor compound of Formula I. The process comprises: hydrolysis of ethyl 4-oxo-1,4- dihydroquinoline-3-carboxylate KSM-I with a suitable base in the presence of a suitable solvent to obtain a 4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound of Formula IV. Condensation of a 4-oxo-1,4-dihydroquinoline-3-carboxylic acid compound of Formula IV with Pivaloyl chloride in the presence of organic base and solvent to obtain 4-oxo-1,4-dihydroquinoline-3-carboxylic pivalic anhydride compound of Formula IVA. Silylation of 5-amino-2,4-di-tert-butylphenol KSM-II with suitable reagent and base to obtain 2,4-di-tert-butyl-5-((trimethylsilyl)oxy)aniline compound of Formula II. Condensation of 2,4-di-tert-butyl-5-((trimethylsilyl)oxy) aniline compound of Formula II with 4-oxo-1,4-dihydroquinoline-3-carboxylic pivalic anhydride compound of Formula IVA in presence of suitable organic base and solvent to obtain N-(2,4-di-tert-butyl-5-((trimethylsilyl)oxy)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide compound of Formula III. Deprotection of N-(2,4-di- tert-butyl-5-((trimethylsilyl)oxy)phenyl)-4-oxo-1,4-dihydroquinoline-3-carboxamide compound of Formula III with 2N HCl and suitable solvent to obtain Ivacaftor.
Disclaimer: Curated by HT Syndication.
