MUMBAI, India, Nov. 2 -- Intellectual Property India has published a patent application (202541012821 A) filed by Neuland Laboratories Limited on February 14, 2025, for An Improved Process For The Preparation Of Ensifentrine.
Inventors include Dr. Narendra Kumar Tripathy; Dr. Mallam Venkataiah; Dr. Arupula Sanjeeva Kumar; Mr. Allu Srinivas; and Mr. Morthala Ramesh.
The application for the patent was published on October 30, 2026, under issue no. 44/2026.
Abstract: The present invention relates to an improved process for the preparation of Ensifentrine of Formula-I. which comprises: reacting of 1-(3,4-dimethoxyphenethyl)urea of Formula II with dimethylmalonate of Formula III to obtain 1-(3,4-dimethoxyphenethyl)pyrimidine-2,4,6(1H,3H,5H)-trione of Formula IV; chlorination of compound of Formula-IV to obtain 2-chloro-9,10-dimethoxy-6,7-dihydro-4H-pyrimido[6,1-a]isoquinolin-4-one compound of Formula V; reacting of compound of Formula V with 2,4,6-trimethylaniline of Formula VI to obtain (E)-2-(mesitylimino)-9,10-dimethoxy-2,3,6,7-tetrahydro-4H-pyrimido[6,1-a]isoquinolin-4-one compound of Formula VII; condensation of compound of Formula VII with a compound of Formula IX or salt thereof, to obtain (E)-1-(2-(2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7- dihydro-2H-pyrimido[6,1-a]isoquinolin-3(4H)-yl)ethyl)urea (Ensifentrine) of Formula I; optionally converting the compound of Formula I to its pharmaceutically acceptable salts thereof.
Disclaimer: Curated by HT Syndication.
