Open AccessAn Efficient Synthesis of 4-Aminomethyl-1-(2-Phenylethyl)-Piperidin-4-ol: A Key Intermediate in Fenspiride HCl Synthesis
Author(s) -
Prasad Panchabhai,
N Kaliaperumal,
Mahesh Gopalakrishnan,
Chinnadurai Anbuselvan
Publication year - 2021
Publication title -
journal of pharmaceutical research international
Language(s) - English
Resource type - Journals
ISSN - 2456-9119
DOI - 10.9734/jpri/2021/v33i51b33523
Subject(s) - reagent , chemistry , yield (engineering) , combinatorial chemistry , environmentally friendly , aqueous solution , hazardous waste , green chemistry , organic chemistry , reaction mechanism , materials science , catalysis , waste management , ecology , engineering , metallurgy , biology
The article confers a scalable manufacturing process of Fenspiride HCl. 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol is the main building block in Fenspiride HCl synthesis. The reported reagents for 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis are costly, explosive, highly toxic, produce hazardous waste, and also need to be handled with most care. The paper introduces aqueous ammonia as an alternate reagent in Fenspiride HCl and used in 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis. The new green chemistry aspect makes the process environment-friendly and cheaper. It also eliminates toxic, sensitive, and hazardous reagents and makes the process safe on uncomplicated on bulk scale production.
The high pure Fenspiride HCl is obtained by following this process and meets the ICH limits with good yield.